CN103432091A - Improved-performance tablet and preparation method thereof - Google Patents

Abstract

The invention discloses an improved-performance tablet which comprises an active component A1, a hydrophilic diluent B1 and a meltable solid dispersion and/or a solid coating C1, wherein the diluent B1 and/or the active component A1 are/is bonded and bridged by the solidified melt of the meltable solid dispersion and/or solid coating C1; and/or the tablet comprises a hydrophilic diluent B2 and a meltable solid dispersion containing an active component A2 and/or a solid coating C2, wherein the diluent B2 is bonded and bridged by the solidified melt of the meltable solid dispersion and/or solid coating C2. The invention also discloses a preparation method of the tablet. The tablet has stronger mechanical performance and/or better weather resistance and/or better hydrophilcity or better disintegration property or better medicine dissolubility and higher porosity.

Description

Tablet of a kind of performance improvement and preparation method thereof

Technical field

The present invention relates to a kind of tablet of performance improvement.More particularly a kind of mechanical performance and/or weatherability and/or hydrophilic and/or drug-eluting and/or/hydrophilic tablet that the performances such as safety are further strengthened.The invention still further relates to the preparation method of this tablet.

Background of invention

Porosity and the mechanical strength of tablet play a very important role at tablet.High porosity is conducive to the medicine in tablet, and especially the stripping of insoluble drug discharges, particularly disintegrate rapidly in oral cavity/or solution tablet.High mechanical strength is conducive to tablet and safeguards its form in the process such as production, transportation, guarantees the accurate of single dosage, thereby guarantees drug safety.

Yet, porosity and mechanical strength are not usually organic unities in same tablet, but conflicting: the porosity that tablet is high usually causes the problems such as mechanical strength deficiency of tablet, as hardness is not high, friability is bad, thereby the quality problems such as drug loading (single dosage) decline, sliver, fragment may appear, and further aggravate the impact on tablet such as dampness, air (oxygen) and light, reduce its stability; And the high mechanical strength of tablet usually causes the porosity deficiency of tablet, the problem such as disintegration of tablet or drug-eluting are slack-off.

In recent years, existing people have invented some and have obtained the tablet of higher porosity by sintering curing (heat fused is cooling curing subsequently) principle.For example, the dissolved in oral cavity matrix agent that Unexamined Patent 11-35451 discloses: active ingredient, saccharide etc. with polyethylene glycols, lipid as lanoline, lanolin alcohol, natural waxes is mixed as low melting points such as Brazil waxs, this mixture low pressure lower sheeting, the tablet of gained is heated at the temperature of this low melting point of melting, natural cooling is feature afterwards the agent of dissolved in oral cavity matrix and manufacture method thereof.More specifically, its right item 1 has been recorded and narrated a kind of Orally dissolving tablet that comprises medicine, sugar, low melting material, it is characterized in that having the loose structure of the bonding bridging between said medicine and sugar by above-mentioned low melting material.Right item 3 has been recorded and narrated above-mentioned low melting material and has been selected from wax, surfactant, PEG and compositions thereof.Right item 8 has been recorded and narrated the preparation method of above-mentioned Orally dissolving tablet, mixes said medicine, sugar, low melting material, and the tablet that heating is made by said mixture makes the low melting material fusing, cooling afterwards.

For another example, US5853758 has disclosed a kind of tablet (a tablet of increased strength) of mechanical strength enhancing of porous: this tablet in the preparation, use lipid as lanoline, lanolin alcohol, natural waxes is as Brazil wax, natural or synthetic polymer is as PEG200～20000, maltodextrin, saccharide is made porogen as the hot melts such as glucose solidify as the volatilization such as handing-over agent or binding agent and ammonium bicarbonate, Camphora or decomposable composition; Its manufacturing process is as follows: (a) active groups of fusible voltinism binding agent, at least one excipient and medicine is combined in tablet, (b) aforesaid fusible voltinism binding agent is made in above-mentioned tablet its fusing reach and (c) make above-mentioned fusible voltinism adhesive.

Two as, WO0247607A2 has disclosed a kind of method for preparing the oral instant preparation, the method is medicine and melting and solidification binding agent (cementing agent), or after selecting other additives to mix, adds in mould or bubble eye again, then heats said mixture and is chilled to proper temperature again and is shaped.

Tablet in above-mentioned technology has higher porosity, mechanical strength has had certain improvement, yet in actual applications, all show to some extent the dissatisfactory shortcoming of mechanical strength, as not high enough as hardness, friability is good not, is prone to the problems such as sliver, fragment in the processes such as production and transport.Its mechanical performance leeway that still has greatly improved.In addition, due to hydrophilic general disclosed in above-mentioned technology, fusible voltinism binding agent fusing point is lower preferably, use the preparation that this fusing point is binding agent fully not being equipped with in the indoor preservation situation of summer air-conditioning equipment, binding agent may melt, the tablet deliquescing, tablet strength and intraoral disintegration time etc. are changed, the ability variation of weatherability or anti-higher temperature.And the relatively high lipophilic fusible voltinism binding agent hydrophilic of fusing point used is bad, above-mentioned preparation disintegrate or the drug-eluting of preparation are relatively slow.Hydrophilic and weatherability are not usually organic unities at this yet, but conflicting.

In addition, someone has disclosed and has a kind ofly contained medicine, diluent and during low saccharide relative to the diluent fusing point is blended in tablet equably than medicine at CN1473036A, between the granule of medicine and/or diluent, form in the oral cavity of crosslinked formation disintegrative tablet and manufacture method thereof rapidly by low-melting saccharide melting and solidification thing.The mechanical performance of the tablet that this technology discloses equally also has larger room for improvement.

On the basis of above-mentioned technology, CN101919822A has disclosed tablet of a kind of improved combination properties and preparation method thereof, the graininess that this tablet comprises active component, water-soluble crystalline state or the diluent of powdered, melting binding agent (water soluble surfactant active), melting mechanical performance improving agent (lipid additive) and/or without pharmaceutically acceptable additive, wherein, above-mentioned diluent and/or above-mentioned active component are by the bonding bridging of solidification of molten thing of above-mentioned binding agent and above-mentioned mechanical performance improving agent.This technology has been done certain improvement to above-mentioned technology, but melting binding agent wherein, melting mechanical performance improving agent and other component are (as active component, the graininess of water-soluble crystalline state or the diluent of powdered and/or without pharmaceutically acceptable additive) directly mixing is together, their major parts by other components (as active component, the graininess of water-soluble crystalline state or the diluent of powdered and/or without pharmaceutically acceptable additive etc.) open or isolate between institute, the two amount directly be in contact with one another and particularly area is very limited---relatively less, therefore melting binding agent, the directly contact and mutually to melt the amount that (melt) close just wherein seldom a part of of melting mechanical performance improving agent, it is less with respect to the total amount of melting binding agent and melting mechanical performance improving agent that the two is formed with the ratio of interaction thing of use, thereby the space that can bring into play very greatly in addition of its effect or performance improvement.In addition, this tablet melting binding agent and local possibility of inconsistent its concentration in other words of the inner concentration possibility of melting mechanical performance improving agent wherein is higher, the concentration part that the interaction thing that the two is formed with use may occur is inconsistent, local most possibility is on the low side or minority is higher, thereby may cause the inner molten point of tablet or weatherability or hydrophilic inconsistent, therefore the aspects such as its mechanical performance, weatherability, hydrophilic also have larger room for improvement.In addition, this technology is just because of above-mentioned reason need to be used melting binding agent (being the water soluble surfactant active) and the melting mechanical performance improving agent (lipotropy melting material) of more amount, yet, the surfactant that more amount is used may affect the safety in utilization of this tablet, because some surfactant has certain toxic and side effects sometimes; The lipotropy melting material that also has more amount to use, when particularly local concentration is higher, may affect the hydrophilic of this tablet.Therefore, both wished in reality that this tablet had good performance, and wished again to use in tablet formulation surfactant and the lipotropy melting material of lower amount, and there is relatively better safety in utilization and hydrophilic, thereby its performance obtains larger improvement.

Special needs to be pointed out is, what above-mentioned all technology of mentioning were focused on is pharmaceutical carrier disintegrate or dissolving fast, and can contained medicine be paid close attention to not by Fast Stripping to it, when contained medicine water solublity is better, medicine can rapider stripping, but when contained medicine water solublity is poor, when particularly its particle is larger, this carrier is little to medicine Fast Stripping role, because of medicine particularly the stripping of the poor medicine of water solublity speed and degree except with the inherent character such as its dissolubility mutually outside the Pass, also state residing with it etc. has than Important Relations, as its particle size and dispersity, particularly the stripping of the poor medicine of water solublity is advantageous particularly to medicine for less particle and good pre-dispersed state, and above-mentioned technology is said nothing this.The drug-eluting performance of the tablet that therefore, above-mentioned technology discloses has larger room for improvement.

Therefore, still need (hydrophilic porous) tablet that performance further improved (or disintegrate rapidly in oral cavity/or solution tablet) in reality.

Point out in passing, turn round and look at Han treasure in " balancing each other and the phasor basis " (BJ University Press, 1991 05 month the 1st edition, the 35th to 37 pages) middle statement: composition-character figure consists of abscissa, take the figure that certain physical property forms as vertical coordinate: the physical property of being measured can be engineering properties (hardness, tensile strength etc.), electrical properties (resistivity, temperature-coefficient of electrical resistance, electric conductance etc.), thermal property (fusing point, Heat of Formation etc.), magnetic property (susceptibility), and proportion, viscosity, lattice paprmeter etc.In a word, may be used to change-character figure of formation group as long as can measure any physical quantity of accurate numerical value.The great many of experiments data shows, in binary system, the variation of composition-character curve has following rule: in two-phase section (or in mechanical impurity district), composition-character curve is a straight line basically; In the solid solution tagma of homogeneous phase, composition-character figure is a u curve; Have in system while not generating from the compound of separating, be equivalent to this compound composition place on composition-character curve, by special point occurring, be referred to as singular point or bifurcation point.But this rule is called Khulna husband rule sometimes.From book, Fig. 2 .31 can know and sees, the solid solution tagma is u curve, and extreme point is arranged, and the performance in mesozone (solid solution tagma) promotes to some extent than two-end-point (monophase field or pure material district).Yet this principle also is not fully utilized in the mechanical performance that improves this tablet and weatherability etc. in (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet).In addition, a large amount of technical literature (as additional reference document 1～11) reports, micron particle (being not more than 100 μ m), submicron particle (being not more than 1 μ m), nanoparticle (being not more than 100nm) be broad research or be applied to composite, it is added to the enhancing of composite for composite, improves mechanical performance.Yet above-mentioned technology also fully is not applied in (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet) improves above-mentioned tablet properties, as improves the mechanical performance of above-mentioned tablet.

Summary of the invention

Purpose of the present invention, just be to provide (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet) of a kind of performance improvement.Specifically, the present invention will reach following any one or a plurality of purposes wherein:

Purpose of the present invention just is to provide: (hydrophilic porous) tablet that a kind of mechanical performance is further strengthened (or disintegrate rapidly in oral cavity/or solution tablet) and preparation method thereof; And/or the person,

(hydrophilic porous) tablet that a kind of weatherability is enhanced (or disintegrate rapidly in oral cavity/or solution tablet) and preparation method thereof; And/or the person,

(hydrophilic porous) tablet that a kind of hydrophilic or disintegrating property or solubility property are enhanced (or disintegrate rapidly in oral cavity/or solution tablet) and preparation method thereof; And/or the person,

(hydrophilic porous) tablet that a kind of drug-eluting performance is enhanced (or disintegrate rapidly in oral cavity/or solution tablet) and preparation method thereof; And/or the person,

(hydrophilic porous) tablet that a kind of security performance is enhanced (or disintegrate rapidly in oral cavity/or solution tablet) and preparation method thereof.

Further, other purposes are shown in following description and embodiment.

In order to achieve the above object, the present inventor conducts in-depth research, found that, the performance of (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet) (as in mechanical performance, hydrophilic, weatherability, drug-eluting performance etc. one or more) has great relation with bonding state or the fusion mode of fusible binding agent and mechanical performance improving agent.

On this basis, the inventor works out (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet) of a kind of performance improvement, and has completed the present invention.

Particularly, on the one hand, the present invention relates to (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet) of a kind of performance improvement, this tablet comprises:

1), at least one active components A 1;

2), at least one pharmaceutically acceptable hydrophilic diluent B 1; And

3), at least one is selected from following fusible adhesion agent C1:

C1-1: at least one fusing point is not less than the fusible solid dispersion I of 25 ℃ of temperature, above-mentioned solid dispersion I contains at least one pharmaceutically acceptable fusing point and is not less than surfactant D 1 25 ℃ of temperature and fusible (fusible binding agent D) and the high medical additive E1(performance enhancers E of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point), perhaps

C1-2: at least one fusing point is not less than the fusible solid dispersion II of 25 ℃ of temperature, above-mentioned solid dispersion II contains at least one fusing point and is not less than the surfactant E2(performance enhancers E that medicinal lipid additive D2 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point are not less than above-mentioned medicinal lipid additive D2), perhaps

C1-3: at least one fusing point is not less than the fusible solid dispersion III of 25 ℃ of temperature, above-mentioned solid dispersion III contain at least one fusing point higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point the hydrophilic surfactant E21(performance enhancers E lower than 25 ℃ of temperature), perhaps

C1-4: at least one fusing point is not less than the fusible solid dispersion IV of 25 ℃ of temperature, above-mentioned solid dispersion IV contain at least one fusing point higher than medicinal lipid additive D21 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point the hydrophilic surfactant E21(performance enhancers E lower than 25 ℃ of temperature), perhaps

C1-5: at least one fusing point is not less than the fusible solid dispersion V of 25 ℃ of temperature, above-mentioned solid dispersion V contains at least one pharmaceutically acceptable fusing point and is not less than the hydrophilic medical additive E2(performance enhancers E that saccharide D3 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point are not less than 25 ℃ of temperature), perhaps

C1-6: at least one fusing point is not less than the fusible solid coating I of 25 ℃ of temperature, above-mentioned solid coating I comprises that fusing point is not less than the fusible outer core core 1(performance enhancers E that covers thing D1 (fusible binding agent D) and be not less than 25 ℃ of temperature by the above-mentioned fusible outer fusing point that covers thing D1 coating of 25 ℃ of temperature), the above-mentioned fusible outer thing D1 that covers comprises at least one pharmaceutically acceptable fusing point and is not less than surfactant D 1 25 ℃ of temperature and fusible, above-mentioned core core 1 comprises the medical additive E3 that at least one pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, perhaps,

C1-7: at least one fusing point is not less than the fusible solid coating II of 25 ℃ of temperature, above-mentioned solid coating II comprises that fusing point is not less than the fusible outer core core 2(performance enhancers E that covers thing D2 (fusible binding agent D) and be not less than 25 ℃ of temperature by the above-mentioned fusible outer fusing point that covers thing D2 coating of 25 ℃ of temperature), the above-mentioned fusible outer thing D2 that covers comprises at least one pharmaceutically acceptable fusing point and is not less than saccharide D3 25 ℃ of temperature and fusible, above-mentioned core core 2 comprises the hydrophilic medical additive E4 that at least one pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, perhaps,

C1-8: the solid dispersion VI of the further combination in any of solid dispersion in above-mentioned fusible adhesion agent C1-1～C1-5, or,

C1-9: the mixture of two or more in above-mentioned fusible adhesion agent C1-1～C1-8;

And above-mentioned diluent B 1 and/or above-mentioned active components A 1 are by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C1;

(and the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (I～VI) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (I～II) is not more than 100 μ m; )

And/or

This tablet comprises:

1), at least one pharmaceutically acceptable hydrophilic diluent B 2;

2), at least one is selected from following fusible adhesion agent C2:

C2-1: at least one fusing point is not less than the fusible solid dispersion VII of 25 ℃ of temperature, above-mentioned solid dispersion VII contains fusible binding agent D1 (fusible binding agent D) and and at least one active components A 2(performance enhancers E that at least one fusing point is not less than 25 ℃ of temperature), above-mentioned fusible binding agent D1 comprises that at least one pharmaceutically acceptable fusing point is not less than surfactant D 1 25 ℃ of temperature and fusible and/or at least one pharmaceutically acceptable fusing point is not less than saccharide D3 25 ℃ of temperature and fusible, and/or

C2-2: at least one fusing point is not less than the fusible solid coating III of 25 ℃ of temperature, above-mentioned solid coating III comprises that fusing point is not less than 25 ℃ of temperature fusible outer cover thing D3 (fusible binding agent D) and by the above-mentioned fusible outer core core 3(performance enhancers E that thing D3 coats that covers), the above-mentioned fusible outer thing D3 that covers comprises at least one pharmaceutically acceptable fusing point and is not less than surfactant D 1 25 ℃ of temperature and fusible, and/or at least one pharmaceutically acceptable fusing point is not less than saccharide D3 25 ℃ of temperature and fusible, above-mentioned core core 3 comprises at least one active components A 2,

And, above-mentioned diluent B 2 by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C2 (;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (VII) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (III) is not more than 100 μ m).

On the other hand, the invention still further relates to the preparation method of above-mentioned tablet, the method comprises:

(1), be selected from the operation of the fusible adhesion agent C1 of following preparation and/or C2:

Make to comprise at least one pharmaceutically acceptable fusing point and be not less than surfactant D 1 25 ℃ of temperature and fusible (fusible binding agent D) and the high medical additive E1(performance enhancers E of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point) supplementary material form the fusible solid dispersion I that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-1, perhaps

Make to comprise at least one fusing point and be not less than the surfactant E2(performance enhancers E that medicinal lipid additive D2 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point are not less than above-mentioned medicinal lipid additive D2) supplementary material form the fusible solid dispersion II that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-2, perhaps

Make to comprise at least one fusing point higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point the hydrophilic surfactant E21(performance enhancers E lower than 25 ℃ of temperature) supplementary material form the fusible solid dispersion III that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-3, perhaps

Make to comprise at least one fusing point higher than medicinal lipid additive D21 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point the hydrophilic surfactant E21(performance enhancers E lower than 25 ℃ of temperature) supplementary material form the fusible solid dispersion IV that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-4, perhaps

Make to comprise at least one pharmaceutically acceptable fusing point and be not less than the hydrophilic medical additive E2(performance enhancers E that saccharide D3 25 ℃ of temperature and fusible (fusible binding agent D) and at least one pharmaceutically acceptable fusing point are not less than 25 ℃ of temperature) supplementary material form the fusible solid dispersion V that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-5, perhaps

What make at least one fusing point be not less than 25 ℃ of temperature covers that thing D1 (fusible binding agent D) is outer is overlying on the core core 1(performance enhancers E that fusing point is not less than 25 ℃ of temperature fusible outward) form the fusible solid coating I that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-6, the above-mentioned fusible outer thing D1 that covers comprises at least one pharmaceutically acceptable fusing point and is not less than surfactant D 1 25 ℃ of temperature and fusible, above-mentioned core core 1 comprises the medical additive E3 that at least one fusing point is not less than 25 ℃ of temperature, perhaps

What make at least one fusing point be not less than 25 ℃ of temperature covers that thing D2 (fusible binding agent D) is outer is overlying on the core core 2(performance enhancers E that fusing point is not less than 25 ℃ of temperature fusible outward) form the fusible solid coating II that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C1-7, the above-mentioned fusible outer thing D2 that covers comprises at least one pharmaceutically acceptable fusing point and is not less than saccharide D3 25 ℃ of temperature and fusible, above-mentioned core core 2 comprises the hydrophilic medical additive E4 that at least one fusing point is not less than 25 ℃ of temperature, perhaps

Make the further combination in any formation of the solid dispersion solid dispersion VI in above-mentioned fusible adhesion agent C1-1～C1-5 obtain fusible adhesion agent C1-8, or,

Make two or more in above-mentioned fusible adhesion agent C1-1～C1-8 be mixed to get fusible adhesion agent C1-9;

And/or

Make to comprise at least one active components A 2(performance enhancers E) and at least one fusing point supplementary material of being not less than the fusible binding agent D1 (fusible binding agent D) of 25 ℃ of temperature form the fusible solid dispersion VII that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C2-1, above-mentioned fusible binding agent D1 comprises that at least one pharmaceutically acceptable fusing point is not less than surfactant D 1 25 ℃ of temperature and fusible and/or at least one pharmaceutically acceptable fusing point is not less than saccharide D3 25 ℃ of temperature and fusible; And/or

Make at least one fusing point be not less than the fusible outer outer core core 3(performance enhancers E that is overlying on of thing D3 (fusible binding agent D) that covers of 25 ℃ of temperature) form the fusible solid coating III that fusing point is not less than 25 ℃ of temperature and obtain fusible adhesion agent C2-2, the above-mentioned fusible outer thing D3 that covers comprises that at least one pharmaceutically acceptable fusing point is not less than surfactant D 1 25 ℃ of temperature and fusible and/or at least one pharmaceutically acceptable fusing point is not less than saccharide D3 25 ℃ of temperature and fusible, and above-mentioned core core 3 comprises at least one active components A 2;

(and the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (I～VII) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (I～III) is not more than 100 μ m; )

(2) the tablet supplementary material that, makes to comprise described active components A 1, described diluent B 1, described fusible adhesion agent C1 mixes and makes it to have the operation of pharmaceutically acceptable tablet spatial shape;

And/or

Make the tablet supplementary material that comprises described diluent B 2, described fusible adhesion agent C2 mix and make it to there is the operation of pharmaceutically acceptable tablet spatial shape;

(3) the tablet form thing that, will be obtained by operation (2) is heated to the melt temperature of the melting composition in above-mentioned fusible adhesion agent C1 and/or C2 or the operation that above temperature makes its fusing;

(4), by the operation of the melting composition cooled and solidified in the above-mentioned fusible adhesion agent C1 melted in the tablet form thing that operation (3) obtain and/or C2.

The term " tablet " that the present invention uses refer to containing the flat or top and bottom of making through pressurization or other non-pressurised techniques of one or more active component a little each composition of inside of disc-shaped, bar-shaped a, shape, ball shape, bulk, taper or other pharmaceutically acceptable shapes of projection disperse basic main for for oral administration, solid dosage forms that also can external and further process on this basis capsule and other the pharmaceutically acceptable dosage forms of making uniformly, in the present invention, " tablet " is preferably rapidly disintegrate in oral cavity/or solution tablet.

The term that the present invention uses " disintegrate rapidly oral cavity in/or solution tablet " refers to while taking and do not absorb water, in oral cavity basically only with saliva in 1 minute with interior (preferably approximately in 30 seconds, more preferably approximately in 10 seconds) disintegrate/or the tablet of dissolving.

The term " porous " that the present invention uses refers to the cellular structure of tablet, and (usually) its porosity is approximately 10 to approximately 95%, and what be satisfied with is approximately 20 to approximately 80%, and more satisfied is approximately 30 to about 60% the meaning.

The term " porosity (Porosity) " that the present invention uses refers in tablet the long-pending ratio with the tablet volume of the shared visitor in space between microgranule inner pore and microgranule, and (usually) means with percent.

The term " fusing point " that the present invention uses refers to that material is converted into liquid temperature from solid-state, when fusing point means with melting range, when particularly relatively the fusing point of two kinds of materials is big or small, be the arithmetic mean of instantaneous value (midrange) that refers in particular to threshold value and the end point values of melting range in the present invention.

The term " fusible " that the present invention uses refers to that substance is not higher than 150 ℃ of temperature, especially not higher than 120 ℃ of temperature, and the meaning particularly do not melted under the condition higher than 100 ℃ of temperature.

The term " performance enhancers " that the present invention uses refers to and can improve solid-state fused mass or tablet properties as one or more performances in mechanical performance, hydrophilic or weatherability, particularly improve mechanical performance as improved hardness (Hardness), hot strength (tensile strength) or ejection force (Ejection Force), the material of the broken degree of Jiang Di Wei (Friability) etc.

The term " mechanical performance parameter " that the present invention uses refers to the parameter of the mechanical performance of reflection tablet, includes but not limited to hardness (the broken degree of Hardness), Wei (Friability), hot strength (tensile strength), ejection force (Ejection Force).

The term that the present invention uses " hydrophilic () " or " hydrophilic () " refer to that balance meltage or the dispersion amount of material in water (25 ℃ of temperature) is not less than 5mg/1ml (solvency or dispersate/water), preferably be not less than 10mg/1ml, more preferably be not less than 33mg/1ml, more preferably be not less than 100mg/1ml (solvency or dispersate/water), be not less than best 500mg/1ml (solvency or dispersate/water), above-mentioned balance meltage or dispersion amount be during lower than 5mg/1ml, think to be insoluble to or be not scattered in water or " lipotropy () "; And/or, the HLB value that refers to surfactant is not less than 10, the HLB value is less than 10 surfactant and thinks " lipotropy () surfactant ", HLB is not less than 10 surfactant and thinks " hydrophilic () surfactant ".

The term that the present invention uses " dissolve in or be scattered in water " or " water solublity " refer to that balance meltage or the dispersion amount of material in water (25 ℃ of temperature) is not less than 33mg/1ml (solvency or dispersate/water), preferably be not less than 100mg/1ml (solvency or dispersate/water), more preferably be not less than 200mg/1ml (solvency or dispersate/water), be not less than best 500mg/1ml (solvency or dispersate/water).

Term " active component ", " bioactive ingredients ", " medical active component ", " active matter ", " activating agent " that the present invention uses reaches " bioactive substance ", " medicine " etc. and refers to that any material has detectable biological effect and comprises any physiological, diagnosis, preventative or pharmacological effect when it bestows live body.This term is intended to include but not limited to material any pharmacy, therapeutic, preventative, the threpsology.

The term that the present invention uses " solid dispersion (/ or body) " refer to that one or more materials are scattered in the another kind of material dispersion existed mutually with continuous solid body with the formation of one or more discontinuous (solid and/or liquid) phase usually, usually there is relatively strict " discontinuous phase " (or title " is dispersed mutually or the dispersate phase ") and " continuous phase " (or title " dispersant phase "), and the two all can contact with other solid phases (or " third phase "), do not have strict " foreign minister " and " interior phase " minute.

The term " solid coating " that the present invention uses refers to that one or more solid-phase materials (outward) are coated on the material dispersion of one or more solids (and/or liquid) phase material, usually have relatively strict " foreign minister " and " interior phase " minute, " foreign minister " be " continuous phase " normally, " interior phase " can be that " discontinuous phase " (a plurality of core core) can be also " continuous phase " (single core core), usually only has " foreign minister " to contact with other solid phases (or " third phase ").

The term that the present invention uses " comprises " and reaches " containing " and refer to and include but not limited to or can also comprise other one-tenth similar implication of grading except this thing.

The term " a kind of " that the present invention uses refer to be at least a kind of, can be a kind of for only having, can be also two or more.

" pharmaceutically acceptable () that the present invention relates to " or " medicinal () " refer to and can be mixed with each other in preparation and mutually can not reduce preparation stability and/or effect without illeffects and be applicable to part or the meaning of whole body administration.

The invention specific embodiment

One, diluent (B)

The diluent (B) used as the present invention, can be water insoluble (its definition sees above), but be preferably hydrophilic (its definition sees below), better is water soluble (its definition sees above), this diluent should be easy to be shaped to process, and tablet should disintegrate or dissolving rapidly in oral cavity while making tablet.For diluent of the present invention normally graininess or powdered, be preferably crystalline state or unformed (state) granule and/or powder, more preferably, be particulate matter or the powder of crystalline state, be prismatic crystal shape granule and/or powder best.The graininess of crystalline state or the diluent of powdered are conducive to improve the mechanical performance of tablet for the present invention, because it has relatively high mechanical performance, particularly with respect to unformed powder.Water-soluble or hydrophilic diluent is conducive to itself and hydrophilic fusible binding agent affinity or adhesion, is conducive to improve the mechanical performance of tablet.

The example (but being not limited to this) that can be used for diluent of the present invention as: medicinal (preferred hydrophilic or more preferably water miscible tasteless) inorganic compound class is (as inorganic salts, the inorganic oxide class) diluent, saccharide or carbohydrate diluent, (preferred hydrophilic or more preferably water miscible) pharmaceutically acceptable cyclodextrin diluent, (preferably preferred hydrophilic or more preferably water miscible) (tasteless or be sweet or delicate flavour) aminoacid, (preferred hydrophilic or more preferably water miscible) (tasteless or be sweet or delicate flavour) edible peptide, the aminoacid that (preferred hydrophilic or more preferably water miscible) (tasteless or be sweet or delicate flavour) is acid or alkaline or the pharmaceutical salts of edible peptide, and their mixture, wherein saccharide (or carbohydrate) or inorganic salts diluent are preferred, wherein saccharide (or carbohydrate) is for more preferably.

Can be used for saccharide of the present invention or the carbohydrate diluent includes, but are not limited to this: monosaccharide or (reaching) its sugar alcohol, oligosaccharide (2～9 sugar) or (reaching) its sugar alcohol, polysaccharide, and their mixture.

Can be used for monosaccharide or (reaching) its sugar alcohol of making diluent of the present invention, the monosaccharide and the sugar alcohol thereof that comprise left-handed and/or dextrorotation, and (in water not from neutrality or the nonionic separated) derivant, as its derivant that methylates, methylolation derivant, hydroxyethylation derivant, hydroxypropylation derivant, hydroxyl butylation or their mixed group derivant (being derivant after hydrogen (atom) in the hydroxyl in the monosaccharide molecular structure is replaced by methyl, methylol, ethoxy, hydroxypropyl, hydroxyl butyl or their mixed group).Its preferred embodiment includes but not limited to: triose (as D-glyceraldehyde (3g:100m (18 ℃), mp145 ℃) and dihydroxy acetone (mp75-80 ℃. dimer, 1g:1ml.Single aggressiveness, soluble in water)), tetrose (as erythritol ((the about 61%w/w of saturated solution) soluble in water, mp121 ℃)), pentose is (as (water-soluble as D-ribose, mp87 ℃), ribitol (very easily water-soluble, mp102 ℃), D-2-deoxyribose (water-soluble, mp91 ℃), D-xylose (1g:0.8ml, mp144 ℃), (L-) arabinose (1g:1ml, mp157-160 ℃)), 1,2,3,4,5-pentanepentol (the D-type, mp103 ℃, very easily water-soluble; The L-type, mp102 ℃, very easily water-soluble; The DL-type, mp105-106 ℃.), xylitol (steady type: mp93-94.5 ℃, 64.2g:100ml, metastable type: mp61-61.5 ℃ .)), hexose is (as glucose (mp83 ℃, 1g:1ml.), galactose (D-galactose, mp167 ℃, saturated solution 68%w/w), galactitol (mp188-189 ℃, 1g:30ml), mannitol (mp166-168 ℃, 1g:5.5ml), mannose (mp133 ℃, 1g:0.4ml), inosite (inositol) (mp225-227 ℃, 14g:100ml), rhamnose (α-Rhamnose, 1 hydrate, mp82-92 ℃, β-Rhamnose, mp122-126 ℃, water-soluble), altrose (water-soluble .mp103-105 ℃), allose (water-soluble, mp128-128.5 ℃), ketohexose (as fructose (dec103-105 ℃, 1g:0.3ml), sorbose (mp165 ℃, very easily water-soluble) or sorbitol (1g:0.45ml, very easily water-soluble (up to83%), mp110-112 ℃), Tagatose (D-Tagatose, 1g:0.7ml (58%w/w, at21 ℃), mp131-133 ℃), lyxose (D-Lyxose, very easily water-soluble, mp106-107 ℃), heptose is (as D-mannoheptulose (Mannoheptulose, mp151-152 ℃, water-soluble), Perseitol (perseitol), D-sedoheptulose (sedoheptulose)), other sugar for example: chalcose (Chalcose, mp96-99 ℃), Quinovose (Quinovose, mp146 ℃, water-soluble), cymarose (cymarose, 2,6-Dideoxy-3-O-methyl-ribo-hexose, mp93-94 ℃, water-soluble), fucose (L/D-Fucose, 6-Deoxy-D-galactose, water-soluble, mp144 ℃), gluconolactone (dec153 ℃, 59g:100ml), 2-ethoxy-D-erythrose, 3-methyl-glucose, 3-hydroxypropyl-L-arabinose, 4-hydroxyl butyl-galactose, and the mixture of above-mentioned sugar.

Can be used for oligosaccharide (2～9 sugar) or (reaching) its sugar alcohol of making diluent of the present invention, comprise equal oligosaccharide and heterooligosaccharide, and their (in water not from neutrality or the nonionic separated) derivant, as its methyl-derivatives, hydroxymethyl derivative, hydroxyethyl derivative, hydroxypropyl derivatives, hydroxyl butyl or their mixed group derivant (be in the oligosaccharide molecular structure hydrogen in the hydroxyl on sugar unit (atom) by methyl, methylol, ethoxy, hydroxypropyl, hydroxyl butyl or their mixed group replace rear derivant) and lactone, the above-mentioned oligosaccharide and the derivant thereof that preferably by 2-6 monosaccharide residue, are formed, type and not restriction of combination to the monosaccharide residue that forms oligosaccharide.In fact such as, but not limited to this: disaccharidase is (as lactose or lactose, (alpha-lactose monohydrate, 1g:5ml, mp201-202 ℃, beta lactose, 1g:2.2ml (15 ℃), the preferably spray drying lactose), sucrose (1g:0.5ml, Dec160-186 ℃. preferably its sugar pill is (as Non-pareil, non-pareil seeds, Nu-Core, Nu-Pareil PG, sacchari sphaerae, sugar seeds, Suglets.), compressible sugar (Compressuc, Comprima, Di-Pac, Nu-Tab.)), cellobiose (cellobiose, 1g:8ml), 6-(.alpha.-D-galactosido)-D-glucose. (melibiose, Dihydrate, mp84-85 ℃, 1g:0.4ml), Sargassum (two) sugar (trehalose, Dihydrate, mp96.5-97.5 ℃, water-soluble), lactitol (Lactitol, mp146 ℃, 1in1.75of water at20 ℃, 1in1.61at30 ℃, 1in1.49at40 ℃, 1in1.39at50 ℃, monohydrate, Non-hygroscopic, mp94-97 ℃, 206g:100ml, dihydrate, mp75 ℃, 140g:100ml), maltose (mp120-125 ℃, soluble in water, monohydrate, mp102-103 ℃, water-soluble), maltose alcohol (mp148-151 ℃, 1g:0.67ml at20 ℃, 1g:0.48ml at40 ℃), dextrinose (120 ℃ of fusing points, soluble in water), hydroxyl isomaltulose (Isomalt, isomer 1, the mixture of 6-GPS and 1,1-GPM, MP, 141 161 ℃ of – for a1:3mixture of1,1-GPM and1,6-GPS, 166 168 ℃ of – for1,6-GPS, 168 171 ℃ of – for1,1-GPM.Solubility:Isomalt galenlQ720,20 ℃: approximately 25%, 30 ℃: approximately 30%, 40 ℃: approximately 40%, Isomalt galenlQ721,20 ℃: approximately 40%, 30 ℃: approximately 50%, 40 ℃: approximately 60%), isomaltulose (Isomaltulose, monohydrate, mp122-124 ℃, soluble in water, in the time of 20 ℃, be 38.4%, in the time of 40 ℃, be 78.2%, 60 ℃ is 133.7%,), lactulose (Lactulose, saturated solution 76.4%w/w (30 ℃), mp 168-171 ℃, Laxative.), 6-(.beta.-D-xylosido)-D-glucose. (Primeverose, mp209-210 ℃, water-soluble), 6-O-.alpha.-L-rhamnosyl-D-glucose. (Rutinose, softensaround140 ℃, dec189-192 ℃. soluble in water), turanose (Turanose, Dec157 ℃. very easily water-soluble .), vicianose (Vicianose, dec210 ℃, soluble in water), trisaccharide is (as Raffinose (Raffinose, mp80 ℃ of .The anhydrous form dec118-119 ℃, 1g:7ml), cellotriose (cellotriose), melezitose (Melezitose, Dihydrate, 110 ℃ of dehydration .When anhydr, mp153-154 ℃. water-soluble), tetrose is (as stachyose (stachyose), cellotetrose (cellotetraose/cellotetrose)), pentasaccharides is (as verbascose (verbascose, Needles, mp219-220 ℃), maltopentaose, cellopentaose (pentosaccharide)), six to nine sugar are (as Fructus Hordei Germinatus six to nine sugar, fiber six to nine sugar), (2) methyl-maltose, hydroxyl butyl-lactose, methylol-sucrose, hydroxypropyl-cellopentaose, ethoxy-sweet seven sugar, hydroxypropyl-Fructus Hordei Germinatus nine sugar, gluconolactone, and their mixture.

Above-mentioned soluble in water or very easily water-soluble monosaccharide, oligosaccharide (2～9 sugar) or (reaching) their sugar alcohol are for most preferably.

Can be used for the polysaccharide of making diluent of the present invention, comprise in its water not from separating or the nonionic derivant, as its derivant that methylates, the methylolation derivant, the hydroxyethylation derivant, the hydroxypropylation derivant, the derivant of hydroxyl butylation or their mixed group replacement (be in the polysaccharide molecule structure hydrogen in the hydroxyl on sugar unit (atom) by methyl, methylol, ethoxy, hydroxypropyl, derivant after hydroxyl butyl or their mixed group replace) reach (neutrality or nonionic) polysaccharide, (usually) selects the mentioned component of (on average) molecular weight low 20000, preferably (on average) molecular weight is lower than 10000 mentioned component, more preferably water-soluble, oligosaccharide (10～100 (preferably 10～50, sugar) and (in water not from neutrality or the nonionic separated) derivant more preferably 10～20).Its available reality such as, but not limited to this: dextrates (Dextrates), oligofructose (as the degree of polymerization 10～100, preferably 10～50, more preferably 10～20), oligomeric isomaltose (as the degree of polymerization 10～100, preferably 10～50, more preferably 10～20)), reduced isomaltooligosaccharide (as the degree of polymerization 10～100, preferably 10～50, more preferably 10～20)), dextrin, glucosan (as molecular weight be 1200～10000 glucosan, the glucosan that preferred molecular weight is 1200～2000), sucrose-dextrin mixture, sucrose-Nulomoline mixture, maltodextrin, pulullan polysaccharide, Tragacanth, starch (preferred water soluble starch), pregelatinized Starch, modified starch, microcrystalline Cellulose, silicified microcrystalline cellulose, the micropowder cellulose, cellulose acetate, carboxymethylcellulose calcium, hydroxyl second methylcellulose, hydroxyethyl-cellulose (product as following as trade name: WP02, WP and QP09, WP and QP3, WP and QP40, WP and QP300), hydroxypropyl cellulose (product as following as trade name: Klucel JF, Klucel LF, Klucel EF), hydroxypropyl methylcellulose (product as following as trade name: Methocel K100Premium LVEP, Methocel F50Premium, Methocel E3Premium LV, Methocel E5Premium LV, Methocel E6Premium LV, Methocel E15Premium LV, Methocel E50Premium LV, low viscosity level Metolose60SH, low viscosity level Metolose65SH, low viscosity level Metolose90SH), methylcellulose (product as following as trade name: A15-LV), and their mixture.

Above-mentioned monosaccharide or (reaching) its sugar alcohol and/or oligosaccharide and to make polysaccharide or other combination of polymers results of use of disintegrating agent better, select in other words the compositions that contains monosaccharide or its sugar alcohol, oligosaccharide or its sugar alcohol or their mixture and disintegrating agent and/or can not form the sweller of strong gel, existing good water-soluble is good aqueous dispersion or disintegrative again, the two (above-mentioned monosaccharide or (reaching) its sugar alcohol and/or above-mentioned other compositions of Gua Tang ︰) use amount proportioning (weight ratio) is generally 1 ︰ 0.05～0.5, is preferably 1 ︰ 0.1～0.3.Some available examples are

r (from RoquetteAmerican, the spray drying solid that contains 15% corn starch and 85% alpha-lactose monohydrate of Inc.),

r (lactose monohydrate-microcrystalline Cellulose) is (as MicroceLac100, from Meggle excipients& The spray drying solid that contains 75% alpha-lactose monohydrate and 25% microcrystalline Cellulose of technology) and

r (lactose monohydrate-micropowder cellulose) is (as Cellactose80, from Meggle excipients& The material of the common drying that the spray-dired compound be comprised of 75% alpha-lactose monohydrate and 25% cellulose powder of technology), Advantose FS95Fructose(is 95% fructose and 5% starch), Ludipress LCE (lactose monohydrate-Povidone).

Can be used for (water solublity or hydrophilic pharmaceutically acceptable) of the present invention cyclodextrin diluent, include but not limited to this: water solublity or hydrophilic pharmaceutically acceptable cyclodextrin are (as alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin) and the hydroxyl carbon number be C1～C4 alkyl derivative, monosaccharide or oligosaccharyl derivant, methyl (as single or two methyl) derivant, sulphur butyl (ether) derivant (be in the cyclodextrin molecular structure in the hydroxyl on sugar unit or hydroxyl hydrogen (atom) by the hydroxyl carbon number, be C1～C4 alkyl, list or oligosaccharide glycosyl, methyl, derivant after the sulphur butyl replaces), water-soluble low-molecular-weight is (lower than 20000, more preferably lower than 10000) (in water not from neutrality or the nonionic separated) cyclodextrin.Its preferred embodiment as, but be not limited to this: alpha-cyclodextrin (1g:7ml (20 ℃)), beta-schardinger dextrin-(1g:50ml (20 ℃)), gamma-cyclodextrin (1g:4.4ml (20 ℃)), (one/or two/or three) methyl-(α-/or β-/or γ-) cyclodextrin is (as 2,6 DM-β-CD (1g:1.75ml), TM-β-CD (1g:3.2ml)), (2-/or 3-) hydroxypropyl-(α-/or β-/or γ-) cyclodextrin is (as 2/3-HP-β-CD, 1g:0.43ml), (2-/or 3-) the hydroxyl butyl-(α-/or β-/or γ-) cyclodextrin (very easily water-soluble), (2-/or 3-) hydroxyethyl-(α-/or β-/or γ-) cyclodextrin (as, 2-HE-β-CD, 1g:2ml), (2-/or 3-) hydroxyl cyclobutenyl (ether)-(α-/or β-/or γ-) cyclodextrin is (very easily water-soluble, as HBe-β-CD, saturated solution >=50%), (one/or two/or three) glucosyl group-(α-/or β-/or γ-) cyclodextrin (easy or very easily water-soluble), (one/or two/or three) malt-base-(α-/or β-/or γ-) cyclodextrin is (easy or very easily water-soluble, as malt-base-alpha-cyclodextrin (1g:2.32ml)), (one/or two/or three) galactosyl-(α-/or β-/or γ-) cyclodextrin (easy or very easily water-soluble), (one/or two/or three) the Pyrusussuriensis glycosyl-(α-/or β-/or γ-) cyclodextrin (easy or very easily water-soluble), (one/or two/or three) mannose group-(α-/or β-/or γ-) cyclodextrin (easy or very easily water-soluble), malt-base-(α-/or β-/or γ-) Beta-cyclodextrin-based-glucose (easy or very easily water-soluble), other monosaccharide (containing sugar alcohol) base-(α-/or β-/or γ-) cyclodextrin (easy or very easily water-soluble), (polysaccharide) side chain-((α-/or β-/or γ-)) cyclodextrin (and as glucosyl group-malt-base-(α-/or β-/or γ-) cyclodextrin, Fructus Vitis viniferae two/or three glycosyls-(α-/or β-/or γ-) cyclodextrin, Fructus Hordei Germinatus two/or three glycosyls-(α-/or β-/or γ-) cyclodextrin) (soluble in water), sulphur butyl (ether)-(α-/or β-/or γ-) cyclodextrin and salt thereof is as sodium salt, (compressibility is good for potassium salt, 1g:2ml), and composition thereof.Above-mentioned soluble in water or very easily water-soluble cyclodextrin diluent is for most preferably.

Can be used for the preferred tasteless pharmaceutical salts of medicinal inorganic compound class of the present invention (as salt, oxide) diluent, more preferably slightly molten, slightly soluble or very slightly soluble tasteless pharmaceutical salts, more more preferably slightly molten, slightly soluble or very slightly soluble medicinal calcium salt and magnesium salt, most preferably slightly molten, slightly soluble or very slightly soluble medicinal calcium salt.The example that can be used for medicinal (preferred water dissolubility or hydrophilic tasteless) inorganic salts salt diluent of the present invention and medicinal inorganic oxide diluent includes but not limited to sodium chloride, potassium chloride, calcium carbonate, calcium sulfate, barium sulfate, calcium bisulfate, calcium phosphate, calcium hydrogen phosphate, calcium glycerophosphate, aluminium silicate, Aluminum calcium silicate., calcium lactate, magnesium carbonate, magnesium oxide, magnesium silicate, magnesium trisilicate, silicon dioxide, aluminium oxide, zinc oxide, titanium dioxide, white carbon black, attapulgite, the soap clay, kaolin, Muscovitum, Talcum and composition thereof.The inorganic diluents preferred embodiment as, but be not limited to this: sodium chloride, magnesium carbonate, magnesium oxide, calcium carbonate, calcium sulfate dihydrate, calcium bisulfate, calcium phosphate, calcium hydrogen phosphate, calcium glycerophosphate, aluminium silicate, Aluminum calcium silicate., kaolin, silicon dioxide, Pulvis Talci, calcium lactate, and their hydrate, and their mixture, wherein, calcium phosphate, calcium hydrogen phosphate, calcium glycerophosphate are for most preferably.

The pharmaceutical salts that can be used for pharmaceutical salts preferred water dissolubility or hydrophilic tasteless or aminoacid that be sweet or delicate flavour and acidity or the basic amino acid of the aminoacid of making diluent of the present invention and acidity or basic amino acid, the example as, but be not limited to this: (L and/or D-) cystine, (D-) tyrosine, aspartic acid and salt thereof are as pharmaceutically acceptable sodium salt, glutamic acid and pharmaceutical salts thereof are as sodium salt, (D-) tryptophan, (L and/or D-) threonine, (D-) leucine, (D-) phenylalanine, (D-) methionine, (D-) isoleucine, (L and/or D-) histidine, (L and/or D-) serine, (D-) valine, (L and/or D-) alanine, glycine, (L and/or D-) hydroxyproline, (L and/or D-) proline, (D-) lysine and pharmaceutical salts thereof, (D-) arginine and pharmaceutical salts thereof, (L and/or D-) glutamine, (D-) agedoite, and their mixture, the pharmaceutical salts of water-soluble or soluble in water or very easily water-soluble tasteless or aminoacid that be sweet or delicate flavour and acidity or basic amino acid is for more preferably, the example as, but be not limited to this: D-methionine, D-phenylalanine, L-Histidine, Serine, L-glutaminate, ALANINE, L-threonine, glycine, L-hydroxyproline, L-PROLINE, and their mixture, the pharmaceutical salts of soluble in water or very easily water-soluble tasteless or aminoacid that be sweet or delicate flavour and acidity or basic amino acid is for most preferably, the example as, but be not limited to this: L-threonine, ALANINE, glycine, L-hydroxyproline, L-PROLINE, particularly ALANINE, glycine, and their mixture.

Can be used for (water solublity or hydrophilic tasteless or be sweet or delicate flavour) edible peptide and edible acidity or basic peptide pharmaceutical salts of making diluent of the present invention, its source is generally the degradation product of food proteins (as hydrolysis, zymolysis, enzymolysis) or synthetic (substituting) thing of its further separator or these degradation products or its separator, be those food source property peptides that derive from directly or indirectly animal food or plant food protein, comprise (water solublity or hydrophilic tasteless or be sweet or delicate flavour) edible dipeptides, edible tripeptides and above peptide, and the pharmaceutical salts of acidity or basic peptide, and their mixture, the edible peptide can be selected 2～100 peptides, general preferred edible 2～10 peptides, edible 2～6 peptides more preferably, more preferably edible 2-3 peptide, comprise its neutral peptide, acidity peptide and basic peptide and pharmaceutical salts thereof.

Edible dipeptides or tripeptides preferably comprise L and/or D-Thr, L and/or D-alanine, glycine, L and/or D-hydroxyproline, L and/or D-PROLINE, L and/or D-Lys and pharmaceutical salts thereof, the dipeptides of L and/or D-Arg and pharmaceutical salts thereof or tripeptides, as by (L and/or D-) threonine, (L and/or D-) alanine, glycine, (L and/or D-) hydroxyproline, (L and/or D-) proline, (L and/or D-, preferred D-) lysine and pharmaceutical salts thereof, (L and/or D-, preferred D-) arginine and pharmaceutical salts thereof each other (comprising that self is as glycylglycine) and/or with other amino acids formed dipeptides or tripeptides, because this has preferably dissolubility or stability (improving the amino acid whose dissolubility of water solublity or poor stability or stability) or sense of taste (as correlation technique US5432160, DE3108079C2, done discussion in EP0087751A1 and EP0087750B1) and more easily absorb.More particularly, preferably the dipeptides example is as A-X, X-A, preferably the tripeptides example is as X '-A-X, X '-X-A, A-X '-X, wherein, A is selected from any (natural) aminoacid, preferred essential amino acid, the low essential amino acid of unstable or water-soluble particularly, as glutamine, tyrosine, tryptophan, methionine, valine, leucine, isoleucine, phenylalanine, X and X ' are selected from (L and/or D-) threonine, (L and/or D-) alanine, glycine, (L and/or D-) hydroxyproline, (L and/or D-) proline, (L and/or D-, preferred D-) lysine and pharmaceutical salts thereof, (L and/or D-, preferred D-) arginine and pharmaceutical salts thereof, preferably use ALANINE and glycine.Some dipeptides or tripeptides instantiation are as glycylalanine, carnosine (alanyl-histidine, anti-oxidation peptide), methylcarnosine, whale carnosine or Serpentis carnosine or anserine (very easily water-soluble), the dipeptides sweetener, the alitame element, lysine two sweet peptides, Aspartame, Gly-Leu (improving palatability), Pro-Glu (improving palatability), Val-Glu (improving palatability), the guanosine peptide, L-Glycylglycine (glycylglycine, (13.4g:100ml 25 ℃), fusing point: 262-264 ℃), glycylglutamine (Gly-Gln, 154g/L (20 ℃)) and alanyl glutamine (power peptide, Ala-Gln, 586g/L (20 ℃)), the glycyl proline dipeptides, lysine glutamic acid dipeptides, glutathion is (very easily water-soluble, mp195 °), alamethicin, glycyl-L-histidyl-L-lysine.

Above-mentioned edible peptide includes but not limited to: beans (legume, as Semen arachidis hypogaeae, Semen sojae atricolor, Semen Pisi sativi, Kidney bean (Semen Phaseoli Vulgaris), Semen phaseoli radiati, Semen Phaseoli (Semen Ormosiae Hosiei, Semen Phaseoli), Semen Viciae fabae, Semen vignae sinensis, Radix Crotalariae szemoensis (Lens culinaris Medic.), Semen sojae atricolor, Semen Canavaliae, Semen Cajani, Semen Psophocarpi tetragonolobi, chickpea, the white jade bean, Semen Phaseoli Vulgaris and Seem Lablab Album) the seed-protein peptide, frumentum (gramineous crop, as Semen Tritici aestivi, Herba bromi japonici, Semen Maydis, Fructus Hordei Vulgaris, rice, Semen setariae, broom corn millet, broomcorn millet, Sorghum vulgare Pers., fructus zizaniae caduciflorae, Semen Fagopyri Esculenti, seed of Job's tears) seed-protein peptide, the amaranth seed protein peptide, Sargassum protein matter peptide (as Thallus Laminariae (Thallus Eckloniae)), the Radix hemerocalis plicatae protein peptide, potato class (tuber crops tuber or rhizome, as Rhizoma Solani tuber osi, Rhizoma Dioscoreae esculentae, Rhizoma amorphophalli, Rhizoma Dioscoreae, Maninot esculenta crantz., Jerusalem artichoke) protein peptide, poultry or fowl produce peptide (by its muscle, internal organs, the peptide that albumen in blood makes through enzymolysis, as the de-fatted beef enzymolysis makes the beef polypeptide, fresh (Hepar Sus domestica) is through enzymolysis, decolouring, deodorize, the liver peptide is made with extra care to obtain in ultrafiltration, (pig) blood makes the hyperglobulinemia peptide through enzymolysis, the collagen peptide that its bone or skin obtain through modes such as hydrolysis or enzymolysis, the Nidus collocaliae collagen peptide, milk peptide, white of an egg peptide), (peptide made as its meat proteolysis, as sardine meat protein peptide for aquatic peptide, the collagen peptide that its bone or skin or squama obtain through modes such as hydrolysis or enzymolysis, as collagen peptides such as fish, Stichopus japonicuss, polypeptide from Chlamys farreri), fibroin peptide, complex peptides (complex peptides that the multiple proteins mixture such as animals and plants, Aquatic product, poultry or fowl product make through enzymolysis).

As: Calcium peptide, (be called for short CCP, be a kind of efficient calcium absorption enhancer to this elite example of edible peptide, and relative molecular mass is about a kind of calcic polypeptide of 3000, and color, to pale yellow powder, has special flavour.(20% fully dissolve) soluble in water), high F value oligopeptide (, by the oligopeptide that high side chain, low aromatic amino acid form that has made after the animal and plant proteolysis, take and hang down the phenylalanine oligopeptide as representative.The F value refers to the molar ratio of branched-chain amino acid (BCAA) and aromatic amino acid (AAA).), mineral element binding peptide (as phosphopeptide caseinate), seasoning peptide (can improve by simulating, shelter, strengthen local flavor the biologically active peptide of the palatability of food, as Umami flavor peptides (Lys-Gly-Asp-Glu-Glu-Ser-Leu-Ala), short chain glutamic acid polypeptide (can effectively cover bitterness), Curculin (Rhizoma Curculiginis sweet protein, can cover tart flavour and make tart flavour change sweet taste into), Mai Ruo Kelin (Miraculin, change the flavor glycoprotein, can cover tart flavour and make tart flavour change sweet taste into), thaumatin, mabinlin, monellin, mannatide.Other diluent, as organic salt diluent, as calcium lactate, high molecular polymer class diluent, as the alginic acid pharmaceutical salts as ammonium or sodium, potassium salt, dimethicone, polymethacrylates.Above-mentioned diluent comprises that any mixture of above-mentioned each example equally also can be used for the present invention.

Above-mentioned is soluble in water, and particularly very easily water-soluble diluent, for most preferably, is because of dissolving or dispersibility in the hydrophilic that can improve significantly tablet or water.

The sweller that one embodiment that is preferred for diluent of the present invention is selected from above-mentioned diluent and super-disintegrant and/or can not forms strong gel prepares excipient mixture by dry or wet granulation, contains above-mentioned diluent and super-disintegrant and/or can not form the particulate matter of the sweller of strong gel.

" super-disintegrant " that the present invention is used, also referred to as superdisintegrantes, can expand considerably, is commonly used for outside disintegrating agent (AGM) and inner disintegrating agent (AGG).Super-disintegrant is well known to those skilled in the art, and more specifically is described in Journal of Pharmaceutical Sciences(85 volume, No.11, in November, 1996).Be preferred for super-disintegrant of the present invention and include but not limited to, low hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose or calcium, cellulose fibre, cross linked polyacrylate, crosslinked Amberlite resin, alginate, carboxymethyl starch or the Microcrystalline Starch replaced, microcrystalline Cellulose and composition thereof.

The present invention " can not form the sweller of strong gel " used is pharmaceutically acceptable swelling considerably (expansion), but can not form strong gel and hinder the insolubility polymer of the release of medicine, be " pharmaceutically acceptable water-swellable and water-insoluble polymer " in other words, refer to so a kind of pharmaceutically acceptable material (polymer), when it is exposed in excessive water, it is expanded to its balance volume, but is not dissolved in solution.With regard to definition used herein, if a kind of material is considered to water miscible, it basically is dissolved in excessive water and forms solution, loses thus that it is initial, granular shape particularly, and with molecularity, is scattered in aqueous solution in fact.Common criterion is that the water dissolvable material is crosslinked without substantial extent, because crosslinked, will make material have water-insoluble.

In the present invention, " can not form the sweller of strong gel " used comprises in pharmaceutically acceptable water not from the water-swellable of separating and water-swellable and the water-insoluble polymer of water-insoluble polymer and pharmaceutically acceptable dissociation in water, preferably, be selected from water-swellable and the water-insoluble polymer of pharmaceutically acceptable dissociation in water.

Molecular weight ranges for the sweller that can not form strong gel of tablet of the present invention or water-swellable and insoluble polymer is very wide.Water-swellable and the insoluble polymer of high molecular, normally favourable for the use in the present invention relatively.But it is normally very wide to be applicable to molecular weight ranges of the present invention.The weight average molecular weight that is applicable to water-swellable of the present invention and insoluble polymer is greater than approximately 20000 usually, take and is greater than approximately 100000 as good, is preferably greater than approximately 200000, more preferably greater than approximately 500000, is greater than 1000000 preferablyly, is up to approximately 10000000.The method of measuring polymer molecular weight is being known in the art usually.

Sometimes the mode of expressing more easily polymer molecular weight is under 25 ℃, the viscosity of the aqueous solutions of polymers of 1.0 % by weight.Be applicable to polymer of the present invention, the viscosity of its 1.0 % by weight aqueous solution under 25 ℃ of take is advisable as about 200～approximately 80000 centipoises (mPas), is preferably approximately 500～approximately 80000 centipoises, and optimum is about 1000～approximately 80000 centipoises.

Pharmaceutically acceptable (dissociation in water) water-swellable and water-insoluble polymer for tablet of the present invention are normally crosslinked.Crosslinked amount should be enough to that polymer is kept on water-insoluble minimum usually, but also should make polymer keep water under the maximum of enough swellings so that polymer can absorb aequum liquid and and swelling.

Be preferably acid and/or alkaline water-swellable and the salt of insoluble polymer for the water-swellable of the pharmaceutically acceptable dissociation in water of tablet of the present invention and water-insoluble polymer.

Be suitable for slightly acidic water swellability of the present invention and insoluble polymer and comprise the functional group that can be used as weak acid.These functional groups include but not limited to carboxyl, sulfate groups, inferior sulfate radical group, and phosphate groups.Suitable functional group is carboxyl.Usually, these functional groups are connected on crosslinked base polymer.Suitable base polymer comprises polyacrylamide, polyvinyl alcohol, ethenyl maleic anhydride copolymer, polyvingl ether, polyacrylic acid, poly-carbon number is C1～C4 alkyl acrylic, poly-hydroxyl carbon number is C1～C4 alkyl acrylic, polyvinyl pyrrolidone, polyvinyl beautiful jade, and their copolymer.Also can use natural polysaccharide polymer, comprise carboxymethyl cellulose, carboxymethyl starch, hydroxypropyl or ethyl cellulose, alginic acid, alginate, humic acids, carrageenin, acrylic acid-grafted starch, acrylic acid-grafted cellulose, and their copolymer.Also can use synthetic polypeptide, as poly-aspartate, polyglutamic acid, poly-mixed acid acidic amino acid, (mix aspartic acid as poly-, the example is as poly-aspartate-aspartic acid-lysine acid (4: 2: 1); The poly-glutamic acid that mixes, the example is as polyglutamic acid-lysine acid (4: 1).Term " poly-mixed acid acidic amino acid " refers in chain and contains the several amino acids that comprises acidic amino acid herein, and the molal quantity of acidic amino acid (as aspartic acid, glutamic acid) be greater than basic amino acid (as lysine, arginine) molal quantity and present acid poly-several amino acids (poly-several amino acids be referring to document: US5247068A).

Be preferred for acid water swellability of the present invention and water-insoluble polymer and usually be greater than approximately 100000 acrylate copolymer including but not limited to weight average molecular weight, poly-carbon number is C1～C4 alkyl acrylic, poly-hydroxyl carbon number is C1～C4 alkyl acrylic, acrylic acid-acrylate polymer, polyvinyl alcohol-acrylic block copolymers, the starch graft acrylic acid polymer, the cellulose graft acrylate copolymer, humic acids, polycarbophil (Polycarbophilpolymers), alginic acid, poly-aspartate, polyglutamic acid, poly-aspartic acid and the poly-glutamic acid that mixes of mixing, and their mixture.

Be suitable for alkalescent water swellability of the present invention and insoluble polymer and comprise the functional group that can be used as weak base.These functional groups include, but is not limited to primary, secondary and tertiary amino, imino group, and acylamino-.Suitable functional group is amino.Usually, these functional groups are connected on crosslinked matrix polymer.Suitable matrix polymer comprises polyamine or poly-imines, polymine, polyethylenepolyamine, polyacrylamide, polypropylene amine, the polypropylene carbon number is C1～C4 alkylamine, and poly-carbon number is C1～C4 alkyl allylamine, and poly-carbon number is that C1～C4 alkyl propylene carbon number is C1～C4 alkylamine, poly-hydroxyl carbon number is C1～C4 alkyl allylamine, poly-hydroxyl carbon number is that C1～C4 alkyl propylene carbon number is C1～C4 alkylamine, and polyquaternary ammonium salt, and their copolymer.Also natural polysaccharide polymer be can use, chitin and chitosan and other aminopolysaccharides comprised.Also can use synthetic polypeptide, as poly-asparagine, polyglutamine, polylysine, poly arginine, (mix lysine as poly-, the example is as polyglutamic acid-lysine (1: 3) for poly-mixed-alkali aminoacid; The poly-arginine that mixes, the example is as poly-aspartate-arginine (1: 4).Term " poly-mixed-alkali aminoacid " refers in chain and contains the several amino acids that comprises basic amino acid herein, and the molal quantity of basic amino acid (as lysine, arginine) be greater than acidic amino acid (as aspartic acid, glutamic acid) molal quantity and present the poly-several amino acids of alkalescence (poly-several amino acids be referring to document: US5247068A).

Be preferred for alkaline water swellability of the present invention and water-insoluble polymer and usually be greater than approximately 100000 polyamine or poly-imines including but not limited to weight average molecular weight, polymine, polypropylene amine, polyethylenepolyamine, the polypropylene carbon number is C1～C4 alkylamine, poly-carbon number is C1～C4 alkyl allylamine, poly-carbon number is that C1～C4 alkyl propylene carbon number is C1～C4 alkylamine, poly-hydroxyl carbon number is C1～C4 alkyl allylamine, poly-hydroxyl carbon number is that C1～C4 alkyl propylene atomic number is C1～C4 alkylamine, chitin, chitosan, other aminopolysaccharides, poly-asparagine, polyglutamine, polylysine, poly arginine, poly-lysine and the poly-arginine that mixes of mixing, and their mixture.

Usually, preferablyly for above-mentioned acidity of the present invention and/or alkaline water swellability and insoluble polymer, be required to be its salt form.Usually wish that the acidity of above-mentioned acidity and/or alkaline water swellability and insoluble polymer and/or the degree of neutralization of basic functionality are approximately 30～approximately 100 % by mole, about 40～about 100(or 90 more advantageously) % by mole, optimum ground is 50～about 100(or 80 approximately) % by mole.Their concrete salt form or embodiment are shown in Chinese patent zl:2012101714300 (application number).

Do from the water-swellable of separating and the example of water-insoluble polymer, not comprise in the pharmaceutically acceptable water of sweller of the present invention, but be not limited to: neutral polysaccharide base polymer, alkyl glycol, polyalkylene oxide (for example poly(ethylene oxide)), oxygen vinyl alkyl ether, and their mixture.

Particularly preferably do sweller of the present invention example comprise, but be not limited to: homopolymer or the copolymer of unsaturated acids (for example acrylic acid or its salt), homopolymer or the copolymer of unsaturated amides (for example acrylamide), the homopolymer of ethylene imine or copolymer, polyvinyl (for example poly-(vinyl alcohol)), the homopolymer of vinyl esters or copolymer (vinyl pyrrolidone for example, Yi Xi oxazolidinone, Yi thiazolinyl methyl oxazolidinone, vinyl amine and vinylpyridine), the polysaccharide sweller, alkyl glycol, polyalkylene oxide (for example poly(ethylene oxide)), oxygen vinyl alkyl ether and the mixture that reaches them.

Above-mentioned polysaccharide sweller comprises neutral polysaccharide, acidic polysaccharose and salt thereof, and the derivant of their covalent cross-linking.Above-mentioned polysaccharide sweller is selected from, but be not limited to: alginate jelly (or alginic acid), pectin, xanthan gum, guar gum, Tragacanth, Radix Acaciae senegalis, glucosan, pectin, locust bean gum, carrageenin (polysaccharide), starch, modified starch (for example hydroxypropyl starch or carboxymethyl starch and slaine thereof)), Microcrystalline Starch, microcrystalline Cellulose, the cellulose of modification (comprises cellulose esters and cellulose ethers, hydroxypropyl cellulose for example, hydroxyethyl-cellulose, hydroxyethylmethyl-cellulose, methylcellulose, carboxymethyl cellulose and slaine thereof), the pharmaceutical salts of above-mentioned acidic polysaccharose (preferred medicinal insoluble metallic salt), the derivant that above-mentioned polysaccharide covalent is crosslinked, and their mixture.

Above-mentioned sweller comprises that the mixture of above-mentioned each example equally also can be used for the present invention.

Above-mentioned diluent and above-mentioned super-disintegrant and/or sweller consumption proportion (weight ratio) are generally 1 ︰ 0.05～0.5, are preferably 1 ︰ 0.1～0.3.

(material) preference ranking as the above-mentioned diluent of the present invention is the direct pressing level.More preferably there is (height) porous above-mentioned diluent, for example prepare by spray drying, as Advantose100Maltose is spray-dired disaccharide carbohydrate.

Term used herein " porous diluent " and equivalent terms thereof refer to its pore volume divided by the determined porosity of cumulative volume higher than approximately 0.14 or its weight divided by the determined density of (always) volume lower than approximately O.86.Term used herein " high (degree) porous diluent " and equivalent terms thereof refer to its pore volume divided by the determined porosity of cumulative volume higher than approximately 0.25 or its weight divided by the determined density of (always) volume lower than approximately O.75.There is highly porous above-mentioned diluent more preferably for the present invention.Above-mentioned " porous diluent " more preferably has plasticity, for example, lower than plastic deformation (tablet formed maintains its shape and size) occurs during with this class powder of inch diameter die head compacting 500mg O.5-under the about pressure of 1500 pounds.Especially, this type of " porous diluent " has " high (degree) plasticity ", no matter when when lower than 1, under the pressure of 500 pounds during with this granule of 0.5-inch diameter punch die compacting 500mg, the fragility that the tablet hardness that they all show formation is greater than about 7 newton (N) or forms tablet is lower than approximately 5%.

Except containing above-mentioned diluent, also can contain the structure agent in above-mentioned " (height) porous diluent "." skeleton " made in the structure agent, and porous support structure should be able to be provided, and makes tablet dissolve fast in oral cavity.Suitable structure agent comprises agar, gelatin, albumin chrondroitin, and preferably constructing agent is gelatin.The consumption of structure agent (as gelatin) is about 1-10%, preferably 1-5%, more preferably 1-3%.Usually above-mentioned diluent and structure agent are dissolved in and should measure in solvent, by as the drying means such as spray drying or lyophilization or fling to by methods such as fluidised bed granulator granulations the particulate matter that solvent prepares " (height) porous diluent ".Dissolve the selection of solvent of above-mentioned diluent and structure agent composition based on providing required porous ability to pearl or granulated product when the drying.Suitable solvent can be selected from water, ethanol, isopropyl alcohol or its mixture, preferred solvent be ethanol and water in 1: 1-1: the mixture of 100 ratios.

In above-mentioned " (height) porous (height) plasticity diluent ", remove containing above-mentioned diluent; or also contain further outside above-mentioned structure agent; also can contain super-disintegrant and/or can not form the sweller of strong gel, be generally above-mentioned diluent and super-disintegrant and/or can not form the sweller of strong gel and/or above-mentioned structure agent by as the drying meanss such as spray drying or lyophilization or the particulate matter for preparing by methods such as fluidised bed granulator granulations.Above-mentioned disintegrating agent and/or sweller make tablet dissolve fast in oral cavity and/or plasticizing (produce plastic deformation, maintain shape and the size of the tablet of formation).Similar patented technology US5,464,632, CN1819819B, can be for referencial use.

Above-mentioned diluent in above-mentioned " (height) porous (height) plasticity diluent " and above-mentioned super-disintegrant and/or sweller consumption proportion (weight ratio) are generally 1 ︰ 0.05～0.5, are preferably 1 ︰ 0.1～0.3.

The commercially available example of this type of " (height) porous (height) plasticity diluent " for example, as pregelatinized Starch (Roquette American Inc.

c), maltodextrin (as the example that can be purchased be MALTRIN series (maltodextrin of Grain Processing Corp. and the solid form of corn syrup), MALTRINQD series (the solid rapid dispersion form of the maltodextrin of Grain Processing Corp. and corn syrup, as Maltrin QD580) and

t (maltodextrin of Roquette American Inc. and spray-dired glucose)).Preferably Maltrin QD series and ADVANTOSEFS95 fructose or its combination, have highly porous and splendid binding characteristic because they can be formed in aggregate.Other examples as

(from the spray-dired mannitol of SPIPharma.Inc.).

Above-mentioned diluent comprises that the mixture of above-mentioned each example equally also can be used for the present invention.

The granule largest cross-sectional sized of above-mentioned diluent is less than approximately 600 microns (about 28 orders, Tyler standard), preferably be less than approximately 250 microns (about 60 orders, Tyler standard), more preferably be less than approximately 150 microns (approximately 100 orders, Tyler standard), more more preferably be less than approximately 75 microns (about 200 orders, Tyler standard), be less than best approximately 25 microns (approximately 500 orders, Tyler standard).

The blended amount of the above-mentioned diluent that the present invention is used can be carried out suitable adjustment by the consumption of medicine and/or the size of tablet, the ratio that above-mentioned diluent (B1) (the particularly diluent of the graininess of its water-soluble crystalline state or powdered (B1)) (usually) accounts for whole tablet (gross weight) is 1%(wt./wt.) to 99%(wt./wt.), be preferably 5%(wt./wt.) to 95%(wt./wt.), be more preferably 10%(wt./wt.) to 90%(wt./wt.), be 20%(wt./wt. best) to 80%(wt./wt.), above percentage by weight is based on the gross weight of tablet, the ratio that above-mentioned diluent (B2) (the particularly diluent of the graininess of its water-soluble crystalline state or powdered (B2)) (usually) accounts for whole tablet is 1%(wt./wt.) to 99.5%(wt./wt.), be preferably 5%(wt./wt.) to 99%(wt./wt.), be more preferably 10%(wt./wt.) to 95%(wt./wt.), be 30%(wt./wt. best) to 92%(wt./wt.), above percentage by weight is based on the gross weight of tablet.This is because the hydrophilic that the blended amount of higher above-mentioned diluent is conducive to improve tablet mechanical performance particularly.

Two, fusible adhesion agent (C)

The fusible adhesion agent (C) the present invention relates to comprises fusible binding agent (D) and performance improving agent (E).Below explain respectively.

The fusible binding agent (hereinafter to be referred as hot-melt adhesive) the present invention relates to (D-1) (being above-mentioned fusible surfactant D 1) for or be selected from pharmaceutically acceptable, the more above-mentioned diluent of fusing point (B) is low more preferably also more above-mentioned active component (A) low, room temperature (25 ℃ of temperature) lower for solid (fusing point is not less than 25 ℃) and (preferably dissolve in or be scattered in water or hydrophilic) fusible surfactant.Fusing point (usually) for fusible binding agent of the present invention (D-1) is 25 to 150 ℃ (containing end points), preferably 35 to 120 ℃ (containing end points), more preferably 40 to 100 ℃ (containing end points).The fusing point of above-mentioned fusible binding agent (D-1) preferably more preferably also at least hangs down 10 ℃ (containing) than the fusing point of active component (A) than above-mentioned diluent (B), more preferably at least hangs down 20 ℃ (containing).The fusing point (usually) of above-mentioned hot-melt adhesive (D-1) is not less than 25 ℃, because the mixing of each component (usually) is carried out and binding agent should keep solid forms at this mixing temperature in this temperature.The melting temperature of above-mentioned hot-melt adhesive (D-1) is not generally higher than 150 ℃, because melt at the temperature that binding agent should not affect adversely in the activity of medical active component.For example, binding agent should melt at the temperature of decomposing lower than medical active component and the excipient that contains arbitrarily.The fusible binding agent (D-1) of above-mentioned (for of the present invention) preferably is selected from and dissolves in or be scattered in water or hydrophilic surfactant, with its neutrality or nonionic surfactant for better.

The fusible binding agent (hereinafter to be referred as hot-melt adhesive) the present invention relates to (D-11) (being above-mentioned fusible lipophilic surfactant D11) for or be selected from that at least one is pharmaceutically acceptable, the more above-mentioned diluent of fusing point (B) is low more preferably also more above-mentioned active component (A) low, be solid (fusing point is not less than 43 ℃ (preferably being not less than 50 ℃)) fusible (lipotropy) surfactant under room temperature.For the fusing point of fusible binding agent of the present invention (D-11), be preferably 50 ℃ to 150 ℃ (containing end points), preferably 60 ℃ to 120 ℃ (containing end points), more preferably 70 ℃ to 120 ℃ (containing end points), more preferably 80 ℃ to 100 ℃ (containing end points) best.The fusing point of above-mentioned fusible binding agent (D-11) preferably more preferably also at least hangs down 10 ℃ (containing) than the fusing point of active component (A) than above-mentioned diluent (B), more preferably at least hangs down 20 ℃ (containing).The fusing point (usually) of above-mentioned hot-melt adhesive (D-11) is not less than 43 ℃ (preferably being not less than 50 ℃), because itself and pharmaceutically acceptable, room temperature (25 ℃ of temperature) lower for liquid (fusing point is lower than 25 ℃), dissolve in or be scattered in water or hydrophilic surfactant (E-22) mixing after to be conducive to this molten mixture room temperature (25 ℃ of temperature) under be solid, because (usually) will carry out mixing of materials at normal temperatures, it is necessary that each material keeps solid forms when this mixes.The melting temperature of above-mentioned hot-melt adhesive (D-11) is not generally higher than 150 ℃, because melt at the temperature that binding agent should not affect adversely in the activity of medical active component.For example, binding agent should melt at the temperature of decomposing lower than medical active component and the excipient that contains arbitrarily.The fusible binding agent (D-11) of above-mentioned (for of the present invention) preferably is selected from and dissolves in or be scattered in water or hydrophilic surfactant, with its neutrality or nonionic surfactant for better.

The fusible binding agent (hereinafter to be referred as hot-melt adhesive) the present invention relates to (D-2) component (being above-mentioned fusible medicinal lipid additive D2) for or be selected from that at least one is pharmaceutically acceptable, the more above-mentioned diluent of fusing point (B) is low more preferably also more above-mentioned active component (A) low, be solid (fusing point is not less than 25 ℃) fusible lipid (medicinal) additive under room temperature.Fusing point (usually) for fusible binding agent of the present invention (D-2) is 25 to 150 ℃ (containing end points), preferably 35 to 120 ℃ (containing end points), more preferably 40 to 100 ℃ (containing end points).The fusing point of above-mentioned fusible binding agent (D-2) preferably more preferably also at least hangs down 10 ℃ (containing) than the fusing point of active component (A) than above-mentioned diluent (B), more preferably at least hangs down 20 ℃ (containing).The fusing point (usually) of above-mentioned hot-melt adhesive (D-2) is not less than 25 ℃, because the mixing of each component (usually) is carried out and binding agent should keep solid forms at this mixing temperature in this temperature.The melting temperature of above-mentioned hot-melt adhesive (D-2) is not generally higher than 150 ℃, because melt at the temperature that binding agent should not affect adversely in the activity of medical active component.For example, binding agent should melt at the temperature of decomposing lower than medical active component and the excipient that contains arbitrarily.

The fusible binding agent (hereinafter to be referred as hot-melt adhesive) the present invention relates to (D-21) component (being above-mentioned fusible medicinal lipid additive D21) for or be selected from that at least one is pharmaceutically acceptable, the more above-mentioned diluent of fusing point (B) low more preferably also more above-mentioned active component (A) is low, under room temperature, be that solid and fusing point are not less than fusible lipid (medicinal) additive of 43 ℃ (preferably being not less than 50 ℃), the fusing point of above-mentioned fusible binding agent (D-21) preferably more preferably also at least hangs down 10 ℃ (containing) than the fusing point of active component (A) than above-mentioned diluent (B), more preferably at least hang down 20 ℃ (containing).Fusing point for fusible binding agent of the present invention (D-21) is preferably 50 to 150 ℃ (containing end points), preferably 60 to 120 ℃ (containing end points), more preferably 70 to 100 ℃ (containing end points).The fusing point (usually) of above-mentioned hot-melt adhesive (D-21) is not less than 43 ℃ (preferably being not less than 50 ℃), because being conducive under this molten mixture room temperature (25 ℃ of temperature) after performance enhancers (E-21) mixing of the surfactant that itself and room temperature (25 ℃ of temperature) time are liquid (fusing point is lower than 25 ℃) is solid, because (usually) will carry out mixing of materials at normal temperatures, it is necessary that each material keeps solid forms when this mixes.The melting temperature of above-mentioned hot-melt adhesive (D-21) is not generally higher than 150 ℃, because melt at the temperature that binding agent should not affect adversely in the activity of medical active component.For example, binding agent should melt at the temperature of decomposing lower than medical active component and the excipient that contains arbitrarily.

The fusible binding agent (hereinafter to be referred as hot-melt adhesive) the present invention relates to (D-3) component (being above-mentioned fusible saccharide D3) is or is selected from the relatively low saccharide of at least one fusing point, refers to hereinafter.

For performance enhancers of the present invention (E) for or be selected from medical additive and/or the active component (medical additive E1 described above, medical additive E2, surfactant E2, surfactant E21, surfactant E23, saccharide E31, active components A 1 or A2 etc.) that the more above-mentioned fusible binding agent of pharmaceutically acceptable fusing point is high.It is the following medical additive of solid that above-mentioned medical additive E1 can be selected from 25 ℃ of temperature: any one in medicinal lipid additive, medicinal surfactant additive, medicinal carbohydrate additive, medicinal cyclodextrin additive, amino acids additive, edible peptide class additive, medicinal salts additive, medicinal bases additive, medicinal acids additive or their combination in any.It is the following medical additive of solid that above-mentioned medical additive E2 can be selected from 25 ℃ of temperature: any one in medicinal carbohydrate additive, medicinal cyclodextrin additive, amino acids additive, edible peptide class additive, ionic surfactant additive, medicinal salts additive, medicinal bases additive, medicinal acids additive or their combination in any.

As for performance enhancers of the present invention (E-1) component (being above-mentioned medicinal lipid additive) for or be selected from low (fusible) lipid (medicinal) additive that more preferably also more above-mentioned active component (A) is low of preferably more above-mentioned diluent (B) that at least one is pharmaceutically acceptable, the more above-mentioned fusible binding agent of fusing point (D-1) (being above-mentioned surfactant D 1) is high.Above-mentioned performance enhancers (E-1) (usually) for or be selected from pharmaceutically acceptable, fusing point and be not less than 25 ℃ and more above-mentioned diluent is low and more fusible binding agent is high (fusible) lipid (medicinal) additive.Above-mentioned performance enhancers (E-1) preferably for or be selected from pharmaceutically acceptable, fusing point and be not less than 40 ℃ and more above-mentioned diluent is low and more fusible binding agent is high (fusible) lipid (medicinal) additive.This performance enhancers (E-1) can improve or improve mechanical performance and/or weatherability and/or the hydrophilic of fusible binding agent (D-1 etc.), thereby improves mechanical performance and/or weatherability and/or the hydrophilic of tablet of the present invention.In addition, reach the surfactant of consumption at high proportion with respect to 100% consumption in conventional art and make adhesion agent, this performance enhancers (E-1) can reduce the consumption of above-mentioned surfactant, thereby may lower its toxic and side effects, improves the application security of tablet.

For another example for performance enhancers of the present invention (E-2) component (being above-mentioned medicinal surfactant additive) for or be selected from that at least one is pharmaceutically acceptable, fusing point be not less than 25 ℃ (preferably more above-mentioned fusible binding agent (D-2) (being above-mentioned fusible medicinal lipid additive D2) high, more preferably more above-mentioned diluent (B) low more preferably also more above-mentioned active component (A) is low) surfactant.Above-mentioned performance enhancers (E-2) (usually) for or be selected from pharmaceutically acceptable, fusing point and be not less than 25 ℃ and be not less than low (fusible) surfactant that more preferably also more above-mentioned active component (A) is low of preferably more above-mentioned diluent (B) of above-mentioned fusible binding agent (D-2).Above-mentioned performance enhancers (E-2) preferably is selected from and dissolves in or be scattered in water or hydrophilic surfactant, with its neutrality or nonionic surfactant for better.This performance enhancers can improve or improve the mechanical performance of fusible binding agent (D-2 etc.) and/or fusible binding agent affinity and/or the dispersibility of fusible binding agent in water to hydrophilic diluents etc., thereby improves the mechanical performance of tablet of the present invention and/or hydrophilic (or in water dispersibility); Perhaps, when the more above-mentioned fusible binding agent of the fusing point of this performance enhancers (D-2) (being above-mentioned fusible medicinal lipid additive D2) is high, can also improve the weatherability of tablet of the present invention.

And for example for performance enhancers of the present invention (E-21) component (being above-mentioned surfactant E21) for or be selected from that at least one is pharmaceutically acceptable, lower the dissolving in or being scattered in water or hydrophilic surfactant for liquid (fusing point is lower than 25 ℃) of room temperature (25 ℃ of temperature).Above-mentioned performance enhancers (E-22) preferably for or be selected from dissolve in be scattered in water or hydrophilic neutrality or nonionic surfactant.This performance enhancers can improve or improve affinity and/or the fusible binding agent dispersibility in water of fusible binding agent to hydrophilic diluents, thereby improves the mechanical performance of tablet of the present invention and/or hydrophilic (or in water dispersibility); Perhaps, can improve or improve technological feasibility, can produce at relatively low temperature, energy-conservation, reduce production costs, be conducive to the stable of heat-labile composition.

And for example for performance enhancers of the present invention (E-3) component for or be selected from least one and pharmaceutically acceptablely be not less than 25 ℃ of temperature but not higher than the saccharide E3 of above-mentioned fusible saccharide D3.This performance enhancers also can be improved mechanical performance and/or the hydrophilic of tablet of the present invention.

Other see the below introduction for performance enhancers of the present invention.

Form solid dispersion (/ or body) between above-mentioned fusible binding agent and above-mentioned performance enhancers and also can be used as fusible binding agent of the present invention and/or performance enhancers.

Fusing point for the following medical additive of solid under 25 ℃ of above-mentioned performance enhancers (E) or said temperatures preferably is not less than 40 ℃ or 50 ℃ and low and above-mentioned active component at least low 5 ℃ (containing) and the more fusible binding agent at least high 5 ℃ (containing) of more above-mentioned diluent.Further, this fusing point preferably is not less than 60 ℃, more preferably is not less than 70 ℃, the most more preferably is not less than 80 ℃, but preferably not higher than 150 ℃, more preferably not higher than 120 ℃; This fusing point preferably at least hangs down 10 ℃ (containing) than the fusing point of above-mentioned diluent and above-mentioned active component, more preferably at least hangs down 20 ℃ (containing); This fusing point is preferably than the fusing point of above-mentioned hot-melt adhesive at least high 10 ℃ (containing), more preferably at least high 20 ℃ (containing), at least high 30 ℃ (containing) best.

" hot-melt adhesive " reaches " performance enhancers " and preferably selects than at least low 10 ℃ of the fusing points of diluent and active component, more preferably at least the advantage of the fusible material of low 20 ℃ is: when these materials all melt, the only above-mentioned diluent of a small amount of or trace and active component fusing, a large amount of above-mentioned diluent and active component exist with original form, be conducive to like this improve the intensity of solid fused mass and tablet, also do not affect the disintegrating property of tablet simultaneously.

" performance enhancers ", for fusing point is not less than 40 ℃ or 50 ℃ or the high fusible material of higher and more above-mentioned fusible binding agent, it is advantageous that: be conducive to the mechanical performance that tablet can tolerate higher temperature and raising solid fused mass and tablet.

Below the present invention's fusible binding agent used (D) and performance improving agent (E) example are elaborated.

One), surfactant (SA)

Surfactant (SA) not only can be made above-mentioned fusible adhesive component but also can make above-mentioned performance enhancers component in the present invention.

For surfactant of the present invention (SA), can be (following with S, mean) of solid under room temperature (25 ℃ of temperature), can be also (following with L, mean) of liquid under room temperature (25 ℃ of temperature), can be to dissolve in (the term declaratives are shown in definition) that maybe can be scattered in water, can be also (the term declaratives are shown in definition) that is insoluble to or is not scattered in water, can be fusible (the term declaratives are shown in definition), can be also (SA that is greater than 150 ℃ as fusing point, as the ion-type SA) that infusibility melts.Wherein, solid or dissolve in the SA that maybe can be scattered in water and be preferred for the present invention, dissolve in the SA that maybe can be scattered in the solid of water and be particularly preferred for the present invention.Lipophilic group in (usually) surfactant is that unsaturated alkyl is (as oleoyl, inferior oleoyl, the Oleum Arachidis hypogaeae semen acyl group, the Oleum Ricini acyl group) or the side chain saturated alkyl such as different saturated alkyl (isostearoyl base) or part C8～C16 especially C8～C14 be particularly liquid under room temperature (25 ℃ of temperature) during short chain straight chain saturated alkyl in C8～C12, lipophilic group in (usually) surfactant be C18 or more senior long-chain straight chain saturated alkyl or lipophilic group be part C8～C16 especially C8～C14 be particularly solid under room temperature (25 ℃ of temperature) during short chain straight chain saturated alkyl in C8～C12.The hydrophilic of surfactant or lipophile also can be weighed by the HLB value.People now Surfactant done deeply research widely, the physicochemical properties such as the dissolubility of surfactant, fusing point or freezing point, HLB value can be consulted be correlated with monograph or document and be obtained as Fiedler.

" HLB " used in the present invention value refers to the hydrophilic of surfactant-lipophilic equilibrium valve, and can be used for having defined relative hydrophilic and the lipotropy of surfactant.The surfactant of low HLB value is lipophilic more, have larger dissolubility in oil, and the surfactant of high HLB value is more hydrophilic, has larger dissolubility in aqueous solution.To achieve the object of the present invention, the HLB value is less than 10 surfactant for " lipophilic surfactant ", and HLB to be greater than 10 surfactant be " hydrophilic surfactant active ".Obtain the HLB value according to the semiempirical formula that is used to indicate surfactant.Its numerical range is 1-45, for non-ionic surface active agent, is 1-20.The basis of HLB system is that some molecules have hydrophilic radical, and other molecules have lipophilic group, and the two concept had concurrently of some molecules.In molecule or mixture, the percentage by weight of each types of radicals is indicating which kind of behavior this molecular structure will demonstrate.Referring to, Griffin for example, WC, J.Soc.Cos.Chem.1:311 (1949), and Griffin, WC, J.Soc.Cos.Chem.5:259 (1954).HLB values can list in table 1 hereinafter for the HLB value of the exemplary table surface-active agent of method and composition of the present invention.

Table 1

Surfactant	HLB	Surfactant	HLB
				The Oleum Ricini of PEG-2 hydrogenation	1.7	The PEG-10 oleyl ether	12.4
Sorbitan trioleate	1.8	The different hot phenylate of PEG-8	12.4
				The anhydrous sorbitol tristearate	2.1	The PEG-10 stearyl ether	12.4
Tristerin	3.5	Cremophor ELP	12.5
				Sorbitan sesquioleate	3.7	The PEG-10 cetyl ether	12.9

Lai Beiruifu (Labrafil)	4.0	N-9	12.9
				Sorbitan monooleate	4.3	The PEG-40 Oleum Ricini	13.0
Sorbitan monostearate	4.7	The different hot phenylate of PEG-10	13.5
				The PEG-2 oleyl ether	4.9	The Oleum Ricini of PEG-40 hydrogenation	14.0
The PEG-2 stearyl ether	4.9	Lay shellfish drag-line (Labrasol)	14
				The Oleum Ricini of PEG-7 hydrogenation	5.0	Igepal co-730	14.2
The PEG-2 cetyl ether	5.3	The PEG-12 tridecyl ether	14.5
				The PEG-4 Span60	5.5	The PEG-18 tridecyl ether	14.5
PEG-2 anhydrous sorbitol isostearate	6.0	Polysorbate60	14.9
				Dehydration Pyrusussuriensis palmitate	6.7	Polysorbate80	15.0
Te Li is with (Triton) SP-135	8.0	PEG-20 glyceryl stearate	15.0
				Sorbitan mono-laurate	8.6	The PEG-20 stearate	15.0
The full oleate of PEG-40 anhydrous sorbitol	9.5	The PEG-20 stearyl ether	15.3
				The PEG-4 lauryl ether	9.7	The PEG-20 oleyl ether	15.3
Polysorbate 81	10.0	Polysorbate40	15.6
				PEG-40 anhydrous sorbitol six oleates	10.0	Brij 58	15.7
The disparate stearate of PEG-40 anhydrous sorbitol	10.0	PEG (20) cetyl ether	15.7
				PEG-10 olive oil glyceride type	10.0	The Oleum Ricini of PEG-60 hydrogenation	16.0
PEG sorbitol six oleates	10.2	The PEG-30 stearate	16.5
				Polysorbate65	10.5	Polysorbate20	16.7
The Oleum Ricini of PEG-25 hydrogenation	10.8	PEG-75 Lan Nuolin (lanolin)	16.7
				Polysorbate85	11.0	The PEG23 lauryl ether	16.9
PEG-7 glyceryl cocos nucifera oil acid esters	11.0	The PEG-40 stearate	17.3
				The PEG-8 stearate	11.1	The PEG-50 stearate	17.7
PEG anhydrous sorbitol four oleates	11.4	The different hot phenylate of PEG40	17.9
				PEG-15 glyceryl isostearate	12.0	The PEG-100 stearate	18.8
PEG-35 almond oil glyceride type	12.0	F68 (Pluronic) F68	29.0

Can use the kinds of surface activating agent for preparation of the present invention, comprise United States Patent (USP) 6,365, disclosed surfactant in 637, be incorporated to the present invention by it by reference, also comprises the compound that belongs to following kind: the polyethoxy fatty acid, Polyethylene Glycol (or PEGization) fatty alcohol ether, Polyethylene Glycol (or PEGization) fatty acid ester, the mixture of Polyethylene Glycol (or PEGization) fatty acid one ester and diester, Polyethylene Glycol glycerol fatty acid ester, alcohol-grease group-transfer product, the fatty acid of bound to polyglycerol, propylene glycol (list) fatty acid ester, the mixture of propylene glycol ester and glycerine ester, glycerol one fatty acid ester and dialycerides fat acid esters, steroid surfactant (sterin and steroid derivatives), polyethylene glycol sorbitan fatty acid esters, polyethylene glycol alkyl ether, sugar ester, polyalkylene glycol alkyl phenol, sorbitan fatty acid ester, lower alcohol fatty acid esters, Polyethylene Glycol (PEG), polyethylene glycol oxide (PEO), polyoxy ethylene-polyoxy propylene-based block copolymer, and ionic surfactant.But hereinafter provide each kind example that above-mentioned excipient commercialization obtains:

A), polyethylene glycol fatty acid monoester class, two esters, list and two ester admixtures, wherein, (being somebody's turn to do) fatty acid (base) preferably carbon number is C8～C32, C10～C22 more preferably, the more preferably fatty acid of C12～C18 (base) or its hydroxy fatty acid (base), above-mentioned linear saturated fatty acids (base) most preferably, (being somebody's turn to do) polyethylene glycol groups polymerization number is preferably approximately 2 to approximately 200, be more preferably approximately 4 to approximately 150 or 120, more preferably approximately 8 to approximately 100, more preferably approximately 12 to approximately 60, more preferably approximately 20 to approximately 50, most preferably be approximately 30 to approximately 40 (this polyethylene glycol groups molecular weight is approximately 100 to approximately 10000 in other words, preferably approximately 200 to approximately 7500 or 6000, more preferably approximately 400 to approximately 5000, more preferably approximately, 600 to approximately 2500, more preferably approximately 1000 to approximately 2500, best 1500 to 2000, in order to distinguish above-mentioned aggregate number, while with molecular weight, indicating polyethylene glycol groups, this numeric indicia is last in this material title, as the PEG-10 laurate, mean that the polyethylene glycol groups aggregate number is 10, PEG-laurate 1000, mean that the polyethylene glycol groups molecular weight is 1000, below herewith, do not reresent).

A-1), polyethylene glycol fatty acid monoester class example includes but not limited to PEG6,7,8,9,10,12,15,20,25,30,32,40,45,50,55,100,200, the lauric acid of 300,400,600 grades (dodecoic acid) (L), (meat) myristic acid (tetradecylic acid) (L), Palmic acid (hexadecylic acid) (L), stearic acid (stearic acid) (S), arachidic acid (20 acid) (S), behenic acid (behenic acid) (S), the esters of oleic acid (L), ricinoleic acid (L).For example, PEG-6 laurate (L) or stearate (S), PEG-7 oleate (L) or laurate (L), PEG-8 laurate (L) or oleate (L) or stearate (S), PEG-9 oleate (L) or stearate (S), PEG-10 laurate (L) or oleate (L) or stearate (S), PEG-12 laurate (L) or oleate (L) or stearate (S) or monoricinolein (L), PEG-15 stearate (S) or oleate (L), PEG-20 laurate (L) or oleate (L) or stearate (S), PEG-25 stearate (S), PEG-32 laurate or oleate (L) or stearate (S), PEG-30 stearate (S), PEG-40 laurate or oleate (L) or stearate (S), PEG-45 stearate (S), PEG-50 stearate (S), PEG-55 stearate (S), PEG-100 oleate (L) or stearate (S), PEG-200 oleate (L), PEG-oleate 400 (L), PEG-oleate 600 (L), PEG-8 laurate (liquid), PEG-24 laurate (paste half is solid), the PEG-40 laurate (Gu), the PEG-100 laurate) (Gu), PEG-laurate 200 (liquid), PEG-laurate 400 (liquid), PEG-laurate 600 (paste half is solid), PEG-laurate 1000～6000 (Gu), the surfactant that belongs to this colony for example is known as Cithrol, Algon, Kessco, Lauridac, Mapeg, Cremophor, Emulgante, Nikkol, Myrj, Crodet, Albunol, Lactomul, the polyethoxy fatty acid of above-mentioned one or more, a-2), polyethylene glycol fatty acid two esters examples include but not limited to PEG-8, 10, 12, 20, 32, 150, the lauric acid of 400 grades (dodecoic acid) (L), (meat) myristic acid (tetradecylic acid) (L), Palmic acid (hexadecylic acid) (L), stearic acid (stearic acid) (S), arachidic acid (20 acid) (S), behenic acid (behenic acid) (S), two esters of oleic acid (L), for example, PEG-8 dilaurate (L) or distearate (S), PEG-10 dipalmitate (L), PEG-12 dilaurate (L) or distearate (S) or dioleate (L), PEG-20 dilaurate (L) or distearate (S) or dioleate, PEG-32 dilaurate or distearate (S) or oleate, PEG-150 distearate (S), PEG-dioleate or distearate 400 (S), the surfactant that belongs to this colony for example is known as Mapeg, Polyalso, Kessco, Cithrol, the cithrol of above-mentioned one or more, a-3), polyethylene glycol fatty acid list and diester mixture examples such as PEG-4～150 lists and distearate (S) etc., the surfactant that belongs to this colony for example is known as Kessco, but the example that commercialization obtains comprises: PEG-4～150 are single, (PEG-200～6000 are single, dilaurate for dilaurate, Stepan), PEG-4～150 are single, (PEG-is mono-, dioleate 200-6000 for dioleate, Stepan), and PEG-4～150 are single, (PEG-is mono-, distearate 200～6000 for distearate, Stepan), PEG-fatty acid one ester or two ester admixtures of above-mentioned one or more,

B), Polyethylene Glycol glycerol fatty acid ester, wherein, (being somebody's turn to do) fatty acid (base) preferably carbon number is C8～C32, C10～C22 more preferably, the more preferably fatty acid of C12～C18 (base) or its (single or two) hydroxy fatty acid (base), above-mentioned linear saturated fatty acids (base) most preferably, (being somebody's turn to do) polyethylene glycol groups polymerization number is preferably approximately 2 to approximately 100, be more preferably approximately 6 to approximately 100, more preferably approximately 8 to approximately 60, more preferably approximately 12 to approximately 40, most preferably be 8 to 30, the surfactant that belongs to this colony for example is known as Tagat, GlyceroxL, Capmul, for example PEG-15 or 20 glyceryl laurate esters (S) or tristerin (S) or olein (L), PEG-30 or 40 glyceryl laurate esters (S) or tristerin (S), PEG-50 or 60 glyceryl laurate esters (S) or tristerin (S) etc., but the example that the part commercialization obtains comprises: stearic acid polyethyleneglycol glyceride (S) (GELUCIRE50/13, Stearoyl polyoxyl-32glycerides, mp46～51 ℃), Gelucire 44/14 (S) (mp42.5～47.5 ℃, Gelucire44/14), Gelucire39/01 (mp39HLB=1), Gelucire50/01, Gelucire50/02, pegoxol 7 stearate (S) 63 fusing points: 46～53 ℃), the Polyethylene Glycol of above-mentioned one or more and glycerol fatty acid ester,

C), alkylene polyol ethers or ester or alcohol-grease group-transfer product, that suitable is C _3～5the ether of alkylene triol, especially glycerol or ester, suitable C _3～5alkylene three alcohol ethers or ester comprise mixed ether or alcohol, comprise other ether or the compound of ester component, for example C _3～5alkylene three alcohol esters and other be single, two or the transesterification product of polyhydric alcohol, especially suitable alkylene polyol ethers or ester are mixed C _3～5the alkylene triol/or poly-(C _2～4alkylidene) diol fatty acid ester, especially mixed glycerol/or Polyethylene Glycol or polypropylene glycol fatty acid ester; According to the present invention, especially suitable alkylene polyol ethers or ester comprise and can pass through glyceride (for example triglyceride) and poly-(C _2～4alkylidene) glycol (for example Polyethylene Glycol) and at random glycerol carry out transesterification reaction and the product that obtains; This class ester exchange offspring generally passes through at poly-(C _2～4alkylidene) glycol for example Polyethylene Glycol and at random glycerol have lower alcoholysis glyceride for example triglyceride be (, realizing from glyceride to ployalkylene glycol/or the transesterification of glycerol composition, namely by the ployalkylene glycol alcoholysis/or glycerolysis) obtain.In general, the reaction of this class is by noble gas, high temperature, constantly the reaction of specified composition under stirring (glyceride, ployalkylene glycol and at random glycerol) realizes; Preferred glyceride is fatty acid triglycercide, for example (C _10～22fatty acid) triglyceride, comprise natural and hydrogenated oil and fat, and especially vegetable oil and hydrogenated oil and fat thereof, as olive oil, almond oil, Oleum Arachidis hypogaeae semen, Oleum Cocois, Petiolus Trachycarpi oil, Oleum Glycines and wheat germ oil, especially, contain abundant (C _12～18fatty acid) the natural or hydrogenated oil and fat of ester residue; Preferred ployalkylene glycol material is Polyethylene Glycol, its molecular weight is generally approximately 100 to about 10000(its degree of polymerization and is generally 2 to 200), preferably approximately 200 to approximately 7500 or 6000, more preferably approximately 400 to approximately 5000, more preferably approximately, 600 to approximately 2500, more preferably approximately 1000 to approximately 2500, best 1500 to 2000; Therefore, suitable alkylene polyol ethers or ester comprises C _3～5alkylene three alcohol esters (list for example existed with variable relative quantity-, two-, three-ester) and poly-(C _2-4alkylidene) glycol list-and two-ester and a small amount of free C _3～5alkylene triol and free poly-(C _2～5alkylidene) mixture of glycol, as set forth above, preferred alkylene three alcohol moieties are glyceryls, preferred ployalkylene glycol be partly Polyethylene Glycol, especially molecular weight be about 500 to approximately 4000 those, preferred fatty acid part is C _10～22the fatty acid ester residue, especially saturated C _10～22the fatty acid ester residue; Therefore, or especially suitable alkylene polyol ethers or ester can be defined as: natural or hydrogenated vegetable oil and Polyethylene Glycol and the product that at random glycerol carries out ester exchange; Or contain the glycerol list-, two-, three-atomic number is C8～C32, C10～C22 more preferably, more preferably the fatty acid ester of C12～C18 and polyethyleneglycol-and two-atomic number be C8～C32, C10～C22 more preferably, the more preferably compositions of the fatty acid ester of C12～C18 (optionally and as a small amount of dissociative glycerin and free Polyethylene Glycol) or the compositions formed by them.General preferred iodine number is up to 2 alkylene polyol ethers or ester.Should be understood that the mixture of addressing following alkylene polyol ethers or ester also can be for compositions of the present invention.

In other words, above-mentioned alkylene polyol ethers or ester comprise the product of alcohol-grease group-transfer effect.Specifically, the product that can be used for alcohol of the present invention-grease group-transfer effect comprises alcohols or as glycerol, propylene glycol, ethylene glycol, Polyethylene Glycol, Sorbitol, the polyalcohols such as tetramethylolmethane, with natural and/or it is hydrogenated oil or oil-soluble vitamins for example, Oleum Ricini, the Oleum Ricini be hydrogenated, vitamin A, vitamin D, vitamin E, vitamin K, edible vegetable oil for example, Semen Maydis oil, olive oil, Oleum Arachidis hypogaeae semen, palmolive core oil, almond oil, the esters that the Semen Juglandis wet goods generates, the surfactant that belongs to this colony for example is known as Emalex, Cremophor, Emulgante, Eumulgin, Nikkol, Thornley, Simulsol, Cerex, Crovol, Labrasol, Softigen, Gelucire, vitamin E TPGS, for example PEG-20 Oleum Ricini (L) or the Oleum Ricini (L) be hydrogenated or Semen Maydis oil glyceride (L) or Semen Juglandis oil glyceride (L), PEG-23 Oleum Ricini (L), the Oleum Ricini that PEG-25 is hydrogenated (L) or trioleate (L), Cremophor ELP (L), PEG-30 Oleum Ricini (L) or the Oleum Ricini (L) be hydrogenated, PEG-38 Oleum Ricini (L), PEG-40 Oleum Ricini (L) or the Oleum Ricini (P) be hydrogenated or palmolive core oil (L), the Oleum Ricini that PEG-45 is hydrogenated (P), PEG-50 Oleum Ricini (L) or the Oleum Ricini (P) be hydrogenated, PEG-56 Oleum Ricini (L), PEG-60 Oleum Ricini (P) or the Oleum Ricini (P) be hydrogenated or Semen Maydis oil glyceride (L) or Semen Juglandis oil glyceride (L), the Oleum Ricini that PEG-80 is hydrogenated (P), PEG-90 Oleum Ricini (S) or the Oleum Ricini (S) be hydrogenated, PEG-100 Oleum Ricini (S) or the Oleum Ricini (S) be hydrogenated, the PEG-200 Oleum Ricini, PEG-8 is sad/or caprin, PEG-50 castor oil hydrogenated (S), PEG-60 castor oil hydrogenated (S), PEG-80 castor oil hydrogenated (S), PEG-100 castor oil hydrogenated (S), PEG-6 is sad/or caprin, lauroyl Polyethylene Glycol-32 glyceryl alcohol (S), stearoyl macrogol glyceride (S), fertility base PEG-1000 succinate (TPGS) (S), the alcohol of above-mentioned one or more-grease group-transfer product,

Following its solid example is preferred for the present invention: HETOXIDE HC-60, Jeechem CA-100, Jeechem CA-200(MP, 125 ℃), Jeechem CAH-60, Jeechem CAH-100, Jeechem CAH-200(MP, 125 ℃), Nikkol HCO-80, Nikkol HCO-100, Polyoxyl60hydrogenated castor oil (MP40), Polyoxyl40hydrogenated castor oil (MP, 30 ℃), POE Cetyl/Stearyl Ether

b3 (mp, 43-46 ℃), Polyoxyl20Cetostearyl Ether

b2PH), Macrogol Cetostearyl Ether12, Polyoxyetheyene behenyl ether, Simulsol165 (self emulsifying glyceride tristerin+PEG100 stearic acid, mp, 55-59 ℃), polyoxyethylene hydrogenated Oleum Ricini condensation substance (approximately 30 ℃ of Cremophor RH40 fusing points, approximately 45 ℃ of Cremophor RH60 fusing points), Ceteareth-6 (and) Stearyl Alcohol (Ceteareth-6 (and) Stearyl Alcohol), Ceteareth-25 (Cremophor A25), Polyglyceryl-3Distearate

gS32), NIKKOL Nikkomulese41 (behenyl alcohol, Natrulon H-10 five stearates, stearoyl dilactic acid sodium, the O/W emulsifying agent, form gel networks in water, excellent waterproof effect, there is long-acting moisture-keeping efficacy, can the various oil of emulsifying, fusing point is between 65～75 ℃), NIKKOLCeralipid PS236 (behenyl alcohol, Natrulon H-10 five stearates, stearoyl dilactic acid sodium, ceramide 3, Cer NS, Cer AP II, phytosphingosine, contain Cer NS, 3, the stable emulsion base material of 6 II, because lower than independent Cer AP fusing point, more soluble in water, during dilute with water, form layer structure, stability while keeping the ceramide dilute with water, powder), fatty alcohol-polyoxyethylene ether O-20 (MP40～42 ℃), spermol polyethers-23(mp, 49 ℃, α-cetyl-ω-hydroxyl-poly-(oxygen ethylene), poly-(oxygen ethylene) cetyl ether, polyoxyethylene ether, cetomacrogol 1000, spermol polyethers-7, spermol polyethers-13, spermol polyethers-14, spermol polyethers-15), ethylene glycol stearate (57～63 ℃ of fusing points),

Especially be suitable for alkylene polyol ethers of the present invention or ester and be well-known and can be from Gattefosse commercially available by trade name Gelucire those, particularly following product: Gelucire33/01, Gelucire35/10, Gelucire37/02, Gelucire42/12, Gelucire44/14, Gelucire46/07, Gelucire48/09, Gelucire50/02, Gelucire50/13, Gelucire53/10, Gelucire62/05.The Gelucire product is the semi-solid waxy substance of inertia with amphiphilic feature.They are identified by its fusing point and HLB value.Most of Gelucire_ kinds are the glyceride of saturated Pegylation, can carry out the polyglycols alcoholysis by natural or hydrogenated vegetable oil and Polyethylene Glycol and obtain.They are by the list of glycerol list, two and three esters and Polyethylene Glycol and the compositions of mixtures of di fatty acid ester.(H.Fiedler, above-mentioned quoted passage are rolled up 1,676 page; Manufacturer's information).

D), the polyglycerol esters that is comprised fatty acid by the fatty acid of bound to polyglycerol, wherein, (being somebody's turn to do) fatty acid (base) preferably atomic number is C8～C32, C10～C22 more preferably, the more preferably fatty acid of C12～C18 (base) or its (single or two) hydroxy fatty acid (base), above-mentioned linear saturated fatty acids (base) most preferably, the degree of polymerization of (being somebody's turn to do) polyglyceryl or polyglycerol base is preferably 2～20, and more preferably 2～10.Due to the safety of polyglyceryl fatty acid ester, they go through as food additive.With the nonionic polyoxyethylene surfactant, compare, they show fabulous oxidation stability and pH stability.Compare with sucrose, glycerol, sorbitan ester etc., there is fabulous heat stability, thereby be particularly preferred for the present invention.The surfactant that belongs to this colony for example is known as Nikkol, Decaglyn, Caprol or Polymuls, Panodan AM VEG, Citrem LC VEG, instantiation is as the monoglyceride of above-mentioned fatty acid, as lactic acid monoglyceride (HLB value 3～7, S), succinic acid monoglyceride (HLB value 5～7, fusing point is 50 ℃ of left and right approximately), citric acid monoglyceride (anionic, HLB value 4～6, S, citrate as monoglyceride), oleic acid monoglyceride, the sour monoglyceride of sad certain herbaceous plants with big flowers, diacetyl Tartaric acid monoglyceride, (HLB value 8～12, the S melting range is at 25～40 ℃), Capmul MCM C8 (40 ℃ of fusing points), Capmul MCM C10 (56～57 ℃ of melting ranges), decanoyl/octanoyl glycerides (L), glyceryl monolaurate, single, glycerol distearate (HLB value 3.5～4, S), take PGFE as main mixed emulsifying stabilizer, polyglycereol monostearate (S), preferred dimerization to ten polyglycereol stearate series (S), as PEG-5 glyceryl stearate PEG-15 glyceryl stearate, polyglyceryl-10 stearate, Tripolyglycerol monostearates (HLB value 6～8, S), dimerization to ten polyglycerol acrylate series (L), as polyglyceryl-10 list and dioleate, dimerization to ten POGE-A POGE-B POGE-C Polyglycerin palmitate series (L), dimerization to ten polyglycereol myristinate series (L), dimerization to ten polyglycereol laurate series (L), as polyglyceryl-10 laurate, the poly-monoricinolein series (L) of polyglycereol, polyglyceryl gathers ricinoleate ester, two polyglycereol dimerization hydroxy stearic acid ester B-18BPH (S), three polyglycereol diisopstearate C-18BI (L), other examples as, lipophile: polyglycereol-2 stearate, polyglycereol-4 oleate, polyglycereol-4 five stearate (anti-fat crystallization agent), polyglycereol-6 tristearate, polyglycereol-6 five stearate (anti-fat crystallization agent), Natrulon H-10 tristearate, Natrulon H-10 five stearates, Natrulon H-10 seven stearates, Natrulon H-10 tristearate, Natrulon H-10 penta hydroxy group stearate, Natrulon H-10 seven hydroxy stearic acid esters, hydrophilic: polyglycereol-6 stearate, Natrulon H-10 stearate, Natrulon H-10 distearate, but the example that the polyglycerol fatty acid commercialization obtains comprises: polyglycereol-2 stearate (Nikkol DGMS, Nikko), polyglycereol-2 oleate (Nikkol DGMO, Nikko), polyglycereol-2 isostearate (Nikkol DGMIS, Nikko), polyglycereol-3 oleate (3GO, ABITEC), polyglycereol-4 oleate (Nikkol Tetraglyn1-O, Nikko), polyglycereol-4 stearate (Nikkol Tetraglyn1-S, Nikko), polyglycereol-6 oleate (Drewpol6-1-O, Stepan), Natrulon H-10 laurate (Nikkol Decaglyn1-L, Nikko), Natrulon H-10 oleate (Nikkol Decaglyn1-O, Nikko), Natrulon H-10 stearate (Nikkol Decaglyn1-S, Nikko), polyglycereol-6 ricinoleate (Nikkol Hexaglyn PR-15, Nikko), Natrulon H-10 linoleate (NikkolDecaglyn1-LN, Nikko), polyglycereol-6 five oleate (Nikkol Hexaglyn5-O, Nikko), polyglycereol-3 dioleate (Cremophor GO32, BASF), polyglycereol-3 distearate (Cremophor GS32, BASF), polyglycereol-4 five oleate (Nikkol Tetraglyn5-O, Nikko), polyglycereol-6 dioleate (6G20, ABITEC), polyglycereol-2 dioleate (Nikkol DGDO, Nikko), Natrulon H-10 trioleate (Nikkol Decaglyn3-O, Nikko), Natrulon H-10 five oleates (Nikkol Decaglyn5-O, Nikko), Natrulon H-10 seven oleates (Nikkol Decaglyn7-O, Nikko), Natrulon H-10 four oleate (10G4O, ABITEC), Natrulon H-10 ten isostearates (Nikkol Decaglyn10-IS, Nikko), Natrulon H-10 10 oleate (Drewpol10-10-O, Stepan), polyglyceryl-10 is single, dioleate (PGE860, ABITEC), and polyglycerol polyricinoleate (Polymuls, Henkel), the polyglycerol fatty acid of above-mentioned one or more,

Its preferred example (lauric acid～) stearate as single as: polyglycereol-2～10, polyglycereol-5～10 pair (lauric acid～) stearate, polyglycereol-7～10 3 (lauric acid～) stearate, Natrulon H-10 three～seven hydroxyls (lauric acid～) stearate.

E), there are for example 2 to 100, preferably 5 to 50, more preferably 10 to 50 [CH ₂-CH ₂-O] unit, most preferably (or polyethylene glycol groups polymerization number is 2 to 100 in 20 to 40 these unit, preferably 5 to 50, more preferably 10 to 50, most preferably 20 to 40) Polyethylene Glycol (PEG) sterol ether also comprises itself and polyoxyethylene alkyl ether combination, the polyethyleneglycol derivative that for example the stearyl alcohol derivant comprises stearyl alcohol for example, PEG-24 cholesterol ethers, PEG-30 gallbladder alcohol, PEG-25 vegetable stearin alcohol, PEG-30 Semen sojae atricolor stearyl alcohol etc.; (surfactant that belongs to this colony for example is known as Solulan or Nikkol BPSH); Preferred polymers is known and is commercially available acquisition, commodity are called Solulan C24 (Choleth24 (with) Ceteth24), purchased from Amerchol, or commodity Forlan C-24 by name (Choleth24 (with) Ceteth24), purchased from R.I.T.A.Corp; Also adaptable similar products are that those are known and be commercially available acquisition, commodity are called Nikkol BPS-30 (polyethoxylated 30 plant sterols) or Nikkol BPSH-25 (polyethoxylated 25 phytostanols (phytostanol)), purchased from for example Nikko Chemicals Co., Ltd;

F), polyethylene glycol sorbitan fatty acid esters also can be for preparation of the present invention, wherein, (being somebody's turn to do) fatty acid (base) preferably atomic number is C8～C32, C10～C22 more preferably, the more preferably fatty acid of C12～C18 (base) or its (single or two) hydroxy fatty acid (base), above-mentioned linear saturated fatty acids (base) most preferably, (being somebody's turn to do) polyethylene glycol groups polymerization number is preferably approximately 2 to approximately 100, be more preferably approximately 4 to approximately 60, more preferably approximately 4 to approximately 40, more preferably approximately 4 to approximately 20, Polyethylene Glycol sorbitan monostearate (liquid) for example, PEG-10 sorbitol anhydride laurate, PEG-20 sorbitol anhydride monolaurate or sorbitol anhydride tristearate or sorbitan mono-oleic acid ester or SPAN85 or sorbitol anhydride list isostearate or sorbitol anhydride monopalmitate or sorbitan monostearate, PEG-4 sorbitol anhydride monolaurate, the PEG-5 sorbitan mono-oleic acid ester, PEG-6 sorbitan mono-oleic acid ester or Span-20 or sorbitan monostearate, the PEG-8 sorbitan monostearate, PEG-30 sorbitol anhydride four oleates, PEG-40 sorbitan mono-oleic acid ester or sorbitol anhydride four oleates, PEG-60 sorbitol anhydride tetrastearate, PEG-80 sorbitol anhydride monolaurate, PEG sorbitol anhydride six oleates, polyoxyethylene (30/40/60EO) sorbitol four oleates, Emulsifier LT-60M etc., its preferred embodiment is as Tween61 (S), Tween65 (S), the surfactant that belongs to this colony for example is known as Liposor, Tween, Dacol MSS, Nikkol, Emalex, Atlas), the polyethylene glycol sorbitan fatty acid esters of above-mentioned one or more,

G), polyalkylene glycol alkyl is C8～C32 as carbon number, C10～C22 more preferably, the more preferably saturated or unsaturated alkyl of C12～C18 or its (single or two) hydroxy alkyl ethers, preferred above-mentioned straight chain saturated alkyl alcohol ether, wherein, (being somebody's turn to do) Polyethylene Glycol based polyalcohol number is approximately 2 to approximately 100, preferably approximately 2 to approximately 60, more preferably from about 10 to approximately 60, more preferably approximately 10 to approximately 50, most preferably be approximately 10 to approximately 40, its available example is as PEG-lauryl ether (liquid, as PEG-9 lauryl ether (liquid), PEG-23 lauryl ether (liquid)), PEG-10 oleyl ether or Petiolus Trachycarpi (cetyl) ether (Gu, water-soluble, a, o) or stearic (octadecyl) ether (Gu, water-soluble, a, o), PEG-20 oleyl ether or palmityl ether or or stearyl ether, PEG-100 stearyl ether etc., the example of polyethylene glycol alkyl ether hydrophilic SA wherein is as Polyethylene Glycol (60EO) sorbitol four stearyl ethers (liquid), laureth-21, laureth-25, spermol polyethers-6, spermol polyethers-7, spermol polyethers-10, spermol polyethers-15, spermol polyethers-20, spermol polyethers-23, spermol polyethers-25, spermol polyethers-30, spermol polyethers-40, stearyl alcohol polyethers-20, oleth-20, oleth-50, behenyl alcohol polyethers-10, behenyl alcohol polyethers-20, behenyl alcohol polyethers-30, C12-15 alkanol polyethers-10, the PEG-20 plant sterol, the PEG-25 plant sterol, the PEG-30 plant sterol, the example of polyethylene glycol alkyl ether lipophile SA wherein is as spermol polyethers-2, stearyl alcohol polyethers-2, stearyl alcohol polyethers-4, behenyl alcohol polyethers-5, PPG-4-spermol polyethers-20, PPG-8-spermol polyethers-20, PPG-6-decyl tetradecyl alchohol polyethers-12, PPG-6-decyl tetradecyl alchohol polyethers-20, PPG-6-decyl tetradecyl alchohol polyethers-30, lanolin alcohol polyethers-30, lanolin alcohol polyethers-40(Wool wax alcohols,ethoxylated/or lanolin alcohol/or the Cera Flava derivant), sorbitol polyethers-20 Cera Flava, sorbitol polyethers-6 Cera Flava, the surfactant that belongs to this colony for example is known as Volpo, Brij, the polyethylene glycol alkyl ether of above-mentioned one or more,

Also operable similar products are PULLRONIC F68 alkyl ether, for example C ₁₂to C ₁₈alcohol polyoxyethylene polyoxypropylene ether, as polyoxyethylene-20-polyoxypropylene-4-cetyl ether, it is well-known and commercially available acquisition, can carry out Nikkl Chemicals Co.Ltd freely, trade mark is NikkolPBC34 (Fiedler, above-mentioned quoted passage., roll up 2,1239 pages); Polyoxypropylene fatty acid ether, for example AccononE also can come into operation; In addition, the polyoxyethylene alkyl ether phosphate ester also can be for preparation of the present invention, and the example is as, two C12-15 alkanol polyethers-10 phosphate esters (not and type, neutralize with alkali according to application target), three-(C12-15 alkanol polyethers-10) phosphate esters;

H), sugar esters is C8～C32 as carbon number, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid sugar esters, preferred above-mentioned saturated straight chain sucrose fatty acid ester class, such as sucrose distearyl acid/or monostearate (S), sucrose monolaurate (S) etc., the surfactant that belongs to this colony for example is known as Sucro ester, Crodesta, sucrose monolaurate, but the example that the sugar ester commercialization obtains comprises: sucrose distearate (SUCRO ESTER7, Gattefosse), sucrose distearate/or monostearate (SUCRO ESTER11, Gattefosse), the sucrose dipalmitate, sucrose monostearate (Crodesta F-160, Croda), sucrose (list) cetylate (SUCRO ESTER15, Gattefosse) (S), and sucrose monolaurate (Saccharose monolaurate 1695, Mitsubisbi-Kasei).Preparation of the present invention according to the present invention can comprise the sugar ester of above-mentioned one or more;

I), polyalkylene glycol alkyl phenol (S) also can be for preparation of the present invention; (being somebody's turn to do) polyalkylene glycol alkyl degree of polymerization is preferably 4～100 (more preferably 10～40); the preferred carbon number of (being somebody's turn to do) alkyl is C8～C32; C10～C22 more preferably; the more preferably saturated or unsaturated alkyl of C12～C18 or its (single or two) hydroxy alkyl; preferred above-mentioned straight chain saturated alkyl; for example PEG-10～100 nonyl phenols (Triton X series), PEG-15～100 octyl phenol ethers (Triton N series, Rohm& Haas) etc., the polyalkylene glycol alkyl phenol of above-mentioned one or more;

J), polyoxy ethylene-polyoxy propylene-based block copolymer (poloxalkol class (poloxamers), usually selecting mean molecule quantity is 1000～20000, more preferably mean molecule quantity is 2000～20000, more preferably mean molecule quantity is 2000～10000, the poloxalkol that most preferably mean molecule quantity is 4000～10000, and the mass ratio that oxyethylene group (oxyethylene) accounts in molecule (Weight percent oxyethylene) is generally 5%～95%, be preferably 30%～90%, be more preferably 40%～90%, be 45%～85% best, preferred embodiment is as poloxamer108 (L), poloxamer124 (L), poloxamer188, poloxamer237, poloxamer288, poloxamer338, poloxamer407 etc., (surfactant that belongs to this colony for example is known as Synperonic PE, Pluronic, Emkalyx, LutrolTM, Supronic, Monolan, Pluracare, Plurodac),

K), ionic surfactant comprises acid (property) surfactant and salt (anionic), alkali formula (property) surfactant and salt (cationic) and zwitterionic surfactant, some available types as:

Containing senior alkyl, (term " senior alkyl " refers to carbon number C8-C32 herein, C10-C22 preferably, saturated or the unsaturated alkyl of C12-C18 or its (single or two) hydroxy alkyl best, preferred above-mentioned straight chain saturated alkyl, do not indicate implication all herewith especially at this paper.Usually in each surfactant molecule containing the senior alkyl of 1 or 2, this is conducive to surfactant stripping from lipidic matrix, the below implication is herewith) the cationic surfactant class, as senior alkyl three ammonium halogenide, senior alkyl trimethyl ammonium halogenide, senior alkyl trimethyl ammonium halogenide, senior alkyl ammonium halogenide, senior alkyl benzyl dimethyl ammonium salt class, diisobutyl phenoxy group ethyoxyl dimethyl benzyl ammonium salt, (senior) alkyl pyridine salt, betaines (betanin that comprises senior alkyl in molecular structure), (comprising senior alkyl in molecular structure) is by the amine of ethoxyquin (polyoxy vinyl-15 coconut amine), N-senior alkyl acylamino acid, N-senior alkyl acylsarcosine, the alkane esters salt that the senior alkane acyl of N-basic amino acid carbon number is C1-C6, N-senior alkyl Gemini class basic amino acid salt surfactant (wherein, the n in-NH-(CH2) n-NH-is 1-18,3-12 preferably, more preferably, 3-9), the N-carbon number is C1-C12's (preferably C1-C8, more preferably C1-C3) alkyl acyl-basic amino acid senior alkyl glyceride salt surfactant etc.,

The senior alkyl sulfosuccinate, senior alkyl ether-2 sulfosuccinate, the alkane sulfonate that senior alkyl acyl methylamine carbon number is C1～C6, higher alkyl sulfates, the senior alkyl taurate, the senior alkyl ether sulfate, senior alkyl glyceryl ether sulfonate esters, the senior alkyl fatty alcohol polyoxyethylene ether sulfate, senior alkyl phosphate esters, the esterification products of senior alkyl aliphatic alcohols or fatty alcohol ethoxy hydrochlorate and phosphoric acid or anhydride, the carboxylic acid that senior alkyl acyl (ester)-carbon number is C1～C6 and salt thereof (polybasic carboxylic acid and salt thereof that preferably carbon number is C2～C6), the carboxylic acid that senior alkyl ether-carbon number is C1～C6 and salt thereof (polybasic carboxylic acid and salt thereof that preferably carbon number is C2～C6), the carboxylic acid that senior alkyl keto-alcohol-carbon number is C1～C6 and salt thereof (polybasic carboxylic acid and salt thereof that preferably carbon number is C2～C6), La Nuoer (Niranol) C2M (acid) that contains senior alkyl in molecular structure, sulphonate-base is for succinic acid two higher alkyl esters, the carboxylic acid that senior alkyl (single and/or two senior alkyls) glycerol carbon number is C1～C6 and salt (polybasic carboxylic acid and salt thereof that preferably carbon number is C2～C6) ester thereof, the carboxylic acid that senior alkyl acyl propylene glycol carbon number is C1～C6 and salt thereof ((polybasic carboxylic acid and salt thereof that preferably carbon number is C2～C6) ester, the carboxylic acid that senior alkyl acyl group carbon number is C1～C6 and salt thereof (polybasic carboxylic acid and salt thereof that preferably carbon number is C2～C6) ester, the senior alkyl acyl-lactate, contain the biosurfactant of senior alkyl in molecular structure (as cholic acid salt surfactant, senior alkyl acyl-peptide condensation substance, phospholipid is (as the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, the acid glycosyl sphingolipid class (gangliosides) that contains senior alkyl in molecular structure), rhamnolipid I-IV, sophorolipid, Ke Linuo Mike acid (Corynornycolic acid), this Boksburg acid (spi-culisporic acid), alginate, propylene glycol alginate, and the pharmaceutical salts of above-mentioned surfactant, and their mixture.

In following per molecule containing the acid surface active agent of the senior alkyl of 1 or 2 for more preferably; because it has biocompatibility more preferably: carboxylic acid multicomponent carboxylate, the senior alkyl acyl group carbon number that the multi-carboxylate that senior alkyl glycerol carbon number is C2～C6, senior alkyl acyl propylene glycol carbon number are C2～C6 is the biosurfactant that contains senior alkyl in C2～C6 multi-carboxylate, senior alkyl acyl group lactic acid, molecular structure; and their pharmaceutical salts, and their mixture.

Some available instantiations as, but be not limited to this: dioctyl sulfosuccinate (dioctyl ester sulfosuccinate), octyl group sulfosuccinate, 9-undecylenic acid single ethanol amide sulfosuccinate, as octyl group disodium sulfosuccinate, endecatylene amide groups-MEA-disodium sulfosuccinate, Laurel ether-2 sulfosuccinate, N, N-oleoyl methyl tauride, (just) lauryl sulfate (being preferred), (just) hexadecanoyl sulfate, stearoyl sulfate, tetradecyl sulfate, cocos nucifera oil/or hydrogenated tallow sulfate, (just) dodecanoate, oleate, (just) myristate, palmitate, ricinate, stearate, lauroyl taurate and methyl cocoyl taurate, Laurel ether-6 citrate, PEG-4 lauramide (amido) carboxylate, laureth-6 carboxylate, PEG-6 cocamidopropyl carboxylate, Laurel ether-13 carboxylate, PEG-6 cocos nucifera oil amido-carboxylic acids salt, PEG-7-olive oil-carboxylate, PEG Laurel ether-3 carboxylate, octyl ether-9 carboxylate, cetyl ether-13 carboxylate, the coconut palm ether sulfate, polyoxyethylene lauryl ether sulfate, octyloxy alcohol-carboxylate, sulphonate-base is for dioctyl succinate, acetyl tartaric acid list/or diglycerol ((just) dodecoic acid is to (just) stearic acid) ester, the diacetyl tartaric acid list/or diglycerol ((just) dodecoic acid is to (just) stearic acid) ester (Diacetyl tartaric acid esters of mono-and diglycerides of fatty acids), oxalyl tartaric acid glycerol list/or two ((just) dodecoic acid is to (just) behenic acid) ester, mixing acetic acid and tartaric acid list/or diglycerol ((just) dodecoic acid is to (just) behenic acid) ester (Mixed acetic and tartaric acid esters of mono-and diglycerides of fatty acids, acetic acid tartaric acid mixing glycerol one/or two ((just) dodecoic acid is to (just) behenic acid) ester), citric acid glycerol list/or two ((just) dodecoic acid is to (just) behenic acid) ester, succinic acid glycerol list/or two ((just) dodecoic acid is to (just) behenic acid) ester, tartaric acid glycerol one/or two ((just) dodecoic acid is to (just) behenic acid) ester, lactic acid glycerol list/or two ((just) dodecoic acid is to (just) behenic acid) ester (Lactic acid esters of mono-and diglycerides of fatty acids), acetic acid glycerol one/or two ((just) dodecoic acid is to (just) behenic acid) ester (Acetic acid esters of mono-and diglycerides of fatty acids is mono--and the list of two glycerolipids/or ((just) dodecoic acid is to (just) behenic acid) esters of diacetyl) (just), octadecanol citric acid glyceryl monoacetate, (annotate: this paper symbol "/" mean "or" or " and/or " or the meanings such as " reach ", in order to simplify, generally no longer other local marks, in an embodiment in measurement units such as "/sheets ", mean to be illustrated in every single unit, be equivalent to " often " or English " per ", " every " or " " per sheet ", first list and compare at this) single (just) dodecoic acid is to (just) behenic acid acyl citrate ester, tartrate list (just) dodecoic acid to (just) behenic acid acyl ester, (just) dodecoic acid to (just) behenic acid acyl butene dioic acid salt, (just) dodecoic acid to (just) behenic acid acyl propylene glycol succinate salt, decoyl lactate, lauroyl lactate, tetradecylic acid lactate, hexadecylic acid lactate, stearyl lactylic acid salt, isostearoyl lactate, oleoyl lactate, cocos nucifera oil acyl lactate, 12-hydroxyl stearyl lactylic acid salt, stearoyl-2-lactate, Oleum Ricini acyl lactate and (just) docosane acyl-lactate, stearoyl-2-lactate, stearic acid lactate, N-senior alkyl acylglycine, N-senior alkyl acyl group alanine, N-senior alkyl acyl group valine, N-senior alkyl acyl glutamic acid, N-senior alkyl acylaspartic acid, N-senior alkyl acyl group-N-methyl-Beta-alanine, N-senior alkyl acyl glutamic acid, N-senior alkyl acylaspartic acid, two-TEA-palmityl aspartic acid, capryl/or caprin glutamic acid, oleoyl glutamic acid, lauroyl glutamic acid, the oleoyl glycine, stearoylglycine, the lauroyl alanine, myristoyl sarcosine, TEA lauroyl sarcosine, Hamposyl S, Hamposyl L, Hamposyl C, N-Oleoylsarcosine, palmitoyl sarcosine, cholate, taurocholate, dexycholate, glycocholate, glycodeoxycholate, taurodeoxycholate, ursodeoxycholic hydrochlorate, CDC, chenodeoxycholyltaurine salt, glycochenodeoxycholate salt, senior alkyl acyl glycyl is for propylhomoserin (as, oleoyl glycyl for propylhomoserin, lauroyl acyl glycyl for propylhomoserin, stearoyl glycyl for propylhomoserin), the acid of just long aliphatic chain phosphoglyceride, for example n-ether-glycerol-phosphatidic acid, specifically lauroyl glycerol-phosphatidic acid, oleoyl glycerol-phosphatidic acid, n-tetradecane base-glycerol-phosphatidic acid, positive long-chain phosphoserine, specifically lauroyl-(/ or myristoyl-/or oleoyl-/or palmityl-/or stearoyl) phosphoserine, octadecylene acyl-phosphoserine, egg/or soybean lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, phosphatidyl ethanolamine, phosphatidyl glycerol, phosphatidyl serine,

N α-senior alkyl (as (just) ten to (just) 18) acyl arginine first/or ethyl ester salt, N α-senior alkyl (as (just) ten to (just) 18)) acyl lysine first/or ethyl ester salt, N α-senior alkyl (as ten to 18)) acyl histidine first/or ethyl ester salt;

N1, N3-bis-(N-senior alkyl (as (just) ten to (just) 18)) acyl arginine/or lysine/or histidine)-1,3-propane diamine salt, N1, N6-bis-(N-senior alkyl (as (just) ten to (just) 18)) acyl arginine/or lysine/or histidine)-1,6-hexamethylene diamine salt, N1, N9-bis-(N-senior alkyl (as (just) ten to (just) 18)) acyl group arginine/or lysine/or histidine)-1,9-nonamethylene diamine salt;

1,2-bis-(senior alkyl (as (just) ten to (just) 18)) acyl group)-3-(N-acetyl group arginyl/or lysine/or histidine) glycerol salt;

Senior alkyl (as (just) ten to (just) 18) bromination triamine, senior alkyl (as (just) ten to (just) 18) bromination trimethylamine, senior alkyl (as (just) ten to (just) 18) bromination trimethylamine, senior alkyl (as (just) ten to (just) 18) ammonium chloride, senior alkyl (as (just) ten to (just) 18) phenyl dimethylamine salt, diisobutyl phenoxy group ethyoxyl dimethyl benzyl amine salt, Fixanol, betanin (trialkyl glycine), lauroyl betanin (N-lauroyl, N, N-dimethylamino acetic acid), and ethoxylated amine (polyoxyethylene-15 coco amine),

Alkalescence senior alkyl acyl-peptide condensation substance (available example is as N-Cortex cocois radicis acyl arginine-ethyl ester of lysine, N-stearoyl arginine-HIS-ALA-threonine-lysine);

The alkalescence glycosyl sphingolipid, as sphingosine, ceramide, sphingomyelins;

And the pharmaceutical salts of above-mentioned surfactant (comprising above-mentioned each example of enumerating), the salt formed as itself and following medicinal acid or alkali, particularly its ammonium salt, sodium salt, potassium salt, or its hydrochlorate, hydrobromate, sulfate, sulphite, nitrate, phosphate, carbonate etc.; And the mixture of above-mentioned surfactant (comprising above-mentioned each example of enumerating) and pharmaceutical salts thereof.

The example of the particularly preferred ionic surfactant of part comprises: sodium stearoyl lactate/or potassium/or ammonium, Sodium caproate/or potassium/or ammonium, sodium caprylate/or potassium/or ammonium, Capric acid sodium salt/or potassium/or ammonium, sodium laurate/or potassium/or ammonium, Sodium myristate/or potassium/or ammonium, sodium palmitate/or potassium/or ammonium, palmitoleic acid sodium/or potassium/or ammonium, enuatrol/or potassium/or ammonium, sodium ricinate/or potassium/or ammonium, linoleic acid sodium/or potassium/or ammonium, linolenic acid sodium/or potassium/or ammonium, sodium stearate/or potassium/or ammonium, lauryl (dodecyl) sodium sulfate/or potassium/or ammonium, 12 (/ or four) alkyl sodium sulfate/or potassium/or ammonium, sodium lauryl sarcosinate/or potassium/or ammonium, dioctyl sodium sulphosuccinate/or potassium/or ammonium, sodium cholate/or potassium/or ammonium, sodium taurocholate/or potassium/or ammonium, sodium glycocholate/or potassium/or ammonium, NaTDC/or potassium/or ammonium, sodium taurodeoxycholate/or potassium/or ammonium, Glycodeoxrycholic acid/or potassium/or ammonium, ursodesoxycholic acid sodium/or potassium/or ammonium, chenodeoxy cholic acid sodium/or potassium/or ammonium, cattle sulphur chenodeoxy cholic acid sodium/or potassium/or ammonium, glyceryl chenodeoxy cholic acid sodium/or potassium/or ammonium, CHOLYLSARCOSINE sodium/or potassium/or ammonium, N-formyl sodium taurocholate/or potassium/or ammonium, lecithin, hydrogenated soy phosphatidyl choline, two myristoyl lecithin, lecithin, hydrolecithin, lysophosphatidylcholine, cuorin, (nerve) sphingomyelins, PHOSPHATIDYL ETHANOLAMINE, phosphatidic acid, the phosphatidyl glycerol, Phosphatidylserine, phospholipid, the succinyl monoglyceride, stearoyl propylene glycol hydrogen succinate salt, single/or diacetyl group tartaric acid monoglyceride and diester, citric acid monoglyceride diester, lactoglyceride, acyl group lactoyl compound, fatty acid lactoyl ester, stearoyl-2 lactoyl sodium/or potassium/or ammonium, stearoyl lactoyl sodium/or potassium/or ammonium, alginate, propylene glycol alginate, above-mentioned salt surfactant comprises the pharmaceutical salts described above that other can be associated naturally.

L), some available important lipophilic surfactants (SA) as:

L-1), the anhydrous sorbitol fatty acid is (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) ester also can be for preparation of the present invention, its HLB value 4.7,52～57 ℃ of fusing points, the example is as sorbitan stearate, the smooth sesquistearate of Pyrusussuriensis, the smooth tristearate of Pyrusussuriensis, but the example that the sorbitan fatty acid ester commercialization obtains comprises: sorbitan mono-laurate (Span-20, Atlas/ICI, faint yellow to yellow paste, be dissolved in oils and multiple organic solvent, be insoluble to cold water, can be scattered in hot water), anhydrous sorbitol monopalmitin (Span-40, Atlas/ICI), sorbitan monooleate (Span-80, Atlas/ICI), sorbitan monostearate (Span-60, Atlas/ICI, white or faint yellow waxy solid, be dissolved in oils and multiple organic solvent, be insoluble to cold water, can be scattered in hot water), sorbitan trioleate (Span-85, Atlas/ICI), sorbitan sesquioleate (Arlacel-C, ICI), anhydrous sorbitol tristearate (Span-65, Atlas/ICI), anhydrous sorbitol list isostearate (Crill6, Croda), with anhydrous sorbitol sesquistearate (Nikkol SS-15, Nikko), the sorbitan fatty acid ester of above-mentioned one or more,

L-2), the polypropylene glycol fatty acid is (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) ester also can be for preparation of the present invention, as propylene glycol fatty acid (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) (this product is nonionic emulsifier to ester, HLB value 2-3, white is to yellow solid or thick liquid, odorless.It is lipophilic emulsifier, water insoluble, dissolve in ethanol, ethyl acetate, chloroform etc.), but the example that its commercialization obtains comprises: Capryol 90 (Capryol90, Gattefosse), PGML (Lauroglycol90, Gattefosse), propylene glycol oleate (Lutrol OP2000, BASF), propylene glycol myristic acid myristate (Mirpyl), propylene glycol monostearate (LIPO PGMS, Lipo Chem.), the propylene glycol hydroxy stearic acid ester, propylene glycol ricinoleate (PROPYMULS, Henkel), the propylene glycol isostearate, propylene glycol mono-oleate (Myverol P-O6, Eastman), the sad dicaprate (200 of propylene glycol two, ABITEC), propylene glycol dicaprylate (800, ABITEC), the sad decanoin of propylene glycol (LABRAFAC PG, Gattefosse), the propylene glycol dilaurate, propylene glycol distearate (PGDS, Stepan), propylene glycol dicaprylate (Nikkol Sefsol228, Nikko), and propylene glycol dicaprate (Nikkol PDD, Nikko), the methyl glycol fatty acid ester of above-mentioned one or more,

L-3), propylene glycol fatty acid is (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) ester and glycerol fatty acid be (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) mixture of ester also can be for the lipophilic surfactant of preparation of the present invention, a kind of preferred compound forms (Arlacel186) by the oleate of propylene glycol and glycerol, the example of these surfactants comprises: its oleate (ATMOS300, ARLACEL186, ICI), with its stearate (ATMOS150), the propylene glycol ester of above-mentioned one or more and the mixture of glycerine ester,

L-4), in addition, glycerol one fatty acid is (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) ester and/or difatty acid be (as carbon number is C8～C32, C10～C22 more preferably, the more preferably saturated or unsaturated fatty acid of C12～C18 or its (single or two) hydroxy fatty acid) ester also can be for the lipophilic surfactant of preparation of the present invention, but the example that monoglyceride and diester commercialization obtain comprises: palmitoleic acid monoglyceride (C16:1) (Larodan), elaidic acid monoglyceride (C18:1) (Larodan), caproic acid monoglyceride (C6) (Larodan), SUNSOFT 700P-2 (Larodan), Sunsoft 767 (Larodan), glyceryl monolaurate (Larodan), monomyristin (C14) (Nikkol MGM, Nikko), glycerin mono-fatty acid ester (C18:1) (PECEOL, Gattefosse), glycerin mono-fatty acid ester (Myverol, Eastman), the glycerol monoleate/or linoleate (OLICINE, Gattefosse), glycerol list linoleate (Maisine, Gattefosse), glycerol ricinoleate (701, Huls), glyceryl monolaurate (MLD, Lonza), glycerol monopalmitate (Emalex GMS-P, Nihon), glycerol monostearate (GMS, ABITEC), glycerol list and dioleate (GMO-K, ABITEC), the glycerol Palmic acid/or stearate (CUTINA MD-A, ESTAGEL-G18), glyceryl acetate (EE, Grunau GmbH), glycerol monolaurate (312, Huls), glycerol citron acid esters/or lactate/or oleate/or linoleate (375, Huls), glycerol caprylate (308, HuIs), glycerol caprylate/or decanoin (MCM, ABITEC), sad list and two glyceride (988, Huls), sad/or caprin (742, Huls), list and diacetyl monoglyceride (9-45, Eastman), glyceryl monostearate (MS, Arlacel129, ICI), glycerol one and lactyl-lactic acid ester (LAMEGIN GLP, Henkel), two caproins (C6) (Larodan), two caprins (C10) (Larodan), two caprylins (C8) (Larodan), two myristin (C14) (Larodan), glycerol-1,3-dipalmitate (C16) (Larodan), distearin (Larodan), GLYCERYL DILAURATE (C12, GDL, ABITEC), glyceryl dioleate (GDO, ABITEC), fatty acid glycerine ester (GELUCIRE39/01, Gattefosse), two palmitoleic acid glyceride (C16:1) (Larodan), 1, 2 and 1, 3-glyceryl dioleate (C18:1) (Larodan), two trielaidins (C18:1) (Larodan), with dilinoleic acid glyceride (C18:2) (Larodan), the monoglyceride of above-mentioned one or more and diester,

L-5), (PEG steroid surfactant) sterin and steroid derivatives also can be for the excipient of preparation of the present invention, but the example that sterin and steroid derivatives commercialization obtain comprises: cholesterol, sitosterol, lanosterol, PEG-24 cholesterol ethers (Solulan C-24, Amerchol), PEG-30 Dihydrocholesterol (Phytosterol GENEROL series, Henkel), PEG-25 plant sterol (Nikkol BPSH-25, Nikko), PEG-5 soyasterol (Nikkol BPS-5, Nikko), PEG-10 soyasterol (Nikkol BPS-10, Nikko), PEG-20 soyasterol (NikkolBPS-20, Nikko), with PEG-30 soyasterol (Nikkol BPS-30, Nikko)., the sterin of above-mentioned one or more and steroid derivatives;

L-6), lower alcohol (C ₂～C ₄) and fatty acid (C ₈～C ₁₈) ether be for applicable lipophilic surfactant of the present invention, the example of these surfactants comprises: ethyl oleate (Crodamol EO, Croda), isopropyl myristic acid ester (Crodamol IPM, Croda), isopropyl cetylate (Crodamol IPP, Croda), ethyl linoleate (Nikkol VF-E, Nikko), with isopropyl linoleate (Nikkol VF-IP, Nikko), the lower alcohol fatty acid esters of above-mentioned one or more;

M), the Polyethylene Glycol of various molecular size ranges (PEG) is all to be suitable for the present invention's (weak surface activity cosolvent of hydrophilic), the mean molecule quantity of the polyethylene glycol polymer that can use in method and composition of the present invention can be from 200Da to 20,000Da, be preferably 800Da to 20,000Da, more preferably from 800Da to 10,000Da, most preferably be from 1 000Da to 6,000Da.Specific example comprises PEG200, PEG300, PEG400, PEG600, PEG800, PEG1,000, PEG1,200, PEG1,500, PEG2,000, PEG2,500, PEG3,000, PEG3,350, PEG3,500, PEG3,750, PEG4,000, PEG6,000, PEG8,000, PEG10,000PEG12,000, and their compositions.

N), the polyethylene glycol oxide (PEO) of various molecular size ranges is all also to be suitable for the present invention's (weak surface activity cosolvent of hydrophilic), the mean molecule quantity of the polyethylene glycol oxide (PEO) that can use in method and composition of the present invention can be from 20,000Da to 10,000,000Da, be preferably from 30,000Da to 4,000,000Da, more preferably from from 30,000Da to 1,000,000Da, most preferably be from from 30 000Da to 500,000Da.Specific example is as Polyox series: WSR N-10, WSR N-80, WSR N-750, WSR N-3000, WSR205, WSR1105, WSR N-12K, WSR N-60K, WSR301, WSR Coagulant, WSR303, and their compositions.

O), above-mentioned surfactant comprises above-mentioned each example of enumerating (arbitrarily) compositions or mixture, above-mentioned surfactant comprises formation solid dispersion or homogeneous phase solid solution and compositions or mixture between above-mentioned each example of enumerating, and their compositions or mixture, also can be used for the present invention.

Preferred surfactant in the present composition belongs to above-mentioned cithrol class, Polyethylene Glycol glycerol fatty acid ester, the alcohol-product of grease group-transfer effect, the fatty acid ester of bound to polyglycerol or polyoxy vinyl-polyoxypropylene block copolymers, PEG (particularly PEG1000～6000) class, and compositions or mixture.Preferably, the surfactant in the present composition belongs to above-mentioned polyglycol distearate class.The fatty acid ester that most preferred surfactant is bound to polyglycerol, polyoxy vinyl-polyoxypropylene block copolymers, polyoxyethylene hydrogenated Oleum Ricini (surfactant that is called as Cremophor), and vitamin E TPGS (α-fertility base-polyethanediol succinate, also be abbreviated as TGPS), Cremophor RH40 or 60 and VE TPGS and PEG1000～6000 especially.Some are preferably as castor oil derivatives (HCO60 as by name as commodity, Nikko Chemical Co., polyoxyethylene (60) castor oil hydrogenated that Ltd produces), Polysorbate (as Tween61, Tween65), polyoxyethylene stearic acid ester (as Polyethylene Glycol (40) stearate), vitamin E TPGS, PEG1000～6000, and the compositions of above-mentioned example or mixture.

In above reaching hereinafter listed suitable surfactant, listed different probabilities, for example PEG-20 Oleum Ricini or the Oleum Ricini be hydrogenated or Semen Maydis glyceride type or the Semen Juglandis glyceride type that is hydrogenated must be pronounced the Semen Juglandis oil glyceride type that Oleum Ricini that PEG-20 Oleum Ricini and PEG-20 be hydrogenated and GROVOL M-40 class and PEG-20 are hydrogenated, and other are analogized.

Two), (fusible) lipid (medicinal) additive

Pharmaceutically acceptable (fusible) lipid (medicinal) additive both can have been made above-mentioned performance enhancers component in the present invention, can make again above-mentioned fusible adhesive component.

Pharmaceutically acceptable (fusible) lipid (medicinal) additive the present invention relates to for or be selected from lipid (medicinal) additive that pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, lipid (medicinal) additive that is preferably 35 ℃～150 ℃ for fusing point, it is more preferably lipid (medicinal) additive of 43 ℃～120 ℃, it is more preferably lipid (medicinal) additive of 50 ℃～100 ℃, described lipid (medicinal) additive comprises but is not limited to fatty acid (as carbon number is C8 or the more senior fatty acid) glyceride that fusing point is not less than 25 ℃ of temperature, fatty acid (as carbon number is C14 or more senior fatty acid) propylene glycol ester, fatty acid (as carbon number is C14 or more senior fatty acid) glycol ester, fatty acid (as carbon number is C14 or more senior fatty acid) binaryglycol ester, fatty acid (as carbon number is C10 or more senior fatty acid), fatty alcohol (as carbon number is C12 or more senior fatty alcohol), the fatty acid ester fatty alcohol is (as carbon number is that C14 or more senior fatty acid carbons atomic number are C14 or more senior fatty alcohol ester, the fatty acid carbons atomic number that carbon number is C12 is C18 or more senior fatty alcohol ester, carbon number is the fatty alcohol ester that C18 or more senior fatty acid carbons atomic number are C12), aliphatic hydrocarbon (as carbon number is C31 or more senior aliphatic hydrocarbon) and the natural product that comprises them and processed goods thereof are (as vegetable and animals oils lipid, semi-synthetic oils and fats, the wax class) and composition thereof.

Wherein, above-mentioned fatty glyceride can be fatty acid glycerine one ester for example, fatty acid diglyceride, fatty acid triglycercide and their mixture, fatty acid described herein (usually) is C8～C32 or more senior fatty acid for carbon number, preferably above-mentioned positive satisfied fatty acid is (as single capric acid (ten acid), lauric acid (dodecoic acid), (meat) myristic acid (tetradecylic acid), Palmic acid (hexadecylic acid), stearic acid (stearic acid), arachidic acid (20 acid), behenic acid (behenic acid), lignoceric acid (tetracosanoic acid, lignin acid), cerinic acid (hydroxyhexacosanoic acid), montanic acid (octocosoic acid), Cera Flava acid (triacontanoic acid), lacceroic acid (lacceroic acid, lacceroic acid)), the fatty acid that more preferably carbon number is C10～C22, the fatty acid that particularly preferably carbon number is C10～C18, above-mentioned fatty acid can be that fatty acid mixed (being the unfixed multiple fatty acid of carbon number) can be also the fixing a kind of fatty acid of carbon number.The fusing point of these fatty glyceride must be not less than 25 ℃ of temperature, preferably is not less than 40 ℃, more preferably is not less than 60 ℃, preferably not higher than 150 ℃.Be preferred for the present invention and can be used for the example of fatty glyceride of the present invention as Capmul MCM C8 (40 ℃ of fusing points), Capmul MCM C10 (56～57 ℃ of melting ranges), two caprins, decanoin (mp, 31-32 ℃), glyceryl monolaurate, GLYCERYL DILAURATE, trilaurin (fusing point 45-47 ℃), single (meat) myristin (fusing point 68-70 ℃), glycerol three (meat) myristate (fusing point 56-57 ℃), two (meat) myristin (59 ℃ of fusing points), hexadecanoic acid direactive glyceride (fusing point 65-68 ℃), tripalmitin (fusing point 66-68 ℃), two tripalmitins (fusing point 72-74 ℃), glyceryl tristearate (fusing point 72-75 ℃), glyceryl monostearate (fusing point 58-59 ℃), distearin (72-74 ℃), glyceryl palmitostearate (52～55 ℃ of fusing points), single arachidic acid glyceride (84 ℃ of fusing points), triarachidin (72.2 ℃ of fusing points), diarachin (75 ℃ of fusing points), the behenic acid monoglyceride, behenic acid two glyceride, behenic acid triglyceride (mixing fat fusing point 69-74 ℃) and their mixture.Can be used for the commercial examples of fatty glyceride of the present invention as Gattefosse Co., CP (37～39 ℃ of fusing points), C, CM, CS2, CS2X, CT (38～40 ℃ of fusing points), D, DM, ND (42～45 ℃ of fusing points) in the Suppocire series that Ltd manufactures, E75, E76 (37～39 ℃ of fusing points), H185 (38～39 ℃ of fusing points), E85 (42～44 ℃ of fusing points) in the Witepsol series that Dynamic Nobel Chemicals Co.Ltd manufactures.

Wherein, it is more preferably C18～C22 of C16～C32(that above-mentioned fatty acid propylene glycol ester is preferably carbon number) or more senior (positive is saturated) fatty acid propylene glycol list or dibasic acid esters or their mixture, described fatty acid example is as stearic acid, arachidic acid, behenic acid, lignoceric acid (tetracosanoic acid, lignin acid), cerinic acid (hydroxyhexacosanoic acid), montanic acid (octocosoic acid), Cera Flava acid (triacontanoic acid), lacceroic acid (lacceroic acid, lacceroic acid).The available commercial examples of part is as propylene glycol monostearate (fusing point is more than or equal to 45 ℃), the two stearates (fusing point 37.0-42.0 ℃) of propylene glycol list.

Wherein, it is more preferably C18～C22 of C16～C32(that above-mentioned ethylene glycol fatty acid is preferably carbon number) or more senior (positive is saturated) fatty acid ethylene glycol list or dibasic acid esters or their mixture, described fatty acid example is as stearic acid, arachidic acid, behenic acid, lignoceric acid (tetracosanoic acid, lignin acid), cerinic acid (hydroxyhexacosanoic acid), montanic acid (octocosoic acid), Cera Flava acid (triacontanoic acid), lacceroic acid (lacceroic acid, lacceroic acid).The available commercial examples of part is as stearic acid ethylene glycol ester (57～63 ℃ of fusing points), stearic acid diethylene glycol dilaurate (fusing point 60-65 ℃), Ethylene Glycol Palmitostearate (54～60 ℃ of fusing points).

Wherein, it is more preferably C18～C22 of C16～C32(that above-mentioned fatty acid binaryglycol ester is preferably carbon number) or more senior (positive is saturated) fatty acid diethylene glycol list or dibasic acid esters and stearic acid Palmic acid binaryglycol ester or their mixture, described fatty acid example is as stearic acid, arachidic acid, behenic acid, lignoceric acid (tetracosanoic acid, lignin acid), cerinic acid (hydroxyhexacosanoic acid), montanic acid (octocosoic acid), Cera Flava acid (triacontanoic acid), lacceroic acid (lacceroic acid, lacceroic acid).The available commercial examples of part is as diethylene glycol monostearate (approximately 44 ℃ of fusing points), diethylene glycol distearate, stearic acid Palmic acid binaryglycol ester (43～50 ℃ of fusing points).

Wherein, it is more preferably C14～C24 of C12～C32(that above-mentioned fatty acid is preferably carbon number) or more senior (positive is saturated) fatty acid, most preferably being carbon number is (positive is saturated) fatty acid of C16～C22, example is as n-capric acid (mp, 27-32 ℃), lauric acid (mp, 44 ℃), (meat) myristic acid (tetradecylic acid), Palmic acid (hexadecylic acid), stearic acid, arachidic acid, behenic acid, lignoceric acid (tetracosanoic acid, lignin acid, mp84 ℃), cerinic acid (hydroxyhexacosanoic acid), montanic acid (octocosoic acid), Cera Flava acid (triacontanoic acid), lacceroic acid (lacceroic acid, lacceroic acid, mp95～96 ℃) or their mixture.The available commercial examples of part is as stearic acid (Chinese Pharmacopoeia record, fusing point is not less than 54 ℃), arachidic acid, behenic acid (80 ℃ of fusing points).

Wherein, it is more preferably C16～C24 of C14～C32(that above-mentioned fatty alcohol is preferably carbon number) or more senior (positive is saturated) fatty alcohol, most preferably being carbon number is (positive is saturated) fatty alcohol of C18～C22, example is as tetradecanol (Mp, 35-39 ℃ or 38-41 ℃ (sterling)), palmityl alcohol, stearyl alcohol, arachidic alcohol, behenyl alcohol, lignoceryl alcohol (tetracosanol, lignin alcohol), ceryl alcohol (hexacosyl alcohol), montanyl alcohol (octacosanol), melissyl alcohol (melissyl alcohol), laccerol (n-Dotriacontanol, lac wax) or their mixture.The available commercial examples of part is as cetyl alcohol (45～50 ℃ of fusing points), positive octadecanol cetyl alcohol mixture (48～56 ℃ of fusing points), positive octadecanol (55～60 ℃ of fusing points).

Wherein, above-mentioned fatty acid ester be preferably carbon number be C14～C36's or more senior (positive is saturated) fatty acid and carbon number be C14～C36's or the ester that forms of more senior (positive is saturated) fatty alcohol, carbon number is that C12's (positive is saturated) fatty acid and carbon number are C18～C36's or the ester that forms of more senior (positive is saturated) fatty alcohol, carbon number is C18's or the ester that forms of more senior (positive is saturated) fatty acid and carbon number (positive the is saturated) fatty alcohol that is C12 or their mixture, hydrogen on wherein said fatty acid or pure carbochain can be single or polyhydroxylated, wherein, carbon number is the ester that forms of (positive is saturated) fatty alcohol that C16～C36's (positive is saturated) fatty acid and carbon number are C16～C36 for more preferably.

Wherein, above-mentioned aliphatic hydrocarbon is preferably the microwax that comprises straight chain that carbon chain lengths is 31 to 70 carbon (preferably carbon chain lengths be 41 to 57 carbon) and random side chain saturated alkane, cycloalkane.

Wherein, (USPNF20 is described as Synthetic Spermacet mainly by saturated fatty alcohol (C as Synthetic Spermacet for the natural product that comprises above-mentioned composition and processed goods preferred embodiment thereof ₁₄～C ₁₈) and satisfied fatty acid (C ₁₄～C ₁₈) the mixture of ester, MP43～47 ℃), (fusing point: 44～52 ℃ is by a series of fatty acid (C to spermaceti ₁₂～C ₁₈) mixture that forms with the hexadecanol esterification, hexadecanol cetylate (C ₁₅h ₃₁cOOC ₁₆h33) be its main component, hexadecanol laurate wherein, the hexadecanol myristinate, hexadecanol cetylate and hexadecanol stearate at least formed the Ester total amount 85%), Brazil wax (cerinic acid, ceryl alcohol and ester thereof account for 80～58%, free ceryl alcohol 10～12%, the chemical formula of ester is CH3(CH2) nCOO(CH2) n+1CH3, n=22～32, 80～88 ℃ of fusing points), bayberry wax, (main component is cerinic acid ceryl alcohol fat to candelilla wax, 30% Arrcostab, 50% hydrocarbon compound and free alcohol, 66～69 ℃ of the fusing points such as free acid), (composition of Cera Flava 70～75% is to have even carbon chain for yellow beeswax or cera alba, the mixture of the monohydroxy straight-chain monohydric alcohol that length is 24 to 36 carbon and the formed various esters of straight-chain acid esterification.The contained even carbon atom of straight-chain acid can reach at most 36, and some of them are C ₁₈the hydroxy acid of position.Formed ester is mainly myricyl palmitate.Simultaneous also have free acid (approximately 14%) and hydrocarbon (approximately 12%), and approximately 1% free ceryl alcohol and the stearic alcohol ester of fatty acid.Fusing point: 61～65 ℃), montan wax (main component is the carbon number alkanol that is 22～32 and fat and the free monomer thereof of alkanoic acid, fusing point: 75～88 ℃), rice bran wax or the decolouring rice bran wax (ester mixture formed by higher fatty acids and high alcohol.Main component is myricyl cerotate and ceryl cerotate, and contain a small amount of other esters and minute quantity alcohols and hydro carbons, 80-82 ℃), (fusing point should be 81～85 ℃, and mainly, containing the esters of macromolecule, alcohols wherein is cerotin, 27 alcohol, Octacosanol, thirty alcohol for Chinese insect wax or Cera Chinensis; Acids wherein is cerin, 27 is sour, 28 is sour, thirty acid, and a small amount of Palmic acid, stearic acid.The rate that contains of the monacid ester mixture of aliphatic accounts for 93～95% of total amount, mainly contain carnaubic acid 28 ester, melissyl lignocerate, the carnaubic acid wax ester, ceryl cerotate, 27 acid 27 ester, ceryl montanate, melissic acid 27 ester, in addition, still containing free melissyl alcohol, it is myricyl alcohol 1%, resin 1～1.5%, heptacosane 2～3%, still containing 27 alcohol, ceryl alcohol etc.), shellac wax (main component resinate, mp74～82 ℃), sugarcane wax (70～84 ℃ of fusing points, the ester that main component is 16 carbon fatty acids and 30 carbon fatty alcohols or stigmasterol formation), (monoacid (put acid and account for 75% by palm fibre for Japan wax or Japanese fine wax, other is by stearic acid, the compositions such as oleic acid) glyceride approximately 90%, binary acid glyceride approximately 5～6%, free fatty 2～3%, free ceryl alcohol 1～2%.In japanic acid, major part is carbon number 20 to 22 acid.Fusing point: 48～55 ℃), Chinese haze tallow (16 acid glycerides 68～80%, olein 4～8%, 18 acid glyceride 5～7% fusing points: 48～55 ℃), castor oil hydrogenated (85～88 ℃ of fusing points), hydrogenated vegetable oil (57～85 ℃ of fusing points), and their mixture.

Sterin and steroid derivatives also can be for the above-mentioned excipient of the present invention, but the example that its commercialization obtains comprises: cholesterol, sitosterol, lanosterol, their fatty acid ester, as cholesterol fatty acid ester, (example is as cholesterol ester stearic acid (82.5 ℃ of fusing points), cholesterol myristinate (70～71 ℃ of fusing points), cholesterol acid ester (44～47 ℃ of fusing points), cholesterol cetylate (90.5 ℃ of fusing points)), the ether of their PEG2～100, as PEG-24 cholesterol ethers (Solulan C-24, Amerchol), PEG-30 Dihydrocholesterol (Phytosterol GENEROL series, Henkel), PEG-25 plant sterol (Nikkol BPSH-25, Nikko), PEG-5 soyasterol (Nikkol BPS-5, Nikko), PEG-10 soyasterol (Nikkol BPS-10, Nikko), PEG-20 soyasterol (Nikkol BPS-20, Nikko), with PEG-30 soyasterol (Nikkol BPS-30, Nikko), the sterin of above-mentioned one or more and steroid derivatives.

Other available (fusible) lipid (medicinal) additives also include but not limited to terpene resin (82～120 ℃ of fusing points), P-hydroxybenzoic acid (C1～C22 alkyl) ester, gallic acid (C1～C22 alkyl) ester, gallic acid (C1～C22 alkyl) ester, ascorbic acid (C1～C22 alkyl) ester, arabo-ascorbic acid (C1～C22 alkyl) ester, (example is as propyl p-hydroxybenzoate (95～98 ℃ of fusing points) for benzyl p-hydroxybenzoate (120 ℃ of fusing points), dodecyl gallate (96～97.5 ℃ of fusing points), gallateoctylester (99～102 ℃ of fusing points), ascorbyl palmitate (107～117 ℃ of fusing points), ascorbyl stearate (approximately 116 ℃ of fusing points)), and their mixture.

Fusing point for lipid of the present invention (medicinal) additive when particularly preferably those contacts with body fluid during not higher than the contacting with body fluid in body cavity in other words of 37 ℃ of temperature with regard to the lipidic matrix of energy liquefaction, emulsifying or thawing.These lipidic matrix comprise fatty glyceride that for example carbon number is C8～C10, the fat-soluble surfactant of some self emulsifyings (as the anhydrous sorbitol tristearate) but and the lipidic matrix of the self emulsifying that contains a certain amount of surfactant (as self-emulsifying monostearate, cetomacrogol emulsifying wax, emulsifing wax).This be because tablet just can liquefaction while contact with body fluid in body cavity, emulsifying or thawing will cause the fast rapid release of medicine.

Wherein, stearic acid, castor oil hydrogenated are for particularly preferably, because their quality are comparatively hard, be conducive to improve the tablet mechanical performance, castor oil hydrogenated is for particularly preferably, because it also has higher fusing point, the mechanical performance that is conducive to improve or improve tablet is weatherability particularly.In addition, preferred performance enhancers also includes but not limited to that fusing point is not less than 43 ℃ fat-soluble and is insoluble in lactic acid fatty acid propylene glycol ester, lactic acid fatty glyceride, the fatty acid lactoyl ester of water, and their mixture, especially preferred is 70% above-mentioned substance of the material of above-mentioned hard, the particularly hardness hardness that is not less than castor oil hydrogenated.

Above-mentioned (fusible) lipid (medicinal) additive comprises (naturally comprising the above-mentioned example of respectively enumerating) (arbitrarily) compositions or the mixture between them, the solid dispersion or the homogeneous phase solid solution that particularly between their (naturally comprising the above-mentioned example of respectively enumerating), form, and their compositions or mixture, also can be used for the present invention.

Three), form solid dispersion (/ or body) or homogeneous phase solid solution and (arbitrarily) compositions or mixture thereof between above-mentioned surfactant (comprising their above-mentioned each examples of enumerating) and above-mentioned (fusible) lipid (medicinal) additive (comprising their above-mentioned each examples of enumerating) and also can be used for the present invention, as fusible binding agent and/or performance enhancers.

Four), (fusible) saccharide

Saccharide not only can be made diluent (B1, B2) in the present invention, also can make above-mentioned performance enhancers (E-3, as saccharide E3) and/or above-mentioned fusible binding agent (D-3) (being above-mentioned fusible saccharide D3).

Above-mentioned fusible binding agent (D-3) (being above-mentioned fusible saccharide D3) for or be selected from the relatively low saccharide of at least one fusing point (following record for " saccharide III "), so long as pharmaceutically allowed, (diluent (B) is while being selected from saccharide for the diluent used with the present invention (B), (following) recorded and narrated as " saccharide I ")) and above-mentioned performance enhancers (E-3) saccharide (following record is " saccharide II ") is (preferably, also with medicine (A)) compare the relative low and melting of fusing point and solidify, maintain the saccharide of figure of tablet, be not particularly limited, satisfied is the approximately saccharide of 80～approximately 180 ℃ of fusing point, more satisfied the is about saccharide of 80～150 ℃, this saccharide includes but not limited to listed saccharide in above-mentioned diluent (B).Some preferred embodiments are if any glucose (83 ℃ of monohydrate, fusing points), xylitol (93 ℃ of fusing points), trehalose (97 ℃ of dihydrate, fusing points), Sorbitol (hydrate, fusing point 100 ℃ less than), maltose (102 ℃ of fusing points), Sorbitol (110 ℃ of fusing points), red moss (sugar) alcohol (122 ℃ of fusing points), glucose (146 ℃ of fusing points), maltose alcohol (150 ℃ of fusing points), mannitol (166 ℃ of fusing points), sucrose (approximately 170 ℃ of fusing points) etc.As such saccharide, be selected one or more saccharides in glucose, xylitol, trehalose, Sorbitol, maltose, erithritol, maltose alcohol and hydrate thereof.Because saccharide itself is difficult to moisture absorption, optimal is easy to handle trehalose, maltose, erithritol or maltose alcohol, especially trehalose and/or erithritol.Saccharide of the present invention, consider the chemical characteristic of applicable medicine, and the stability of medicine to temperature, can carry out suitable selection.And, but such saccharide one or more be used in combination.In addition, these saccharides also can be done the hydrate use.When without hydrate being the different saccharide of fusing point, can correspondingly set suitable heating-up temperature at hydrate.

(corresponding with above-mentioned fusible binding agent (D-3)) above-mentioned performance enhancers (E-3) is selected from that at least one is higher than the fusing point of above-mentioned fusible binding agent (D-3) " saccharide III ", more above-mentioned diluent (B) (as " the saccharide I) fusing point low (preferably, also than the present invention, the fusing point of medicine (A) used is low) " saccharide II ", this saccharide includes but not limited to listed saccharide in above-mentioned diluent (B), comprise above-mentioned polysaccharide, its microfibre particularly, as micron order cellulose or microcrystalline Cellulose, particularly nanoscale dermatosome or microcrystalline Cellulose.This paper term as used herein " microfibre " refers to the granular materials that can (usually) be described as fiber due to their length-width ratio, for the length-width ratio of the preferred microfibre of this paper, is the about 500:1 of about 10:1-, more preferably from about 25:1-300:1.The mean diameter of above-mentioned " microfibre " (diameter) (usually) is not more than 1 μ m (approximately 10000 orders, taylor criteria), preferably is not more than 100nm.In order to reduce process costs, the mean diameter of above-mentioned " microfibre " (diameter) preferably is not less than 10nm, more preferably is not less than 1nm.The average length of above-mentioned " microfibre " (usually) is not more than 100 μ m (about 155 orders, taylor criteria), preferably be not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (approximately 2000 orders, taylor criteria), more more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), be not more than best 100nm.Some preferred embodiments are if any xylitol (93 ℃ of fusing points), trehalose (97 ℃ of dihydrate, fusing points), Sorbitol (hydrate, fusing point 100 ℃ less than), maltose (102 ℃ of fusing points), Sorbitol (110 ℃ of fusing points), erithritol (122 ℃ of fusing points), glucose (146 ℃ of fusing points), maltose alcohol (150 ℃ of fusing points), mannitol (166 ℃ of fusing points), sucrose (approximately 170 ℃ of fusing points) etc.As such saccharide, be to select one or more saccharides in xylitol, trehalose, Sorbitol hydrate, maltose, Sorbitol, erythritol, glucose, maltose alcohol, mannitol, sucrose and hydrate thereof.

Saccharide can be made above-mentioned performance enhancers (E-3) in the present invention, while making again above-mentioned fusible binding agent (D-3), above-mentioned diluent (B) can be selected from saccharide, below record and narrate as " saccharide I ", should " saccharide I " be selected from than the fusing point of above-mentioned fusible binding agent (D-3) " saccharide III " and performance enhancers (E-3) " saccharide II " high (preferably, also than the present invention, the fusing point of medicine (A) used is low) " saccharide I ", this saccharide includes but not limited to listed saccharide in above-mentioned diluent (B).Some preferred embodiments are if any trehalose (97 ℃ of dihydrate, fusing points), Sorbitol (hydrate, fusing point 100 ℃ less than), maltose (102 ℃ of fusing points), Sorbitol (110 ℃ of fusing points), erithritol (122 ℃ of fusing points), glucose (146 ℃ of fusing points), maltose alcohol (150 ℃ of fusing points), mannitol (166 ℃ of fusing points), sucrose (approximately 170 ℃ of fusing points), lactose (202 ℃ of fusing points) etc.As such saccharide, be to select one or more saccharides in trehalose, Sorbitol hydrate, maltose, Sorbitol, erythritol, glucose, maltose alcohol, mannitol, sucrose, lactose and hydrate thereof.

As with some preferred embodiment to above-mentioned " saccharide III ", " saccharide II " reaches " saccharide I " and explains, for example as the present invention, fusible binding agent (D-3) " saccharide III " used is used glucose (monohydrate, 83 ℃ of fusing points) time, as above-mentioned performance enhancers (E-3) " saccharide II ", can use xylitol, trehalose, Sorbitol, erithritol, glucose, maltose alcohol, mannitol, sucrose, or its hydrate, above-mentioned diluent (B) " saccharide I " is selected from trehalose, the Sorbitol hydrate, maltose, Sorbitol, erythritol, glucose, maltose alcohol, mannitol, sucrose, lactose, and hydrate.And, the fusible binding agent (D-3) " saccharide III " used as the present invention used xylitol (93 ℃ of fusing points), trehalose (dihydrate, 97 ℃) time, can use Sorbitol, erythritol, glucose, maltose alcohol, mannitol, sucrose or its hydrate as above-mentioned performance enhancers (E-3) " saccharide II ", above-mentioned diluent (B) " saccharide I " is selected from erythritol, glucose, maltose alcohol, mannitol, sucrose, lactose and hydrate thereof.In addition, as the present invention, fusible binding agent (D-3) " saccharide III " used is used erithritol (fusing point 122 ℃ time), can use glucose, maltose alcohol, mannitol, sucrose as above-mentioned performance enhancers (E-3) " saccharide II ", above-mentioned diluent (B) " saccharide I " is selected from maltose alcohol, mannitol, sucrose, lactose and hydrate thereof.Have again, used as the present invention " when fusible binding agent (D-3) " saccharide III " is used maltose alcohol (150 ℃ of fusing points); can use mannitol, sucrose or lactose as above-mentioned performance enhancers (E-3) " saccharide II ", above-mentioned diluent (B) " saccharide I " is selected from sucrose, lactose and hydrate thereof.As illustration, above-mentioned performance enhancers (E-3) " saccharide II " and above-mentioned diluent (B) " saccharide I " suitably determine according to used saccharide kind.When selecting the poor large saccharide of fusing point, above-mentioned performance enhancers (E-3) " saccharide II ", above-mentioned diluent (B) " saccharide I " particularly, satisfied is to select one or more saccharides from glucose, maltose alcohol, mannitol, sucrose and lactose, and more satisfied is maltose alcohol, sucrose and lactose.The one kind or two or more mixing of these saccharides, suitably used in right amount.Temperature difference hour at above-mentioned diluent (B) " saccharide I " fusing point, in tablet the present invention's fusible binding agent (D-3) " saccharide III " used and above-mentioned performance enhancers (E-3) " saccharide II " together with its melting and solidification, because saccharide contained in tablet forms between granule crosslinked, tablet strength increase to surpass essential value, also may appear in oral cavity the problem of disintegrate rapidly.Therefore, select the larger saccharide of temperature difference of fusing point, be applicable on the disintegrative tablet rapidly in manufacturing oral cavity.Poor as fusing point, satisfied is more than 10 ℃, more satisfied is more than 20 ℃.

Saccharide is in the present invention's (doing corresponding with above-mentioned fusible binding agent (D-1)) above-mentioned performance enhancers (E-3), and this saccharide (E-3) includes but not limited to listed saccharide in above-mentioned diluent (B).Some preferred embodiments are if any glucose (83 ℃ of monohydrate, fusing points), xylitol (93 ℃ of fusing points), trehalose (97 ℃ of dihydrate, fusing points), Sorbitol (hydrate, fusing point 100 ℃ less than), maltose (102 ℃ of fusing points), Sorbitol (110 ℃ of fusing points), red moss (sugar) alcohol (122 ℃ of fusing points), glucose (146 ℃ of fusing points), maltose alcohol (150 ℃ of fusing points), mannitol (166 ℃ of fusing points), sucrose (approximately 170 ℃ of fusing points), lactose (202 ℃ of fusing points) etc.As such saccharide, be selected one or more saccharides in glucose, xylitol, trehalose, Sorbitol, maltose, erithritol, maltose alcohol and hydrate thereof.Because saccharide itself is difficult to moisture absorption, optimal is easy to handle trehalose, maltose, erithritol or maltose alcohol, especially trehalose and/or erithritol.Saccharide of the present invention, consider the chemical characteristic of applicable medicine, and the stability of medicine to temperature, can carry out suitable selection.And, but such saccharide one or more be used in combination.In addition, these saccharides also can be done the hydrate use.When without hydrate being the different saccharide of fusing point, can correspondingly set suitable heating-up temperature at hydrate.

The system of selection of above-mentioned fusible binding agent (D-3) and/or above-mentioned saccharide performance enhancers (E-3) or fusing point matching process may extend to the match selection of other above-mentioned fusible binding agents (D) and/or above-mentioned saccharide performance enhancers (E), as select fusible medicinal surfactant additive to join another dystectic medicinal surfactant additive, fusible medicinal surfactant additive makes up a prescription and uses the lipid additive, medicinal carbohydrate additive, medicinal cyclodextrin additive, the amino acids additive, edible peptide class additive, the medicinal salts additive, medicinal bases additive, any one in medicinal acids additive or their combination in any, fusible medicinal lipid additive makes up a prescription and uses surfactant additive, and fusible medicinal carbohydrate additive is made up a prescription and is used the cyclodextrin additive, the amino acids additive, edible peptide class additive, the medicinal salts additive, medicinal bases additive, any one in medicinal acids additive or their combination in any all can be carried out in accordance with the law.

Above-mentioned fusible binding agent (D-3) and/or above-mentioned saccharide performance enhancers (E-3) be " sugar that mouldability is large " particularly preferably, they not only are conducive to improve the tablet mechanical performance, and be particularly conducive to and improve its technique ease for operation, weaken or eliminate former correlation technique (referring to U.S. Pat 5, 576, 014) defect, as former technology need be carried out the processing such as crystal conversion to " sugar that mouldability is large " in tablet under high humidity or under high humidity high temperature, these processing may cause adverse effect to the stability of active component in tablet, " sugar that mouldability is large " is coated on and better does on " sugar that mouldability is little " of diluent because of solubility property for another example, this diluent is dissolved and cause adverse effect, thereby tablet is dissolved in water or dispersive property decline, " sugar that mouldability is large " is coated on a large amount of " sugar that mouldability is little " in addition, treating capacity is large, operating time is long, process costs is high, and the present invention only processes the adhesion agent (C) that comprises above-mentioned fusible binding agent (D-3) and/or above-mentioned saccharide performance enhancers (E-3) in a small amount, workload is little, operating time is short, process costs is low.Refer to that at this bright term used herein " sugar that mouldability is large " (referring to U.S. Pat 5,576,014) working as its 150mg is used the drift of diameter 8mm with 10～50kg/cm ²pressure while making tablet, generally show the sugar of 2kg or the above hardness of 2kg.The example of this sugar comprises Sorbitol, maltose, maltose alcohol, other oligosaccharides etc., wherein, take maltose and maltose alcohol as good.The oligosaccharide that above-mentioned oligosaccharide preferably is comprised of 2～6 monosaccharide residues, to type and the not restriction of combination of the monosaccharide residue that forms oligosaccharide.The illustrative example of oligosaccharide comprises lactosucrose (lactosucrose) powder (for example Nyuka Oligo LS-55P (ProductName, the former Itochu of woods produces)).These sugar can be used alone or two or more is mixed and uses.

Corresponding with " sugar that mouldability is large " is " sugar that mouldability is little " (referring to U.S. Pat 5,576,014).The term " sugar that mouldability is little " used in this article refers to that working as its 150mg is used the drift of diameter 8mm with 10～50kg/cm ²pressure while making tablet, generally show the sugar of 0～2kg hardness.The example of this sugar comprises lactose, mannitol, glucose, sucrose, xylitol etc., wherein, take lactose and mannitol as good.These sugar can be used alone or two or more mixing is made as diluent.Use this class diluent to be conducive to improve the water solublity of tablet or the dissolubility in oral cavity.

Saccharide is made above-mentioned performance enhancers (E-3) in the present invention, to fusible binding agent (D-1) involved in the present invention and/or fusible binding agent (D-3) role is identical with above-mentioned performance enhancers (E1) or class is near effect, can improve or improve mechanical performance and/or weatherability and/or the hydrophilic of fusible binding agent (D-1) and/or fusible binding agent (D-3), thereby improve mechanical performance and/or weatherability and/or the hydrophilic of tablet of the present invention, also can reduce above-mentioned fusible binding agent (D-1) is the consumption of surfactant, lower its toxic and side effects, improve the application security of tablet.

Five), medicinal (micro-) (non-saccharide) performance enhancers (E-4) granule and (micro-) active component or drug particles (A) are (E-5)

Medicinal (micro-) (non-saccharide) performance enhancers (E-4) and (micro-) active component or drug particles (A) (E-5) also can strengthen or improve tablet mechanical performance or weatherability or safety in utilization.Can be used for medicinal (micro-) of the present invention (non-saccharide) performance enhancers (E-4) is mainly medicinal (micro-) (non-saccharide) solid additive (E-4), it includes but not limited to: medicinal (preferred water dissolubility or hydrophilic tasteless) inorganic salts or organic salt additive, pharmaceutically acceptable room temperature (25 ℃ of temperature) is lower is (preferred water dissolubility or hydrophilic) organic base of solid/or inorganic base additive, pharmaceutically acceptable room temperature (25 ℃ of temperature) is lower is (preferred water dissolubility or hydrophilic) organic acid of solid/or inorganic acids additive, (preferred water dissolubility or hydrophilic) pharmaceutically acceptable cyclodextrin additive, (preferred water dissolubility or hydrophilic tasteless or be sweet or delicate flavour) aminoacid, (preferred water dissolubility or hydrophilic tasteless or be sweet or delicate flavour) edible peptide, and their mixture, mentioned component and instantiation have been introduced in the part of diluent (B) above mostly, at this, do not repeat.

Below to not being described in (non-saccharide) performance enhancers (E-4) that above diluent (B) part illustrates.

Can be used under pharmaceutically acceptable room temperature of the present invention (25 ℃ of temperature) for the preferred embodiment of medicinal organic bases additive of solid as, but be not limited to this: basic amino acid, medicinal basic peptide, derivant after medicinal osamine (preferably (single or two) amido monosaccharide and amido (one or two) first or ethylization or second or formylated and by the derivative amido oligosaccharide formed of above-mentioned amido monosaccharide (pair to nine sugar) and basic salt or basic salt, as deoxystreptamine, desosamine (as the 2-desosamine), deoxy-glucose amine (as 6-deoxidation-GLUCOSAMINE), fucosamine, galactosamine (as D-galactosamine), glucamine, glucosamine, N-first (or second) base-GLUCOSAMINE (Portugal's first (or second) amine), neamine (double focusing osamine), trehalosamine (disaccharidase amine), streptobiosamine, 4-O-(2-Amino-2-deoxy-.beta.-D-glucosyl)-D-glucosamine., oligochitosan), with their mixture.

The preferred embodiment of the lower medicinal inorganic base additive for solid of pharmaceutically acceptable room temperature (25 ℃ of temperature) as, but be not limited to this: medicinal metal oxide (magnesium oxide for example, calcium oxide, ferrum oxide, ferrous oxide, zinc oxide, aluminium oxide), medicinal hydroxide is (as sodium hydroxide, potassium hydroxide, aluminium hydroxide, magnesium hydroxide, calcium hydroxide, hydrated ferric oxide., ferrous hydroxide, zinc hydroxide, gold hydroxide, aluminium hydroxide), medicinal inorganic alkaline salt is (as carbonic acid (just) salt, alkaline carbonic acid (just) salt, bicarbonate, glycine carbonate, the carbonate of lysine, arginic carbonate, amino acid whose carbonate, carbonate containing glycosyl, medicinal percarbonate, medicinal sulfurous acid (just) salt, medicinal thiosulfuric acid (just) salt, medicinal phosphoric acid (just) salt, medicinal hydrophosphate, as its sodium salt, potassium salt, calcium salt, magnesium salt, zinc salt, preferred above-mentioned carbonate wherein, bicarbonate, glycine carbonate, the carbonate of 1B, arginic carbonate, amino acid whose carbonate, containing the carbonate of glycosyl, hydrophosphate, sulphite, percarbonate, as sodium salt, potassium salt, ammonium salt, and their mixture, wherein, medicinal charcoal hydrochlorate or bicarbonate and organic base are preferred.

Can be used under pharmaceutically acceptable room temperature of the present invention (25 ℃ of temperature) for the preferred embodiment of the pharmaceutically acceptable organic acid class additive of solid as, but be not limited to this: along or coelonychia base butene dioic acid, dihydroxy along or fumaric acid, maleic acid (maleic acid), fumaric acid (fumaric acid, Fumaric acid), galactosaccharic acid, glucosaccharic acid, itaconic acid (enedioic acid class), malic acid, oxalic acid, malonic acid, succinic acid (succinic acid), citric acid, tartaric acid, citramalic acid, dihydroxytartaric acid, gluconic acid, glycolic, ethylene lactic acid is (as D-ALPHA-Hydroxypropionic acid, Pfansteihl), hydroxybutyric acid, the hydroxyl valeric acid, hydroxycaproic acid, dihydrochalcone, galacturonic acid, glucuronic acid, ascorbic acid, dehydroascorbic acid, deoxidation-L-AA, glucoascorbic acid, arabo-ascorbic acid, carboxyglutamic acid, single ethyl tartaric acid, glucoheptonic acid, glycolic, taurine, glycyrrhizic acid, hydroxyglutamic acid, lactobionic acid, sorbic acid, edetic acid, pentaacetic acid, clavulanic acid, ribonucleotide, Deoxydization nucleotide, inosinic acid, Alpha-Methyl furan inosinic acid, adenylic acid, guanyl, cytidylic acid, uridylic acid, thymidylic acid, inosine monophosphate, IMP (inosinic acid), xanthylic acid, phosphorylated amino acid is (as phosphotyrosine, phosphoserine and phosphothreonine) and acidic amino acid (as glutamic acid, and the acid salt of above-mentioned multicomponent organic acid or ackd salt aspartic acid).Wherein, tartaric acid, citric acid, maleic acid, fumaric acid, malic acid, succinic acid, taurine, 'alpha '-hydroxy acids, ascorbic acid and acidic amino acid (as glutamic acid, aspartic acid), acidity peptide, and their mixture.

Can be used under pharmaceutically acceptable room temperature of the present invention (25 ℃ of temperature) for the preferred embodiment of the medicinal inorganic acids additive of solid as, but be not limited to this: the medicinal metal oxide, zinc oxide for example, aluminium oxide, and medicinal mineral acid salt, for example, as medicinal strong acid (hydrochloric acid, sulphuric acid, nitric acid, phosphoric acid etc.) zinc salt, iron salt, ferrous salt, calcium salt, magnesium salt, (example is as iron chloride or ferrous iron or aluminum for aluminum salt etc., ferric nitrate or ferrous iron or aluminum, iron sulfate or ferrous iron or zinc or aluminum or aluminum potassium or aluminum sodium), medicinal disulfate, medicinal bisulfites, medicinal dihydric phosphate, medicinal pyrosulfate, medicinal pyrosulfurous acid, as sodium salt, potassium salt, and medicinal solid (under 25 ℃ of room temperatures) mineral acid, phosphoric acid for example.

Can be used for also comprising for the alkali of solid (or acid) under pharmaceutically acceptable room temperature of the present invention (25 ℃ of temperature) the medicinal organic polymer of alkalescence mentioned above (or acid).

The preferred embodiment that can be used for medicinal (preferred water dissolubility or hydrophilic tasteless) additive salt of the present invention and medicinal (inorganic) oxide addition includes but not limited to above-mentioned medicinal inorganic alkaline salt, above-mentioned medicinal mineral acid salt, the salt of above-mentioned medicinal basic or acid, medicinal inorganic acid highly basic (neutrality) salt (example hydrochloric acid, sulphuric acid, nitric acid, the potassium of phosphoric acid etc., sodium salt, preferably sulfuric acid salt, phosphate), the medicinal metal oxide, medicinal carbon element compound, medicinal silicon-containing compound is (as Si oxide, silicate) and composition thereof, available more preferably example includes but not limited to attapulgite, the soap clay, calcium carbonate, calcium sulfate, barium sulfate, white carbon black, silicon dioxide, aluminium oxide, zinc oxide, titanium dioxide, kaolin, Muscovitum, Talcum, calcium phosphate, magnesium carbonate, magnesium oxide, magnesium silicate, magnesium trisilicate and composition thereof.

Any mixture of above-mentioned additive and the example also can be used for the present invention.

Above-mentioned additive (E-1～4) granule and (micro-) active component or drug particles (A) mean diameter (diameter) (usually) (E-5) are not more than 100 μ m (about 155 orders, taylor criteria), preferably be not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), be not more than best 100nm, be not less than best 10nm, particularly be not less than 1nm.The less particle of particle diameter can be conducive to improve tablet strength and/or the performances such as weatherability and/or hydrophilic and/or drug-eluting as nano level particle (being not more than 100nm), and the smaller the better.

Above-mentioned non-carbohydrate additive (E-4) and polysaccharide additive also can be used its microfibre to form and make performance enhancers (E), micro-polymer class additive described above.This paper term as used herein " microfibre " refers to the granular materials that can (usually) be described as fiber due to their length-width ratio, for the length-width ratio of the preferred microfibre of this paper, is the about 500:1 of about 10:1-, more preferably from about 25:1-300:1.The mean diameter of above-mentioned " microfibre " (diameter) (usually) is not more than 1 μ m (approximately 10000 orders, taylor criteria), preferably is not more than 100nm.In order to reduce process costs, the mean diameter of above-mentioned " microfibre " (diameter) preferably is not less than 10nm, more preferably is not less than 1nm.The average length of above-mentioned " microfibre " (usually) is not more than 100 μ m (about 155 orders, taylor criteria), preferably be not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (approximately 2000 orders, taylor criteria), more more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), be not more than best 100nm.

In the present invention, above-mentioned fusible binding agent (D) is coated on upper solid coating particle or above-mentioned hot-melt adhesive (D) and the above-mentioned performance enhancers (E) of forming of above-mentioned performance enhancers (E) and forms solid dispersion (/ or body) particle, thereby forms " shell-core structure ".In above-mentioned " shell-core structure ", " shell " can coat " core " wholly or in part; Can contain one or more (identical or different kind) " core " in " shell "; Can also contain less " core " in " shell "; Shell " in " core " in also can comprise the component of " shell " or less " shell-core structure "; It can also be the particle of more complicated shell/shell/three layers of cores, shell/core/three layers, shell, shell/core/mode such as four layers of shell/cores.In above-mentioned " shell-core structure ", " shell " preferably accounts for 0.5～50% of total volume, and more preferably 1～30%, best 2～10%.

The present invention's above-mentioned " shell-core structure " particle used using certain shape and the size particle be stored in tablet as performance improving agent.About its shape, they can have any applicable shape, the method preparation that the particle of various shapes can be known by particle manufacturing technology field.The example of the shape of particle that it is applicable includes but not limited to: the ellipsoid particle, certain kind of berries shape particle, multi-petal shape particle, dumb-bell shape grain that spherical, draw ratio is greater than 1:1 is in, aggregated particle, bivalve shape particle, square, rhombus, taper, avette, random shape and hollow ball particle etc.Above-mentioned fusible binding agent (D) or above-mentioned fusible binding agent (D) and above-mentioned performance enhancers (E) are at heating and melting again after cooling curing, and above-mentioned shape of particle can change further, as from above-mentioned regular shape, become random shape.About its size, (usually) its mean diameter (diameter) is not more than 100 μ m (approximately 155 orders, taylor criteria).Preferably, its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (approximately 2000 orders, taylor criteria), more more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more more preferably be not more than 100nm, be not more than best 10nm, particularly be not less than 1nm.Usually, less particle is conducive to improve the tablet tablet properties, as improved tablet strength.

" solid dispersion (/ or body) " that the present invention uses while with above-mentioned performance enhancers (E), forming solid dispersion (/ or body) (be above-mentioned hot-melt adhesive (D)), usually there is relatively strict " discontinuous phase " (or title " is dispersed mutually or the dispersate phase ") and " continuous phase " (or title " dispersant phase "), and the two all can contact with other solid phases (or " third phase "), do not have strict " foreign minister " and " interior phase " minute, " discontinuous phase " is generally performance enhancers (E), " continuous phase " is generally fusible binding agent (D), " discontinuous phase " wherein or dispersed average particle size are not more than 100 μ m (about 155 orders, taylor criteria), preferably be not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, more preferably be not more than 10nm, be not more than best 1nm.

" solid coating " (being that above-mentioned fusible binding agent (D) is coated on above-mentioned performance enhancers (E)) that the present invention uses, usually have relatively strict " foreign minister " and " interior phase " minute, usually only have " foreign minister " to contact with other solid phases (or " third phase "), " foreign minister " be " continuous phase " normally, " interior phase " can be that " discontinuous phase " (a plurality of core core) can be also " continuous phase " (single core core), " the solid coating " that " interior phase " is generally performance enhancers (E) or comprises performance enhancers (E) and/or " solid dispersion (/ or body) ", corresponding is that " foreign minister " is generally fusible binding agent (D) with it, but wherein can contain " performance enhancers (E) " or other compositions, " interior phase " particle wherein or core core mean diameter (usually) are not more than 100 μ m (about 155 orders, taylor criteria) or be 100 μ m to 10nm(or 1nm) (containing two-end-point), preferably be not more than 25 μ m (about 500 orders, taylor criteria) or be 25 μ m to 10nm(or 1nm) (containing two-end-point), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria) or be 5 μ m to 10nm(or 1nm) (containing two-end-point), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria) or be 1 μ m to 10nm(or 1nm) (containing two-end-point), more preferably be not more than 100nm or for 100nm to 10nm(or 1nm) (containing two-end-point), be not more than best 10nm or for 10nm to 1nm(containing two-end-point).

From being not difficult to find out, the present invention's use " solid dispersion (/ or body) " do not have substantial difference with " solid coating ", the two is unified, and can mutually transform, while not coating fully as " solid coating " its core core, can regard " solid dispersion " as, and " continuous phase " melted by heat of " solid dispersion (/ or body) " is coated on its all " discontinuous phase " fully when interior and can regards " solid coating " as, when " foreign minister " melted by heat of " solid coating " exposes its part core core, can regard " solid dispersion " as again.

Above-mentioned hot-melt adhesive (D) and above-mentioned performance enhancers (E) form solid sols or solid solution (or homogeneous phase solid solution), and (its " discontinuous phase " average particle size is not more than 100 or 10nm, be " solid dispersion " that people usually say) time, can see the special case of " solid dispersion (/ or body) " of its formation as, (its " discontinuous phase " average particle size is not more than 100 or 10nm for above-mentioned solid sols or solid solution (or homogeneous phase solid solution), in the time of " solid dispersion " it has often been said), can see " the solid coating " of its formation as, can see again " solid dispersion (/ or body) " of its formation as, (the solid sols that part embodiment is obtained by spray drying method or solid solution (or homogeneous phase solid solution) powder during powder that particularly it is obtained by spray drying method, only be designated as in the text " powder ", they are " solid coating ", be again " solid dispersion (/ or body) ", at this, be specifically noted), the two more is difficult to distinguish.

The ratio that the consumption (usually) of above-mentioned fusible adhesion agent (C1) accounts for whole tablet total weight amount is 0.5%(wt./wt.) to 90%(wt./wt.), be preferably 1%(wt./wt.) to 70%(wt./wt.), be more preferably 5%(wt./wt.) to 50%(wt./wt.), be 8%(wt./wt. best) to 30%(wt./wt.), above percentage by weight is based on the gross weight of tablet.

The ratio that the consumption (usually) of above-mentioned fusible adhesion agent (C2) accounts for whole tablet total weight amount is 0.5%(wt./wt.) to 99%(wt./wt.), be preferably 1%(wt./wt.) to 95%(wt./wt.), be more preferably 5%(wt./wt.) to 90%(wt./wt.), be 8%(wt./wt. best) to 70%(wt./wt.), above percentage by weight is based on the gross weight of tablet.

At above-mentioned fusible adhesion agent (C1-1, C1-2 and C1-5) or solid dispersion (I, II, V) in, above-mentioned performance enhancers (E: i.e. medical additive E1 wherein, surfactant E2, medical additive E2, surfactant E23, saccharide E3 etc.) ratio that accounts for whole above-mentioned fusible adhesion agent can be arbitrarily, but normally be positioned at 0.005 to 0.995(weight ratio), preferably be positioned at 0.05 to 0.95(weight ratio) between (containing end points), more preferably be positioned at 0.15 to 0.85(weight ratio) between (containing end points), more more preferably be positioned at 0.25 to 0.75(weight ratio) between (containing end points), be positioned at best 0.35 to 0.65(weight ratio), correspondingly, the ratio that above-mentioned hot-melt adhesive (D: i.e. surfactant D 1, medicinal lipid additive D2, fusible saccharide D3 etc. wherein) accounts for whole above-mentioned fusible adhesion agent normally is positioned at 0.005 to 0.995(weight ratio), preferably be positioned at 0.05 to 0.95(weight ratio) between (containing end points), more preferably be positioned at 0.15 to 0.85(weight ratio) between (containing end points), more more preferably be positioned at 0.25 to 0.75(weight ratio) between (containing end points), be positioned at best 0.35 to 0.65(weight ratio).When tablet of the present invention has been supposed to better machine performance, aforementioned proportion is positioned at 0.3 to 0.7(weight ratio).In above-mentioned fusible adhesion agent (C1-1～C1-2), when tablet of the present invention has been supposed to better hydrophilic (or in water dispersibility) (preferably, and (D) is hydrophilic for above-mentioned hot-melt adhesive) time, the ratio that above-mentioned performance enhancers (E) accounts for whole above-mentioned fusible adhesion agent is positioned at 0.005 to 0.50(weight ratio) (preferably 0.05 to 0.45(weight ratio)); When tablet of the present invention has been supposed to better weatherability (preferably, and (D) is hydrophilic for above-mentioned hot-melt adhesive) time, the ratio that above-mentioned performance enhancers (E) accounts for whole above-mentioned fusible adhesion agent is positioned at 0.50 to 0.995(weight ratio), 0.50 to 0.95(weight ratio preferably).In above-mentioned fusible adhesion agent (C1-1～C1-2 and C1-5), when above-mentioned hot-melt adhesive (D) or above-mentioned performance enhancers (E) are selected from (listed) multi-component combination, between these components, amount ratio can be arbitrarily.

At above-mentioned fusible adhesion agent (C1-3, 4) or solid dispersion (III, IV) in, the ratio that above-mentioned performance enhancers (E: i.e. dissolving in or being scattered in water or hydrophilic surfactant E21 wherein) accounts for whole above-mentioned fusible adhesion agent is usually located at 0.005 to 0.50(weight ratio), 0.005 to 0.25(weight ratio preferably), more preferably be positioned at 0.01 to 0.20(weight ratio) between (containing end points), more preferably be positioned at 0.02 to 0.15(weight ratio) between (containing end points), be positioned at best 0.03 to 0.10(weight ratio) between (containing end points), correspondingly, the ratio that above-mentioned hot-melt adhesive (D: i.e. fusible lipophilic surfactant D11 and/or medicinal lipid additive D21 wherein) accounts for whole above-mentioned fusible adhesion agent normally is positioned at 0.50 to 0.995(weight ratio), 0.75 to 0.995(weight ratio preferably), more preferably be positioned at 0.80 to 0.99(weight ratio) between (containing end points), more preferably be positioned at 0.85 to 0.98(weight ratio) between (containing end points), be positioned at best 0.90 to 0.97(weight ratio).

In above-mentioned fusible adhesion agent (C1-6 or C1-7), above-mentioned fusible binding agent (being fusible outer cover thing D1 or D2) is coated on the core core 1 or 2 that comprises above-mentioned performance enhancers (E), the ratio that above-mentioned performance enhancers (E: i.e. medical additive E1 or E2 wherein) or above-mentioned core core 1 or 2 account for whole above-mentioned fusible adhesion agent is usually located at 0.05 to 0.995(weight ratio), preferably be positioned at 0.125 to 0.99(weight ratio) between (containing end points), more preferably be positioned at 0.25 to 0.98(weight ratio), more preferably be positioned at 0.5 to 0.95(weight ratio), correspondingly, the ratio that above-mentioned hot-melt adhesive (D: i.e. fusible outer thing D1 or the D2 of covering wherein) accounts for whole above-mentioned fusible adhesion agent is usually located at 0.005 to 0.95(weight ratio), preferably be positioned at 0.01 to 0.875(weight ratio) between (containing end points), more preferably be positioned at 0.02 to 0.75(weight ratio), more preferably be positioned at 0.05 to 0.50(weight ratio).

In above-mentioned fusible adhesion agent (C1-6,7), its performance enhancers (E) for or be selected from the more above-mentioned fusible outer core core that contains medical additive (E1) that thing (D) is high that covers of at least one fusing point.Composition in this core core is that medical additive (E1) can be that single component or multicomponent can be also multicomponent solid dispersion (/ or body) or their physical mixture, and between the multicomponent component, amount ratio can be arbitrarily.

In above-mentioned fusible adhesion agent, can also further include other components, active component as mentioned below or medicine (preferably fat-soluble active ingredient or medicine), active component or medicine (preferably fat-soluble active ingredient or medicine) be dissolved fast or the pharmaceutic adjuvant acid of stripping or pharmaceutic adjuvant alkali, super-disintegrant, the sweller that can not form strong gel, foaming agent (effervescent) etc.These component particle particle diameters (usually) are less than 30 μ m (about 155 orders, taylor criteria), preferably be less than 10 μ m (about 500 orders, taylor criteria), more preferably be less than 5 μ m (approximately 2000 orders, taylor criteria), more more preferably be less than 1 μ m (about 10000 orders, taylor criteria), more more preferably be less than 100nm, be less than best 10nm.The ratio that the consumption of these components in above-mentioned fusible adhesion agent (C1-1～C1-9) accounts for whole above-mentioned fusible adhesion agent (C1-1～C1-9) gross weight is 0.1%(wt./wt.) to 50%(wt./wt.), be preferably 0.5%(wt./wt.) to 30%(wt./wt.), be more preferably 0.5%(wt./wt.) to 20%(wt./wt.), be 1%(wt./wt. best) to 15%(wt./wt.), above percentage by weight is based on the gross weight of above-mentioned fusible adhesion agent (C1-1～C1-9).

" super-disintegrant " same above described " super-disintegrant " that the present invention is used at this, no longer repeat." can not form the sweller of strong gel " same above described " can not form the sweller of strong gel " that the present invention is used at this, no longer repeat.The components such as super-disintegrant, the sweller that can not form strong gel, foaming agent (effervescent) make above-mentioned fusible adhesion agent fracture fast, thereby make the quicker disintegrate of tablet, for medicine discharges and provides safeguard fast.

Active component or medicine (preferably fat-soluble active ingredient or medicine) are particularly conducive to medicine while disperseing with above-mentioned superfine particle (as particle diameter is less than in 5 μ m or 100nm), particularly unimolecule state (as particle diameter is less than 1nm) in above-mentioned fusible adhesion agent and discharge fast.

Three, active component or medicine

The active component used as the present invention, can be any pharmaceutically or the threpsology on there is material therapeutical effect or preventive effect, just have no particular limits.The present invention can with the active component example be listed below:

-medicine for central nervous system :-central stimulants: idebenone, phendimetrazine, piracetam, pyritinol, vinpocetine, dimefline, aniracetam, meclofenoxate, caffeine, modafinil, pentetrazole.-analgesic: bucinnazine, buprenorphine, dihydroetorphine, floctafenine, dicentrine, codeine, rotundine, morphine, Ergotamine, meptazinol, methadone, nefopam, Pethidine, piminodine, oxycodone, hydromorphinol, tramadol, sumatriptan, tetrahydropalmatine, dextropropoxyphene, dextromethorphan, levorphanol, levomoramide.-antipyretic analgesic: aspirin, acetaminophen, phenacetin, oxyphenbutazone, tiaramide, magnesium salicylate, imidazole salicylate, isopropylantipyrine.-anti-inflammation analgesia medicine: alminoprofen, acemetacin, azapropazone, ampiroxicam, orgotein, olsalazine, benorylate, pirprofen, ibuprofen, bucillamine, aceclofenac, bufexamac, diflunisal, fenbufen, flurbiprofen, flufenamic acid, Guacetisal, clidanac, mefenamic acid, meclofenamic acid, aurothioglucose, auranofin, leflunomide, clofenamic acid, loxoprofen, Aristolochic Acid, meloxicam, mesalazine, nabumetone, naproxen, niflumic acid, etodolac, zaltoprofen, guaiazulene, etofenamate, isoxicam, ketoprofen, tenoxicam.-antigout drug: glucosamine, benzbromarone, allopurinol, colchicine, probenecid, irtemazole.-antiparkinsonian drug: benzhexol, biperiden, doreptide, entacapone, amantadine, carbidopa, quinagolide, rasagiline, memantine, selegiline, tolcapone, bromocriptine, levodopa, mofegiline, moxifensine, pareptide, donepezil.-psychosis: alizapride, anisopirol, azaperone, amperozide, amisulpride, ocaperidone, oxaflumazine, oxypertine, prochlorperazine, fluphenazine, haloperidol, droperidol, flupentixol, fluspirilene, risperidone, rimcazole, tiapride, thioridazine, clozapine, clopipazan, clopenthixol, chlorprothixene, loxapine, mosapramine, nemonapride, pipotiazine, pimozide, pramipexole, remoxipride, sulpiride, penfluridol, zotepine, bromperidol, olanzapine.-antianxiety drugs: alprazolam, estazolam, buspirone, flutazolam, lorazepam, chlormezanone, metaxalone, zuclopenthixol, etizolam, fludiazepam.-antidepressant: amitriptyline, amoxapine, amfebutamone, opipramol, desipramine, demexiptiline, fluvoxamine, fluoxetine, carpipramine, clomipramine, maprotiline, mianserin, paroxetine, methylphenidate, protriptyline, trimeprimine, Sertraline, Herba Hyperici perforati extract sheet, viloxazine, venlafaxine, sibutramine, citalopram, isocarboxazid.-antuepileptic: oxcarbazepine, beclamide, phenytoin, valproic acid and sodium thereof, magnesium salt, paramethadione, carbamazepine, carzenide, lamotrigine, riluzole, primidone, topiramate, ethadione, etazepine, ethotoin, ethosuximide, zonisamide, tiagabine, mephenytoin.-tranquilizer, hypnotic, anticonvulsant and other: oxazolam, barbital, phenobarbital, glutethimide, Quetiapine, nizofenone, gastrodine, bromisoval, etomidate, acegastrodine, Zaleplon, zopiclone, zolpidem, betahistine, vincamine, flunarizine, flumedroxone, flurotyl, cyclandelate, pentoxifylline, dihydroergotamine mesilate, rizatriptan, methysergide, naratriptan, xantinol nicotinate, nicergoline, kallidinogenase, nicotinic acid, iprindole, eletriptan, epoprostenol, iprazochrome, papaverine, Zolmitriptan, levetiracetam.-automonic thing: arotinolol, alprenolol, atenolol, esmolol, benzatropine, bisoprolol, scopolamine, spectinomycin hydrochloride, carteolol, carvedilol, labetalol, metoprolol, moprolol, thymoxamine, nadolol, Anisodamine, celiprolol, cetamolol, timolol, tamsulosin, sotalol, Yohimbine, Anisodine, carvedilol, tamsulosin, tropicamide, propantheline bromide.-circulatory system drug :-calcium antagonists: anipamil, barnidipine, benidipine, bepridil, devapamil, falipamil, cinnarizine, lacidipine, Manidipine, tiapamil, verapamil, dexverapamil.The medicine of-treatment chronic cardiac insufficiency: bucladesine, digoxin, denopamine, strophanthin K, dobutamine, docarpamine, thevetin, milrinone, enoximone, levosimendan, alifedrine.-anti-arrhythmic: aprindine, amiodarone, pilsicainide, disopyramide, flecainide, quinidine, modecainide, moracizine, procainamide, Propafenone, Ivabradine, itrocainide, bretylium tosilate, mexiletine, stirocainide.-control angina pectoris medicine: oxyfedrine, isosorbide mononitrate, ligustrazine, diltiazem, erythrityl tetranitrate, hexobendine, adenosine cyclophosphate, lidoflazine, muscone, dipyridamole, pentaerithrityl tetranitrate, nitroglycerin, imolamine, etafenone, adenosine cyclophosphate.-peripheral vasodilators: apovincamine, vincamine, pinacidil, vinconate, vintoperol, dagapamil, buflomedil, fasudil, gallopamil, hydralazine, cadralazine, minoxidil, nicorandil, naftidrofuryl, trapidil, dihydralazine, urapidil, brovincamine, inositol nicotinate, elnadipine, isopropyl ground, iproxamine, papaveroline, stevaladil, levemopamil, zolertine.-hypotensor: alfuzosin, alacepril, anaritide, amlodipine, betanidine, benazepril, Rhomotoxin, bunazosin, bendazol, delapril, dilevalol, bupicomide, doxazosin, irbesartan, felodipine, fosinopril, tetrandrine, methyldopa, daidzein, pentolinium tartrate, captopril, Candesartan, quinapril, clonidine, lisinopril, ramiprilat, rilmenidine, reserpine, spirapril, lofexidine, mecamylamine, nilvadipine, nicardipine, nimodipine, nitrendipine, nisoldipine, pargyline, perindopril, trandolapril, terazosin, temocapril, tolonidine, cilazapril, nifedipine, valsartan, isradipine, Elisartan, enalkiren, enalapril, enalaprilat, Eprosartan, indoramine, levlofexidine, zofenopril, zofenoprilat, telmisartan.-adjusting blood fat medicine and antiatherosclerotic: atorvastatin, acipimox, phenylpropanolamine, felypressin, bezafibrate, pyricarbate, beclobrate, dalvastatin, Elastase, dopamine, dopexamine, fenofibrate, fluvastatin, ciprofibrate, gemfibrozil, colestipol, colestyramine, crilvastatin, clinofibrate, lecimibide, clofibrate, aluminum clofibrate, lovastatin, mevastatin, Nicanartine, nicofibrate, pravastatin, probucol, cerivastatin, simvastatin, linoleic acid, etofylline clofibrate, dextrothyroxine sodium, Hyodeoxycholic Acid.-medicine for respiratory system: aminophylline, ambroxol, orciprenaline, oxeladin, benproperine, bitolterol, benzonatate, pirbuterol, sodium dibunate, dimethoxanate, deptropine, erdosteine, fenoterol, pholcodine, hexoprenaline, clenbuterol, clobutinol, Mabuterol, montelukast, picoperine, terbutaline, guaifenesin, sulfogaiacol, xamoterol, levopropoxyphene, isoaminile, acetylcysteine, ketotifen, terbutaline, tulobuterol, eprazinone, terpinol.-medicine for digestive system :-drugs for antiacid and peptic ulcer diseases: omeprazole, balsalazide, ornoprostil, enprostil, famotidine, dihydroxyaluminum aminoacetate, bismuth potassium citrate, lansoprazole, rabeprazole, sucralfate, almagate, bismuth aluminate, hydrotalcite, rosaprostol, roxatidine, misoprostol, nizatidine, pirenzepine, plaunotol, pantoprazole, troxipide, sofalcone, telenzepine, vitamin U, irsogladine, ecabet.-gastrointestinal antispasmodic medicine: adiphenine.-digestant: ociltide, Pancreozymin amylase, citric acid, carnitine, pepsin, cisapride, trypsin, pancreatin, pancreatic lipase.-Bendectin, emetic and the intestines and stomach promote medicine: ondansetron, domperidone, granisetron, metoclopramide, clebopride, tropisetron, itopride, Bergeninum, levosulpiride, luteolin, lerisetron, lintopride, moguisteine, mosapride.-liver and gall diseases adjuvant drug: orazamide, chenodeoxycholic acid, febuprol, anethol trithione, inositol, inosine, bifendate, armillarisin A, tiopronin, thioctic acid, Malotilate, glucurolactone, oleanolic acid, hymecromone, nicotinylmethylamide, dehydrocholic acid, sodium dehydrocholate, deoxycholic acid, lactulose, silibinin, silymarin, cianidanol, ademetionine, ursodesoxycholic acid, protoporphrin disodium.-medicine for urological system: amiloride, azosemide, triamterene, bemetizide, polythiazide, bumetanide, piretanide, furosemide, cyclopenthiazide, the clorexolone, spirorenone, metyrapone, spironolactone, mefruside, lypressin, indapamide, epitizide, ethoxzolamide, etacrynic acid, sodium etacrynate, etozolin, ethiazide, acetazolamide, isopropamide iodide, ibopamine, Desmopressin, diclofenamide (dichlorphenamide), teprenone, metyrapone.-affect the medicine of blood and hemopoietic system: Sarpogrelate, ethylidenedicoumarol, the two bean ethyl esters of second, warfarin, phenindione, acenocoumarol, ferrous sulfate, Ferrous gluconate, calcium folinate, folic acid, iron dextran, mecobalamin, ferrous fumarate, gleptoferron, sodium ferulate, nucleotide, anethole, Rubidate, batilol, berbamine, acadesine, anagrelide, ataprost, ozagrel, Beraprost, pirmagrel, dazmegrel, dazoxiben, furegrelate, limaprost, clopidogrel, Rolafagrel, midazogrel, modipafant, nafagrel, pamicogrel, Alprostadil, troxerutin, ticlopidine, trifenagrel, Satigrel, sunagrel, cilostazol, ciprostene, nicogrelate, oxagrelate, itazigrel, oxybenzene sulphur ester calcium.-allergy preparations :-antihistaminic: acrivastine, alimemazine, astemizole, oxatomide, oxomemazine, diphenhydramine, phenindamine, propiomazine, buclizine, dimenhydrinate, the promethazine teoclate, azelastine, bufrolin, dorastine, doxylamine, embramine, pheniramine, fexofenadine, dimetindene, loratadine, clemastine, cloperastine, chlorphenamine maleate, mebhydrolin, meclizine, mequitazine, niaprazine, Cyproheptadine, setastine, ebastine, emedastine, epinastine, dexbrompheniramine, zafirlukast, levocabastine.-anaphylaxis medium sustained-release agent and other: azatadine, amlexanox, lodoxamide, tranilast, sodium cromoglicate, cetirizine, zaprinast, probicromil, proxicromil, tazanolast.-adrenocortical hormone and thyroliberin: deflazacort, dexamethasone, methylprednisolone, meprednisone, cortisone, triamcinolone.-gonadal hormone and short gonadal hormone: bicalutamide, estrone, estriol, medroxyprogesterone acetate, danazol, furazabol, flutamide, dienestrol, hexestrol, diethylstilbestrol, megestrol, medroxyprogesterone, raloxifene, nilutamide, gestrinone, toremifene, stanozolol, norgestrel.-pancreas hormone and other affect the medicine of blood glucose: acarbose, pioglitazone, metformin, voglibose, glibenclamide, glyclopyramide, glipizide, glyprothiazole, glibornuride, gliquidone, glimepiride, gliclazide, tolbutamide, miglitol, troglitazone, repaglinide, tolazamide.-thyroid hormones medicine and antithyroid drug: orotirelin, posatirelin, azetirelin, liothyronine, dibromotyrosine, thyropropic acid, thyromedan, thyroglobulin, montirelin, mipimazole, diotyrosine, tiratricol, levothyroxine, levothyroxine sodium, aminothiazole, propylthiouracil, iodothiouracil, methylthiouracil, thiamazole, carbimazole, thibenzazoline.-antimicrobial agents/antibiotic :-penicillins: amoxicillin, ampicillin, bacampicillin, oxazacillin, flucloxacillin, hetacillin, ciclacillin, sulbenicillin, carindacillin, cloxacillin, lenampicillin, nafcillin, pivampicillin, pivmecillinam, penicillin V, sultamicillin, dicloxacillin, talampicillin.-cephalosporins: Loracarbef, cefalexin, cefprozil, cefpodoxime, ceftibuten, cefaclor, cefixime, cefradine, cefbuperazone, cefaloglycin, cefadroxil, cefroxadine, cefteram, cefdinir.-beta-lactamase inhibitor: clavulanic acid, sulbactam, brobactam.-aminoglycoside: paromomycin, kanamycin, gentamycin, neomycin.-Tetracyclines and other: demeclocycline, doxycycline, guamecycline, metacycline, minocycline, oxytetracycline, tetracycline, chloromycetin.-Macrolide: azithromycin, triacetyloleandomycin, dirithromycin, erythromycin, erythromycin ethylsuccinate, kitasamycin, josamycin, clarithromycin, Roxithromycin, rokitamycin, spiramycin, meleumycin, midecamycin, erythromycin stinoprate, erythromycin estolate, acetylspiramycin.-other bacterial-infection resisting medicines: levofloxacin, ofloxacin, ciprofloxacin, norfloxacin, polymyxin E, clindamycin, lincomycin, fosfomycin, mikamycin, nysfungin, fibrauretin, berberine, hemsleyadin, Sodium Houttuyfonate.-antituberculotic: pyrazinamide, aminosalicylic acid, sodium aminosalicylate, prothionamide, cycloserine, rifabutin, rifapentine, rifampicin, ethambutol, isoniazid.-antifungal agent: flucytosine, fluconazol, griseofulvin, miconazole, itraconazole, ketoconazole, nystatin.-antiviral agents: acyclovir, famciclovir, valaciclovir, lamivudine, ribavirin, Moroxydine, zidovudine, doxifluridine, didanosine, zalcitabine.-antitumor drug: busulfan, cyclophosphamide, lomustine, semustine, thioguanine, mercaptopurine, idarubicin, aminoglutethimide, tamoxifen, Anastrozole, procarbazine, cantharidin, capecitabine, letrozole, melphalan.-affect the medicine of body's immunity: actarit, propagermanium, azathioprine, mizoribine, tacrolimus.-protein: DNA enzyme, alginase, superoxide dismutase and lipase, polypeptide, oligopeptide.-nucleotide.-vitamin and Amitin: vitamin A, B, C, D, E, K etc. and derivant thereof, aminoacid;-appetrol: aminorex, amfepramone, amfepentorex, amfecloral, ortetamine, benfluorex, difemetorex, benzfetamine, propylhexedrine, chlorphentermine, fenisorex, fenbutrazate sweet smell, fluorine Lamine, oxazimedrine, fenproporex, phentermine, furfenorex.-other drug: finasteride, Alendronate sodium, alosetron, orlistat, epristeride, epalrestat, tolterodine, tolrestat, Chinese herbal medicine powder and the Chinese herbal medicine extract that contains active component.

Comprise following active component its pharmaceutically available salt form, free acid form, free alkali form, hydrate, various crystal formation and optical isomer for active matter of the present invention.

The present invention is more suitable for the poor active component of compressibility, medicine as poor as viscosity (example is as agysical, ferrous sulfate, quinine sulfate and banthine bromide), the medicine that viscosity is very large (as protein-based: yeast tablet and polyzyme tablets, Chinese herbal medicine extractum), the larger medicine of elasticity is as the Chinese herbal medicine powder.

Use level to related activity composition A1, general so long as measure and be not particularly limited safely and effectively in treatment, but with respect to tablet weight, be better the treatment on safe and effective (agent) amount more than, the tablet weight (or 0.0001%wt./wt. to 90%wt./wt.) that 90%wt./wt. is following, be more preferably the treatment on safe and effective (agent) amount more than, the tablet weight (or 0.001%wt./wt. to 70%wt./wt.) that 70%w/w is following, best is in treatment more than safe and effective (agent) amount, the tablet weight (or 0.001%wt./wt. to 50%wt./wt.) that 50%w/w is following, above percentage by weight is based on the gross weight of tablet.

Use level to related activity composition A2 in above-mentioned fusible adhesion agent (C2-1, C2-2), the ratio that above-mentioned active components A 2 or core core 3 account for whole above-mentioned fusible adhesion agent can be arbitrarily, but normally be positioned at 0.005 to 0.995(weight ratio), preferably be positioned at 0.05 to 0.95(weight ratio) between (containing end points), more preferably be positioned at 0.15 to 0.85(weight ratio) between (containing end points), more more preferably be positioned at 0.25 to 0.75(weight ratio) between (containing end points), be positioned at best 0.35 to 0.65(weight ratio); Correspondingly, and above-mentioned hot-melt adhesive (D:, the fusible binding agent D1 in C2-1; The fusible outer thing D3 that covers in C2-2) ratio that accounts for whole above-mentioned fusible adhesion agent normally is positioned at 0.005 to 0.995(weight ratio), preferably be positioned at 0.05 to 0.95(weight ratio) between (containing end points), more preferably be positioned at 0.15 to 0.85(weight ratio) between (containing end points), more more preferably be positioned at 0.25 to 0.75(weight ratio) between (containing end points), be positioned at best 0.35 to 0.65(weight ratio).

When tablet of the present invention has been supposed to better machine performance, aforementioned proportion is positioned at 0.3 to 0.7(weight ratio).When active components A 2 is not hydrophilic and tablet has been supposed to better hydrophilic (or in water dispersibility), aforementioned proportion is positioned at 0.005 to 0.50(weight ratio) (preferably 0.05 to 0.45(weight ratio)); When tablet of the present invention has been supposed to better weatherability, aforementioned proportion is positioned at 0.50 to 0.995(weight ratio), 0.50 to 0.95(weight ratio preferably).

Due to the present invention can be when keeping original cellular structure, obtain enough tablet strength, therefore can improve medicine or the active components A incorporation with respect to tablet weight.In the large situation of the particle diameter of medicine or active components A, the cause of rough sense is arranged during due to intraoral disintegration, thereby comparatively ideal be that average particulate diameter is below 250 μ m.In case of necessity, can be crushed to average particulate diameter approximately below 200 μ m with suitable pulverizer equipment in advance to medicine, be crushed to preferably average particulate diameter approximately below 100 μ m (approximately 155 orders, taylor criteria), better to approximately below 25 μ m.

The bad active component for stability, available macromolecule filming material, cured etc. carries out coating.Active component to volatile and chemical instability etc. can carry out enclose by cyclodextrin and derivant thereof.Such coating material can be enumerated water-insoluble macromolecule, gastric solubility macromolecule, enteric solubility macromolecule or the waxy substance etc. as polymer substance.

" the pharmaceutically acceptable additive " the present invention relates to refer to that solid formulation comprises one or more can be mixed with each other and can not reduce solid-state or the liquid and medicinal auxiliary material that be applicable to part or whole body administration (containing its capsule compound) of solid formulation stability and/or effect without interaction.Concrete dosage form, solid formulation practical situation, preparation method and the subjective demands etc. of the selection of the additive the present invention relates to and the selective basis of consumption thereof are determined, not exclusively are confined to the restriction of this paper.As other additive used in the present invention, so long as pharmaceutically allowed, can be used as the various excipient that additive is used, have no particular limits.Such as super-disintegrant, the sweller that can not form strong gel, foaming agent (effervescent), binding agent (preferably dry adhesives), lubricant, plasticizer, sweeting agent, aromatic, coloring agent, tart flavour flavoring agent, stabilizing agent etc. are arranged.Such additive can be used one or more to be used in combination.In acid flavoring, such as citric acid, Tartaric acid, malic acid etc. are arranged.In foaming agent, such as sodium bicarbonate etc. is arranged.Stabilizing agent can carry out various research and select on medicine.These additives can suitably add in right amount, make certain a kind to be used in combination with two or more.

" super-disintegrant " same above described " super-disintegrant " that the present invention is used at this, no longer repeat." can not form the sweller of strong gel " same above described " can not form the sweller of strong gel " that the present invention is used at this, no longer repeat.

The components such as super-disintegrant, the sweller that can not form strong gel, foaming agent (effervescent) are except being included in above-mentioned diluent (B) and/or above-mentioned fusible adhesion agent (C) granule China and foreign countries, also addition is admixed at tablet in addition, so that the quicker disintegrate of tablet is accelerated medicine and is discharged fast.

" dry adhesives " that the present invention is used, its effect is to make to be bonded together than small-particle, after guaranteeing to granulate, larger particle can keep certain form, can and guarantee that the fragility that reaches certain is beneficial to disintegrate, can also guarantee the more effective performance of effect of disintegrating agent and sweller, avoid the adverse effect of solvent to disintegrate (expansion) effect of disintegrating agent (sweller) simultaneously.Useful dry adhesives includes, but are not limited to: starch, for example Rhizoma Solani tuber osi, wheat and maize starch; The Polyethylene Glycol that Polyethylene Glycol, especially molecular weight are 4000～6000; Polyvinylpyrrolidone, crospolyvinylpyrrolidone; Cross-linked carboxymethyl cellulose, carboxymethyl cellulose, hydroxypropyl emthylcellulose; Pregelatinized Starch, carboxymethyl starch; The microcrystalline Cellulose of microcrystalline Cellulose, crystalline cellulose, cellulose powder, silication; Dicalcium phosphate, tricalcium phosphate, magnesium trisilicate, Pulvis Talci, Aerosil 200 (as Aerosil), light anhydrous silicic acid; Mannitol, lactose, maltose alcohol, Sorbitol, xylitol, lactose (anhydrous or as hydrate, for example monohydrate), D-glucose, maltose, sucrose, glucose, fructose or maltodextrin; And concurrent mixture.Particularly preferably, dry adhesives is microcrystalline Cellulose.

Above-mentioned " pharmaceutically acceptable additive " particularly above-mentioned super-disintegrant, the sweller that can not form strong gel, foaming agent (effervescent), dry adhesives and composition thereof consumption in tablet preferably with about 0.1～50% (w/w), more preferably with 0.5～40%, more preferably, with 3～30%, this is based on the weight of tablet.

Four, preparation method

On the other hand, the present invention relates to the preparation method of (hydrophilic porous) tablet (or rapidly disintegrate in oral cavity/or solution tablet) of a kind of performance improvement, the method comprises four basic operations:

(1), fusible adhesion agent (C) preparation section

Make the particulate matter that forms solid dispersion (/ or body) (particulate matter) and/or make above-mentioned fusible binding agent (D) be coated on above-mentioned performance enhancers (E) as the above-mentioned fusible binding agent (D) of dispersant and above-mentioned performance enhancers (E) as being dispersed thing (dispersate) form the solid coating, must be for fusible adhesion agent of the present invention (C).This fusible adhesion agent (C) particulate matter comprises the preparation method that the solid dispersion (/ or body) (particulate matter) of above-mentioned fusible binding agent (D) and above-mentioned performance enhancers (E) and/or above-mentioned fusible binding agent (D) be coated on the solid coating (particulate matter) that above-mentioned performance enhancers (E) forms and includes but not limited to the pelletize of melting dispersion method, the pelletize of solvent melting dispersion method, solvent dispersion (as emulsifying) method pelletize and further spray drying method thereof, spray drying coats method, (spraying) coating method pelletize or bed spray coating pelletizing method or etc.Because existing relevant monograph is explained in detail this, as " novel pharmaceutical formulation and new technique ", Lu Bin, People's Health Publisher, April in 1998 the 1st edition, the 1st, 2,5,6 chapters), below only it is briefly described:

1), as the above-mentioned fusible binding agent (D) of dispersant and above-mentioned performance enhancers (E) as being dispersed thing (dispersate), form the preparation method of solid dispersion (/ or body) (particulate matter)

Melting dispersion method pelletize-i:, heat above-mentioned fusible binding agent (D) and make its fusing with above-mentioned performance enhancers (E), the fusible binding agent (D) that perhaps heats above-mentioned solid makes its fusing, add above-mentioned performance enhancers (E) or pulverized that (thin Yu of granule Yu is good, (usually) its mean diameter is not more than 100 μ m (about 155 orders, taylor criteria), preferably its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, be not more than best 10nm) performance enhancers (E) granule of above-mentioned solid, make it to be uniformly dispersed and form liquid mixing thing ((usually) dispersate mean diameter is not more than 100 μ m (about 155 orders, taylor criteria), preferably its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, be not more than best 10nm) preferably form homogeneous phase liquid molten thing as liquid solution, press afterwards the stirring-granulating method, rotate comminution granulation, cooling crush, casting, the spreading comminution granulation, extrude the various proper method pelletizes such as spheronization, usually finally sieve on demand the particulate matter of required size ((usually) is less than 28 orders, preferably be less than 60 orders, more preferably be less than 100 orders, preferably be less than 200 orders, taylor criteria).

Solvent melting dispersion method pelletize-i: the fusible binding agent (D) that heats above-mentioned solid makes its fusing, add and be dissolved in or be scattered in suitable volatile medicinal solvent (as that heated or water or volatile oil or ethanol not heating, acetone, ethyl acetate, ether or etc. medicinal volatile organic solvent and composition thereof) above-mentioned performance enhancers (E), make it to be uniformly dispersed and form liquid mixing thing ((usually) dispersate mean diameter is not more than 100 μ m (about 155 orders, taylor criteria), preferably its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, be not more than best 10nm) preferably form homogeneous phase liquid molten thing as liquid solution, fling to above-mentioned medicinal solvent and by the stirring-granulating method, rotate comminution granulation, cooling crush, casting, the spreading comminution granulation, extrude the various proper method pelletizes such as spheronization, usually finally sieve on demand the particulate matter of required size ((usually) is less than 28 orders, preferably be less than 60 orders, more preferably be less than 100 orders, preferably be less than 200 orders, taylor criteria).This method is more suitable for that high-melting-point or infusibility melt or the dispersibility in above-mentioned fusible binding agent (D) fused solution or poor above-mentioned (solid) performance enhancers (E) of dissolubility, as ionic surfactant, steroid compound.

Solvent dispersion method pelletize-i: as an embodiment, the fusible binding agent (D) of above-mentioned solid and above-mentioned performance enhancers (E) are dissolved in and/or disperse appropriate suitably volatile medicinal solvent (as that heated or water or volatile oil or ethanol not heating, acetone, ethyl acetate, ether or etc. medicinal volatile organic solvent and composition thereof), make it to be uniformly dispersed and form liquid dispersed mixture (as Emulsion) (((usually) dispersate mean diameter is not more than 100 μ m (about 155 orders, taylor criteria), preferably its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, be not more than best 10nm)) homogeneous phase liquid solution preferably, fling to above-mentioned medicinal solvent and by the stirring-granulating method, rotate comminution granulation, the fusing cooling crush, casting, the spreading comminution granulation, extrude the whole bag of tricks pelletizes such as spheronization, usually finally sieve on demand the particulate matter of required size ((usually) is less than 28 orders, preferably be less than 60 orders, more preferably be less than 100 orders, preferably be less than 200 orders, taylor criteria).

2), above-mentioned fusible binding agent (D) outsourcing is overlying on the preparation of the particulate matter of above-mentioned performance enhancers (E)

Solvent dispersion spraying or lyophilization coat method pelletize-i: as an embodiment, above-mentioned (solid) fusible binding agent (D) and above-mentioned (solid) performance enhancers (E) are dissolved in and/or disperse appropriate suitably volatile medicinal solvent (as that heated or water or volatile oil or ethanol not heating, acetone, ethyl acetate, ether or etc. medicinal volatile organic solvent and composition thereof), make it to be uniformly dispersed and form liquid dispersed mixture (as Emulsion) ((usually) dispersate mean diameter is not more than 100 μ m (about 155 orders, taylor criteria), preferably its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, be not more than best 10nm) homogeneous phase liquid solution preferably, spraying or the above-mentioned liquid dispersed mixture of lyophilization (as Emulsion) or homogeneous phase liquid solution (also having flung to above-mentioned solvent simultaneously) and get final product, usually finally the particulate matter of required size on demand sieves to obtain.

Dissolution with solvents or dispersion spray coated method pelletize or fluid bed coat method comminution granulation-i: as an embodiment, above-mentioned (solid) fusible binding agent (D) is dissolved in and/or disperses appropriate suitably volatile medicinal solvent (as that heated or water or volatile oil or ethanol not heating, acetone, ethyl acetate, ether or etc. medicinal volatile organic solvent and composition thereof), to above-mentioned (solid) performance enhancers (E) granule of suspend (as in fluid bed), ((usually) its mean diameter is not more than 100 μ m (about 155 orders, taylor criteria), preferably its mean diameter is not more than 25 μ m (about 500 orders, taylor criteria), more preferably be not more than 5 μ m (about 2000 orders, taylor criteria), more preferably be not more than 1 μ m (about 10000 orders, taylor criteria), more preferably be not more than 100nm, be not more than best 10nm) spray coated (also flung to above-mentioned solvent) and get final product simultaneously, usually finally the particulate matter of required size on demand sieves to obtain.

In the middle of, from the productivity aspect, above-mentioned hot-melt adhesive (D) is dispersed on above-mentioned performance enhancers (E) surface, fluidized bed granulation is satisfied.

In above-mentioned spray coated method, this coating thickness with use coating increment 0.5 to 200% weight (1 to 100% weight preferably, more preferably 2 to 50% weight, 3 to 20% weight best) above-mentioned hot-melt adhesive (D) corresponding, in concrete application, can suitably increase and decrease.

In the preparation process of above-mentioned solid dispersion (/ or body) (particulate matter) and/or above-mentioned solid coating (particulate matter), sometimes need above-mentioned decentralized photo is disperseed to reach the dispersed phase particles of required particle size, below above-mentioned decentralized photo is disperseed to be briefly described, refer to relevant monograph or data, above-mentioned decentralized photo carried out to process for dispersing and include but not limited to:

1), mechanical force dispersion method (a kind of form that micron, submicron, nanoparticle (decentralized photo) is fully disperseed in medium (continuous phase) by mechanical energy such as extraneous shearing force or impact forces.Commonly used have high-speed stirred, ball milling dispersion, grinding distribution, a colloid mill dispersion etc.This technology obtains applications well in the preparation process of pharmaceutical preparation);

2), ultrasound wave disperses (localized hyperthermia produced while utilizing ultrasonic cavitation, high pressure or strong shock wave and microjet etc., can weaken the interaction energy between making it fully to disperse greatly, effectively prevent from making it fully disperseing to reunite and make it abundant dispersion);

3), the high power treatment method (is not directly micron, submicron, nanoparticle (decentralized photo) to be disperseed, but by the high energy particle effect, produce active site at above-mentioned particle surface, increase surface activity, make it easily and other material generation chemical reaction or adhere to, above-mentioned improving particle surface is reached to the purpose of easy dispersion.The high power treatment method comprises corona, ultraviolet light, microwave, plasma ray etc.);

4), chemical method disperses (to utilize the surface active groups of nanometer, submicron, micron particle (decentralized photo), with can react or association organic compound deposits yields chemical bond or hydrogen bond etc. link, nanometer, submicron, micron particle (decentralized photo) are connected with organic compounds side chain or group because of surface, there is solubility in organic media, thereby strengthen the dispersion of grain husk grain in organic media).

Above-mentioned nanometer, submicron, the stable dispersion of micron particle (decentralized photo) in the liquid phase medium of above-mentioned fusible binding agent (D) generally comprise following process: moistening, mechanical dispersion and stably dispersing.Moistening is often referred to the process that the interface between above-mentioned granule and granule is replaced by the liquid phase medium interface of granule and above-mentioned fusible binding agent (D), and the heat of wetting is larger, and granule more easily disperses in the liquid phase medium of above-mentioned fusible binding agent (D).Mechanical dispersion is to utilize shearing force.By a large amount of grain refines, diplomatic corps's aggressiveness depolymerization, wetted, dissolved, the process that is wrapped absorption.Stably dispersing refers to primary partical or less aggregate is shielded to Van der Waals force under the effects such as electrostatic repulsion, sterically hindered repulsion, is the process that particles no longer is assembled.

In addition, vacuum pressure infiltration method, reaction in-situ composite algorithm, pressure-free impregnation method, spray co deposition method, machinery " alloying " method, also can be used for the solid dispersion that the present invention preparation comprises above-mentioned fusible binding agent (D) and above-mentioned performance enhancers (E) (/ or body) (particulate matter) and/or above-mentioned fusible binding agent (D) and be coated on the solid coating (particulate matter) that above-mentioned performance enhancers (E) forms.Nanometer, submicron and micron particle that these methods also can be used for preparing medicine or medical additive in the present invention, make its micronization.

(2), tablet forming process

That is: be the state of basic homogeneous dispersion and make it there is the operation that pharmaceutically acceptable spatial shape (tablet) maintains tablet form in pharmacy for the tablet material that will contain active component (A1), pharmaceutically acceptable (water soluble or hydrophilic) diluent (B1), above-mentioned fusible adhesion agent (C1);

And/or

The tablet material of (water soluble or hydrophilic) diluent pharmaceutically acceptable in order to contain (B2), above-mentioned fusible adhesion agent (C2) is the state of basic homogeneous dispersion and makes it have the operation that pharmaceutically acceptable tablet spatial shape maintains tablet form in pharmacy.

This operation is to make the above-mentioned preparation supplementary material the present invention relates to: the particulate matter of diluent (B1), active component (A1) and fusible adhesion agent (C1) or diluent (B2), above-mentioned fusible adhesion agent (C2) is the state of basic homogeneous dispersion and makes it have pharmaceutically acceptable spatial shape in pharmacy is tablet form, except having no particular limits in addition.To the preparation supplementary material that the present invention relates to by following modulator approach, as, adopt physical mixed, wet granulation, dry granulation, spray drying method (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete), fluidized bed prilling (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete), the stirring-granulating method (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete), rotating comminution granulation (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete), the fusing cooling crush (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete or fusible adhesion agent (C) preparation section, forming process, heating process and refrigerating work procedure concentrate a step to complete), casting (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete or fusible adhesion agent (C) preparation section, forming process, heating process and refrigerating work procedure concentrate a step to complete), the spreading comminution granulation (is fusible adhesion agent (C) preparation section, forming process concentrates a step to complete) etc. the whole bag of tricks pelletize, perhaps complete after above-mentioned technique more further as repressed process forming is lamellar, the preparation supplementary material direct compression, the dry powder sheeting that have perhaps mixed, tablet (being that fusible adhesion agent (C) preparation section, forming process, heating process and refrigerating work procedure concentrate a step to complete) is made in the fusing of preparation supplementary material, the casting perhaps mixed, perhaps sintering system draw, push and subsequently rounding or directly make ball or tablet (as, by flat board) (be fusible adhesion agent (C) preparation section, forming process, heating process and refrigerating work procedure concentrate a step complete), or complete after above-mentioned technique more further by as pressing process, making tablet.

In forming technology, (usually) adopts pressing process.Such pressing process, (usually) is after tablet supplementary material fusion lubricant, to adopt in advance tablet machine to carry out tabletting.For making the shape maintains of tablet, pressing process must be used the pressure that is not less than the minimum pressure limit, simultaneously, in order to obtain satisfied porosity, need again to adopt lower pressure, now tabletting pressure (usually) is the 10-700kg/ pestle, and satisfied is the 30-4OOkg/ pestle, and more satisfied is the 50-250kg/ pestle.

Forming process in the solid preparation preparation method the present invention relates to preferably adopts non-pressing process.

As an embodiment, above-mentioned preparation supplementary material: after the particulate matter of diluent (B1), active component (A1) and fusible adhesion agent (C1) or diluent (B2), above-mentioned fusible adhesion agent (C2) etc. mixes or dissolve and/or be suspended in the solvent allowed in pharmacy after direct packaging in preparation nib (moulds) or packaging material mold pressing bubble eye (blisters of final pack), heating, when being arranged, solvent can fling in the lump, melting, cooling.This technique is without working pressure.Concrete operations are referring to referring to US6083531, WO0247607.

As another embodiment, above-mentioned preparation supplementary material pack into heatable feed hopper or other appropriate containers, heat fused preparation supplementary material is as above-mentioned fusible adhesion agent (C), fusion mixture is introduced in the calender that two reverse molded rollers are arranged and is molded as tablet, and this two reverse molded rollers surface there is contrary mutually depression to accept and the molded tablet compositions.Concrete operations are referring to US4880585.

(3), tablet heating process

The temperature that the tablet molding soon obtained by operation (2) is heated to the melt temperature above (containing melt temperature) of the melting composition in above-mentioned fusible adhesion agent (C1 and/or C2) makes melting become the operation of fractional melting.

In " heating " of the present invention, by known method, undertaken, molding with operation (2) gained, so long as heating energy is dissolved by the above-mentioned hot-melt adhesive used in the present invention and above-mentioned performance enhancers or above-mentioned hot-melt adhesive is that above-mentioned fusible adhesion agent (C) dissolves, except active component in fusion process, composition in diluent and fusible adhesion agent does not degrade or non-volatile (but following degraded or volatilization porogen can except) in when heating in processing or preparation process, perhaps, above-mentioned active component, the 10%(that when the composition in diluent and above-mentioned fusible adhesion agent heats in processing or preparation process, the amount of degraded and/or volatilization is no more than the amount before processing or preparation is no more than 5% of amount before processing or preparation preferably, be no more than better processing or the preparation before amount 2%), more preferably, above-mentioned diluent and the infusible method of above-mentioned active component just have no particular limits outward." heating " operation like this, for example can adopt draft furnace, baking oven, calorstat to carry out.The kind of the bridging agent particulate matter that temperature conditions (above-mentioned) diluent, active component, hot-melt adhesive and the performance enhancers used according to the present invention forms suitably determines, as long as the above-mentioned hot-melt adhesive used and above-mentioned performance enhancers is dissolved or above-mentioned hot-melt adhesive dissolves in (usually) the present invention, in this process without material as active component in when heating degraded or volatilization (but following degraded or volatilization porogen can except), more preferably above-mentioned diluent and above-mentioned active component just do not melt and have no particular limits.In the present invention, temperature (usually) used is higher than the fusing point of (going out) above-mentioned hot-melt adhesive, more preferably higher than the fusing point of (going out) above-mentioned performance enhancers, temperature used (usually) is approximately 40 to approximately 150 ℃, is preferably approximately 60 to approximately 120 ℃, is more preferably approximately 70 to approximately 90 ℃.Kind, particularly desirable solid preparation intensity, the solid preparation disintegrating property etc. of the bridging agent particulate matter that time conditions forms according to diluent used, active component, hot-melt adhesive and performance enhancers suitably determine, (usually) is 0.5 to 120 minute, being preferably 1 to 60 minute, is more preferably 2 to 30 minutes.

" heating " of the present invention operation, also can be at surface or contiguous its surface heating of article shaped, make top layer as the above-mentioned hot-melt adhesive of 0.1 to 2mm the degree of depth and performance enhancers is dissolved or above-mentioned hot-melt adhesive dissolves, and inner hot-melt adhesive, performance enhancers are remained stationary, can obtain more quickly disintegrated solid preparation like this.Concrete operations are referring to US6258381.

(4), tablet refrigerating work procedure

That is: by the operation of the melting composition cooled and solidified in the above-mentioned fusible adhesion agent melted (C1 and/or C2) in the tablet molding that operation (3) obtain.The present invention so-called " cooling ", by known method, undertaken, so long as the present invention's above-mentioned hot-melt adhesive used and the method for above-mentioned performance enhancers or above-mentioned hot-melt adhesive melting after fixing (solidifying) just have no particular limits." cooling " like this, such as can adopt at room temperature place and the low temperature environment such as freezer under preserve and carry out.

Above-mentioned two connected steps or multistep or whole technique can concentrate a step to complete, as two steps or multistep in above-mentioned operation (2,3,4).

In of the present invention one preferred specific embodiments, in tablet, can also contain the volatilization or the degraded porogen be volatile component and/or the component that can be biodegradable into innocuous gas, to obtain the more tablet of macroporosity.Volatile component and/or the component fusion that can be biodegradable into innocuous gas by heating under normal pressure or reduced pressure, are volatilized volatile component to remove to form porous tablet after being mixed in the tablet supplementary material and making tablet from tablet.Volatile component is preferably volatilized and is removed in the melting stage.In a preferred preparation method, tablet is being heated to 45 to 110 ℃ under purging with nitrogen gas or decompression continuously, preferably 50 to 80 ℃, until volatile component is all volatilized away through distillation.Use purging with nitrogen gas to contribute to protect unsettled active component to avoid under these conditions degraded.Yet, for stable active component, 45 to 110 ℃ of temperature, preferably under 50 to 80 ℃, also can use air blowing.Suitable volatile component and the component that can be biodegradable into innocuous gas comprise normal pressure (1atm) or the lower material that can distil and/or can decompose of decompression (lower than 1atm), it can be used for example of the present invention as benzoic acid (mp121.5～123.5 ℃, 100 ℃ start distillation (1atm)), vanillin (mp81～83 ℃), ethyl vanillin (mp76～81 ℃, sterling mp77～78 ℃), natural or artificial camphor (natural camphor mp176～181 ℃, artificial camphor mp174～179 ℃), gum camphor (approximately 179.8 ℃ of mp, 204 ℃ start distillation (1atm)), levo-camphor (approximately 178.6 ℃ of mp, 204 ℃ start distillation (1atm)), raceme Mentholum (alcohol) (mp42～44 ℃), levorotatory menthol (mp41～45 ℃), natural or synthetic borneol (mp205-210 ℃), dextro Borneolum Syntheticum (approximately 208 ℃ of mp), L-Borneol (approximately 204 ℃ of mp), dextrorotation isoborneol (approximately 214 ℃ of mp), left-handed isoborneol (approximately 214 ℃ of mp), raceme isoborneol (approximately 212 ℃ of mp), dithiooxamide (dithio diamides) (approximately 41 ℃ of mp), 6-methyl-2-deracil (methylthiouracil) (approximately 330 ℃ of mp, 326～331 ℃ of decomposition), azulene sulfonic acid and salt thereof, butylated hydroxyarisol (mp57～65 ℃), di-tert-butyl hydroxy-methylbenzene (2,6-d-tert-butyl-p-cresol) (mp69～71 ℃), salicylic acid (mp158 ℃, 76 ℃ start distillation), aspirin, ethenzamide, the caffeine compounds is (as caffeine hydrate (mp238 °, 178 ° of distillations), the caffeine anhydride, caffeine citrate, caffeine benzoate), alanine, leucine, isoleucine, valine, phenylalanine, carbamide, urethane, ammonium halide is as ammonium chloride, ammonium bicarbonate, ammonium carbonate, ammonium acetate and composition thereof, preferably benzoic acid, vanillin, ethyl vanillin, raceme Mentholum (alcohol), levorotatory menthol, natural or synthetic borneol, left-handed isoborneol (approximately 214 ℃ of mp), raceme isoborneol (approximately 212 ℃ of mp), ammonium halide, ammonium bicarbonate, ammonium carbonate, ammonium acetate and composition thereof.The consumption of volatile component is 1% to 95% weight ratio, preferably 20% to 70%, more preferably 30% to 50%, and this is based on the weight of the tablet ingredients while mixing.

The tablet prepared according to above-mentioned the whole bag of tricks is " porous ", and (usually) its porosity is approximately 10 to approximately 95%, and satisfied is approximately 20 to approximately 90%, and more satisfied is approximately 40 to approximately 80%.

The tablet prepared by above-mentioned either method can be wrapped the skim coating material to improve the surface integral of sheet punishment.Suitable coating material include but not limited to disaccharide as sucrose, polysaccharide as maltodextrin and pectin and cellulose derivative as hydroxypropyl emthylcellulose and hydroxypropyl cellulose, yet, arbitrary coating all should be fully thin and be water-soluble, the rapid disintegrate ability with the obstruction free tablet in mouth.

Be below part optimal technical scheme of the present invention, list separately special instruction.

The tablet of 1. 1 kinds of performance improvements of optimal technical scheme, this tablet comprises:

1), at least one active components A 1;

2), at least one pharmaceutically acceptable hydrophilic diluent B 1; And

3), at least one is selected from following fusible adhesion agent C1:

C1-1: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion I of 25 ℃ of temperature, above-mentioned solid dispersion I contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, perhaps

C1-2: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion II of 25 ℃ of temperature, above-mentioned solid dispersion II contain at least one fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the surfactant E2 of above-mentioned medicinal lipid additive D2, perhaps

C1-3: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion III of 25 ℃ of temperature, above-mentioned solid dispersion III contain at least one fusing point (more above-mentioned diluent B 1 low but) hydrophilic surfactant E21 higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, perhaps

C1-4: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion IV of 25 ℃ of temperature, above-mentioned solid dispersion IV contain at least one fusing point (more above-mentioned diluent B 1 low but) hydrophilic surfactant E21 higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, perhaps

C1-5: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion V of 25 ℃ of temperature, above-mentioned solid dispersion V contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than the hydrophilic medical additive E2 of 25 ℃ of temperature, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, perhaps,

C1-6: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating I of 25 ℃ of temperature, above-mentioned solid coating I comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D1 and by the above-mentioned fusible outer core core 1 that fusing point that thing D1 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned fusible outer cover thing D1 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, above-mentioned core core 1 comprises the medical additive E3 that at least one pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, perhaps,

C1-7: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating II of 25 ℃ of temperature, above-mentioned solid coating II comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D2 and by the above-mentioned fusible outer core core 2 that fusing point that thing D2 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned fusible outer cover thing D2 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, above-mentioned core core 2 comprises the hydrophilic medical additive E4 that at least one pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, perhaps,

C1-8: the solid dispersion VI of the further combination in any of solid dispersion in above-mentioned fusible adhesion agent C1-1～C1-5, or,

C1-9: the mixture of two or more in above-mentioned fusible adhesion agent C1-1～C1-8;

And above-mentioned diluent B 1 and/or above-mentioned active components A 1 are by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C1;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (I～VI) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (I～II) is not more than 100 μ m;

And/or

This tablet comprises:

1), at least one pharmaceutically acceptable hydrophilic diluent B 2;

2), at least one is selected from following fusible adhesion agent C2:

C2-1: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid dispersion VII of 25 ℃ of temperature, above-mentioned solid dispersion VII contain at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature fusible binding agent D1 and and at least one active components A 2, above-mentioned fusible binding agent D1 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, and/or

C2-2: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid coating III of 25 ℃ of temperature, above-mentioned solid coating III comprise fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature cover thing D3 and by the above-mentioned fusible outer core core 3 that thing D3 coats that covers fusible outward, above-mentioned fusible outer cover thing D3 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, above-mentioned core core 3 comprises at least one active components A 2,

And above-mentioned diluent B 2 is by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C2;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (VII) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (III) is not more than 100 μ m.

The tablet of 2. 1 kinds of performance improvements of optimal technical scheme, this tablet comprises:

1), at least one active components A 1;

2), at least one pharmaceutically acceptable hydrophilic diluent B 1; And

3), at least one is selected from following fusible adhesion agent C1:

C1-10: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating IV of 25 ℃ of temperature, above-mentioned solid coating IV comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D4 and by the above-mentioned fusible outer core core 4 that fusing point that thing D4 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned core core 4 comprises the medical additive E3 that at least one fusing point is not less than 25 ℃ of temperature, above-mentionedly fusiblely outer cover thing D4 and comprise at least one following solid dispersion: contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) solid dispersion I that be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, or contain at least one fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion II of the surfactant E2 of above-mentioned medicinal lipid additive D2, or contain at least one fusing point (more above-mentioned diluent B 1 low but) solid dispersion III higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the hydrophilic surfactant E21 of 25 ℃ of temperature, or contain at least one fusing point (more above-mentioned diluent B 1 low but) higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the solid dispersion IV of the hydrophilic surfactant E21 of 25 ℃ of temperature or the solid dispersion VIII of their combination in any, above-mentioned solid dispersion (I～IV, VIII) the dispersed component particle in or dispersate particle or discontinuous phase average particle size are not more than 100 μ m, and/or

C1-11: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating V of 25 ℃ of temperature, above-mentioned solid coating V comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D5 and by the above-mentioned fusible outer core core 5 that fusing point that thing D5 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned core core 5 comprises the hydrophilic medical additive E4 that at least one fusing point is not less than 25 ℃ of temperature, above-mentioned fusible outer cover thing D5 comprise contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion V of the hydrophilic medical additive E2 of 25 ℃ of temperature, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, dispersed component particle in above-mentioned solid dispersion (V) or dispersate particle or discontinuous phase average particle size are not more than 100 μ m,

And above-mentioned diluent B 1 and/or above-mentioned active components A 1 are by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C1;

And the core core mean diameter be wrapped by above-mentioned solid coating (IV～V) is not more than 100 μ m;

And/or

This tablet comprises:

1), at least one pharmaceutically acceptable hydrophilic diluent B 2;

2), at least one is selected from following fusible adhesion agent C2:

C2-3: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid dispersion IX of 25 ℃ of temperature, above-mentioned solid dispersion IX contain at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature fusible binding agent D2 and and at least one active components A 2, above-mentioned fusible binding agent D2 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, or at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the surfactant E2 of above-mentioned medicinal lipid additive D2, or at least one fusing point (more above-mentioned diluent B 2 low but) hydrophilic surfactant E21 higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, or at least one fusing point (more above-mentioned diluent B 2 low but) hydrophilic surfactant E21 higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, or at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than hydrophilic medical additive E2 or their combination in any of 25 ℃ of temperature, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or

C2-4: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid coating VI of 25 ℃ of temperature, above-mentioned solid coating VI comprise fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature cover thing D6 and by the above-mentioned fusible outer core core 6 that thing D6 coats that covers fusible outward, above-mentioned core core 6 comprises at least one active components A 2, above-mentionedly fusiblely outer cover thing D6 and comprise at least one following solid dispersion: contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) solid dispersion I that be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, or contain at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion II of the surfactant E2 of above-mentioned medicinal lipid additive D2, or contain at least one fusing point (more above-mentioned diluent B 2 low but) solid dispersion III higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the hydrophilic surfactant E21 of 25 ℃ of temperature, or contain at least one fusing point (more above-mentioned diluent B 2 low but) solid dispersion IV higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the hydrophilic surfactant E21 of 25 ℃ of temperature, or contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion V of hydrophilic medical additive E2 of 25 ℃ of temperature or the solid dispersion X of their combination in any, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, above-mentioned solid dispersion (I～V, X) the dispersed component particle in or dispersate particle or discontinuous phase average particle size are not more than 100 μ m,

And above-mentioned diluent B 2 is by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C2;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (IX) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (VI) is not more than 100 μ m.

Optimal technical scheme 3. is according to the tablet of optimal technical scheme 1 or 2, and the core core mean diameter be wrapped by the dispersed component particle in wherein said solid dispersion or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating is not more than 25 μ m.

Optimal technical scheme 4. is according to the tablet of any one in optimal technical scheme 1 to 3, and the core core mean diameter be wrapped by the dispersed component particle in wherein said solid dispersion or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating is not more than 5 μ m.

Optimal technical scheme 5. is according to the tablet of any one in optimal technical scheme 1 to 4, and the core core mean diameter be wrapped by the dispersed component particle in wherein said solid dispersion or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating is not more than 1 μ m.

Optimal technical scheme 6. is according to the tablet of any one in optimal technical scheme 1 to 5, and the core core mean diameter be wrapped by the dispersed component particle in wherein said solid dispersion or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating is not more than 100nm.

Optimal technical scheme 7. is according to the tablet of any one in optimal technical scheme 1 to 6, and the core core mean diameter be wrapped by the dispersed component particle in wherein said solid dispersion or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating is not more than 10nm.

Optimal technical scheme 8. is according to the tablet of any one in optimal technical scheme 1 to 7, and the core core mean diameter be wrapped by the dispersed component particle in wherein said solid dispersion or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating is not more than 1nm.

Optimal technical scheme 9. is according to the tablet of any one in optimal technical scheme 1 to 8, and wherein said tablet is hydrophilic porous tablet.

Optimal technical scheme 10. is according to the tablet of any one in optimal technical scheme 1 to 9, and the porosity of wherein said tablet is 20 to 80%(preferably 30 to 60%).

Optimal technical scheme 11. is according to the tablet of any one in optimal technical scheme 1 to 10, and wherein said tablet is disintegrate rapidly in oral cavity/or solution tablet rapidly.

Optimal technical scheme 12. is according to the tablet of any one in optimal technical scheme 1 to 11, and wherein said tablet does not absorb water when taking, in oral cavity basically only with saliva in 30 seconds (preferably 10 seconds, more preferably 5 seconds) with interior disintegrate/or tablet of dissolving.

Optimal technical scheme 13. is according to the tablet of any one in optimal technical scheme 1 to 12, and wherein said diluent B 1 and/or diluent B 2 are selected from granule and/or the powder of hydrophilic crystalline state.

Optimal technical scheme 14. is according to the tablet of any one in optimal technical scheme 1 to 13, and wherein said diluent B 1 and/or diluent B 2 are selected from the diluent that balance meltage in the water of 25 ℃ of temperature or dispersion amount are not less than 10mg/1ml.

Optimal technical scheme 15. is according to the tablet of any one in optimal technical scheme 1 to 14, and wherein said diluent B 1 and/or diluent B 2 are selected from the diluent that balance meltage in the water of 25 ℃ of temperature or dispersion amount are not less than 33mg/1ml.

Optimal technical scheme 16. is according to the tablet of any one in optimal technical scheme 1 to 15, and wherein said diluent B 1 and/or diluent B 2 are selected from the diluent that balance meltage in the water of 25 ℃ of temperature or dispersion amount are not less than 100mg/1ml.

Optimal technical scheme 17. is according to the tablet of any one in optimal technical scheme 1 to 16, wherein said diluent B 1 and/or diluent B 2 be selected from its pore volume divided by the determined porosity of cumulative volume higher than 0.25 or its weight divided by the determined density of cumulative volume lower than diluent O.75.

Optimal technical scheme 18. is according to the tablet of any one in optimal technical scheme 1 to 17, and wherein said diluent B 1 and/or diluent B 2 are selected from the particulate matter that contains described diluent and disintegrating agent and/or can not form the sweller of strong gel.

Optimal technical scheme 19. is according to the tablet of optimal technical scheme 18, and in wherein said diluent, contained diluent and disintegrating agent and/or the use amount proportioning that can not form the sweller of strong gel are 1 ︰ 0.05～0.5(weight ratio).

Optimal technical scheme 20. is according to the tablet of any one in optimal technical scheme 1 to 19, and wherein said diluent B 1 and/or diluent B 2 are selected from the compositions that contains monosaccharide or its sugar alcohol, oligosaccharide or its sugar alcohol or their mixture and disintegrating agent and/or can not form the sweller of strong gel.

Optimal technical scheme 21. is according to the tablet of optimal technical scheme 20, and in wherein said diluent, contained monosaccharide or its sugar alcohol, oligosaccharide or its sugar alcohol or their mixture and disintegrating agent and/or the use amount proportioning that can not form the sweller of strong gel are 1 ︰ 0.05～0.5(weight ratio).

Optimal technical scheme 22. is according to the tablet of any one in optimal technical scheme 1 to 21, and wherein said diluent B 1 and/or diluent B 2 are selected from water miscible saccharide.

Optimal technical scheme 23. is according to the tablet of any one in optimal technical scheme 1 to 22, wherein said diluent B 1 and/or diluent B 2 are selected from hydrophilic following medicinal diluent: the oligosaccharide that monosaccharide, oligosaccharide, the degree of polymerization are 10～100, the sugar alcohol of above-mentioned sugar, the modularization derivant of the derivant that methylates of above-mentioned sugar or its sugar alcohol, methylolation derivant, hydroxyethylation derivant, hydroxypropylation derivant, hydroxyl butylation or above-mentioned group, and their mixture.

Optimal technical scheme 24. is according to the tablet of any one in optimal technical scheme 1 to 23, wherein said diluent B 1 and/or diluent B 2 are selected from calcium phosphate, calcium hydrogen phosphate, calcium glycerophosphate, calcium lactate, and their hydrate, and their combination or mixture.

Optimal technical scheme 25. is according to the tablet of any one in optimal technical scheme 1 to 24, wherein said diluent B 1 and/or diluent B 2 are selected from D-methionine, D-phenylalanine, L-Histidine, Serine, L-glutaminate, ALANINE, L-threonine, glycine, L-hydroxyproline, L-PROLINE, and their mixture.

Optimal technical scheme 26. is according to the tablet of any one in optimal technical scheme 1 to 25, and wherein said diluent B 1 and/or diluent B 2 are selected from L-threonine, ALANINE, glycine, L-hydroxyproline, L-PROLINE, and their mixture.

Optimal technical scheme 27. is according to the tablet of any one in optimal technical scheme 1 to 26, and wherein said diluent B 1 and/or diluent B 2 are selected from ALANINE, glycine, and their mixture.

Optimal technical scheme 28. is according to the tablet of any one in optimal technical scheme 1 to 27, and wherein said diluent B 1 and/or diluent B 2 are selected from dipeptides or the tripeptides that comprises L and/or D-Thr, L and/or D-alanine, glycine, L-hydroxyproline, L-PROLINE, lysine and pharmaceutical salts, arginine and pharmaceutical salts thereof.

Optimal technical scheme 29. is according to the tablet of any one in optimal technical scheme 1 to 28, wherein said diluent B 1 and/or diluent B 2 are selected from Calcium peptide, high F value oligopeptide, mineral element binding peptide, seasoning peptide, mannatide, and their combination or mixture.

Optimal technical scheme 30. is according to the tablet of any one in optimal technical scheme 1 to 29, wherein said diluent B 1 and/or diluent B 2 are selected from Umami flavor peptides, short chain glutamic acid polypeptide, Curculin, thaumatin, mabinlin, monellin, Mai Ruo Kelin, and their combination or mixture.

Optimal technical scheme 31. is according to the tablet of any one in optimal technical scheme 1 to 30, wherein said diluent B 1 and/or diluent B 2 are selected from lactose, mannitol, glucose, sucrose, xylitol or their combination, and described fusible saccharide D3 and/or medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from Sorbitol, oligosaccharide or their combination.

Optimal technical scheme 32. is according to the tablet of any one in optimal technical scheme 1 to 31, wherein said diluent B 1 and/or diluent B 2 are selected from lactose, mannitol, glucose, sucrose, xylitol or their combination, and described fusible saccharide D3 and/or medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from Sorbitol, maltose, maltose alcohol or their combination.

Optimal technical scheme 33. is according to the tablet of any one in optimal technical scheme 1 to 32, wherein said diluent B 1 and/or diluent B 2 are selected from lactose, mannitol or their combination, and described fusible saccharide D3 and/or medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from maltose, maltose alcohol or their combination.

Optimal technical scheme 34. is according to the tablet of any one in optimal technical scheme 1 to 33, and the more described fusible binding agent D1 of the fusing point of wherein said active components A 2 and/or the described fusible outer fusing point that covers thing D3 are high.

Optimal technical scheme 35. is according to the tablet of any one in optimal technical scheme 1 to 34, and the fusing point of wherein said fusible surfactant D 1 and/or fusible medicinal lipid additive D2 and/or fusible saccharide D3 is 40 to 120 ℃ (preferably 45 to 100 ℃).

Optimal technical scheme 36. is according to the tablet of any one in optimal technical scheme 1 to 35, the fusing point of wherein said fusible lipophilic surfactant D11 or fusible medicinal lipid additive D21 is 40 to 150 ℃ (preferably 45 to 120 ℃, more preferably 50 or 60 or 70 or 80 to 120 ℃).

Optimal technical scheme 37. is according to the tablet of any one in optimal technical scheme 1 to 36, and the more described diluent of fusing point of wherein said fusible surfactant D 1 and/or fusible medicinal lipid additive D2 and/or fusible saccharide D3 and/or fusible lipophilic surfactant D11 or fusible medicinal lipid additive D21 and/or the fusing point of described active component at least hang down 20 ℃.

Optimal technical scheme 38. is according to the tablet of any one in optimal technical scheme 1 to 37, the fusing point of the fusible surfactant D 1 in the more described fusible adhesion agent C1-1 of the fusing point of the medical additive E1 in wherein said fusible adhesion agent C1-1 at least high 20 ℃ (more preferably high 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent and/or described active component (more preferably low 20 ℃); And/or

The fusing point of fusible medicinal lipid additive D2 in the more described fusible adhesion agent C1-2 of the fusing point of surfactant E2 in described fusible adhesion agent C1-2 at least high 20 ℃ (more preferably high 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent and/or described active component (more preferably low 20 ℃); And/or

The fusing point of fusible saccharide D3 in the more described fusible adhesion agent C1-5 of the fusing point of medical additive E2 in described fusible adhesion agent C1-5 is at least high 10 ℃ (preferably high 20 ℃, more preferably high 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent and/or described active component (more preferably low 20 ℃); And/or

The more described fusible outer fusing point that covers thing D1 of medical additive E3 in described fusible adhesion agent C1-6 or the fusing point of core core 1 is at least high 10 ℃ (preferably high 20 ℃, more preferably high 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent and/or described active component (more preferably low 20 ℃); And/or

The more described fusible outer fusing point that covers thing D2 of medical additive E4 in described fusible adhesion agent C1-7 or the fusing point of core core 2 is at least high 10 ℃ (preferably high 20 ℃, more preferably high 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent and/or described active component (more preferably low 20 ℃).

Optimal technical scheme 39. is according to the tablet of any one in optimal technical scheme 1 to 38, at least low 10 ℃ (preferably low 20 ℃ of the fusing points of the more described active components A 2 of fusing point of the fusible binding agent D1 in wherein said fusible adhesion agent C2-1, more preferably low 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent B 2 (preferably low 20 ℃, more preferably low 30 ℃); And/or

Fusible outer in described fusible adhesion agent C2-2 covers at least low 10 ℃ (preferably low 20 ℃ of the fusing points of the more described active components A 2 of fusing point of thing D3 or core core 3, more preferably low 30 ℃), and/or at least low 10 ℃ of the fusing points of more described diluent B 2 (preferably low 20 ℃, more preferably low 30 ℃).

Optimal technical scheme 40. is according to the tablet of any one in optimal technical scheme 1 to 39, wherein said surfactant is selected from the esters that polyalcohols and the natural and/or oil that is hydrogenated or oil-soluble vitamins generate, and polyalcohols wherein is selected from Polyethylene Glycol that glycerol, propylene glycol, ethylene glycol, Sorbitol, tetramethylolmethane, the degree of polymerization are 2 to 200 and their combination.

Optimal technical scheme 41. is according to the tablet of optimal technical scheme 40, and wherein said natural and/or oil or oil-soluble vitamins that be hydrogenated are selected from Oleum Ricini, the Oleum Ricini be hydrogenated, vitamin A, vitamin D, vitamin E, vitamin K, edible vegetable oil, the edible vegetable oil be hydrogenated and their combination.

Optimal technical scheme 42. is according to the tablet of optimal technical scheme 40, and wherein said edible vegetable oil is selected from Semen Maydis oil, olive oil, Oleum Arachidis hypogaeae semen, palmolive core oil, almond oil, Semen Juglandis oil, Oleum Cocois, Petiolus Trachycarpi oil, Oleum Glycines and wheat germ oil and their combination.

Optimal technical scheme 43. is according to the tablet of optimal technical scheme 40, and the wherein said edible vegetable oil be hydrogenated is selected from the Semen Maydis oil be hydrogenated, the olive oil be hydrogenated, the Oleum Arachidis hypogaeae semen be hydrogenated, the palmolive core oil be hydrogenated, the almond oil be hydrogenated, the Semen Juglandis oil be hydrogenated, the Oleum Cocois be hydrogenated, the Petiolus Trachycarpi oil be hydrogenated, the Oleum Glycines be hydrogenated and the wheat germ oil be hydrogenated and their combination.

Optimal technical scheme 44. is according to the tablet of any one in optimal technical scheme 1 to 43, and wherein said surfactant D 1 and/or described surfactant E2 are selected from hydrophilic surfactant.

Optimal technical scheme 45. is according to the tablet of any one in optimal technical scheme 1 to 44, and wherein said surfactant E2 is selected from the surfactant of fusing point higher than described fusible medicinal lipid additive D2 at least 10 ℃ (preferably 20 ℃).

Optimal technical scheme 46. is according to the tablet of any one in optimal technical scheme 1 to 45, the fusing point of the more described diluent B 1 of the fusing point of wherein said solid dispersion (I～IX) and/or described solid coating (I～VI) and/or B2 and/or described active components A 1 and/or A2 is low (preferably low 10 ℃, more preferably low 20 ℃, low 30 ℃ best).

Optimal technical scheme 47. is according to the tablet of any one in optimal technical scheme 1 to 46, and wherein said medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from the described diluent of part or all of consumption.

Optimal technical scheme 48. is according to the tablet of any one in optimal technical scheme 1 to 47, and wherein said medical additive E1 and/or medical additive E3 are selected from hydrophilic medical additive (more preferably water miscible medical additive).

Optimal technical scheme 49. is according to the tablet of any one in optimal technical scheme 1 to 48, wherein said medical additive E1 and/or medical additive E2 and/or E3 and/or E4 are selected from microfibre, the length-width ratio of this microfibre is 10:1～500:1, and its mean diameter is not more than 1 μ m.

Optimal technical scheme 50. is according to the tablet of any one in optimal technical scheme 1 to 49, and wherein said medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from disintegrating agent and/or can not form the sweller of strong gel.

Optimal technical scheme 51. is according to the tablet of any one in optimal technical scheme 1 to 50, and wherein said medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from stearyl lactylic acid salt, caproate, caprylate, caprate, laruate, myristate, palmitate, the Petiolus Trachycarpi oil hydrochlorate, oleate, ricinoleate, linoleate, linolenate, stearate, lauryl sulfate, tetradecyl sulfate, the lauryl sarcosinate, the dioctyl sulfosuccinate, cholate, taurocholate, glycocholate, dexycholate, taurodeoxycholate, glycodeoxycholate, ursodeoxycholate, chenodesoxy cholate, cattle sulphur chenodesoxy cholate, the glyceryl chenodesoxy cholate, CHOLYLSARCOSINE salt, N-formyl taurocholate, two myristoyl lecithin, lecithin, hydrolecithin, lysophosphatidylcholine, cuorin, sphingomyelins, PHOSPHATIDYL ETHANOLAMINE, phosphatidic acid, the phosphatidyl glycerol, Phosphatidylserine, succinyl monoglyceride salt, stearoyl propylene glycol succinate, single/or diacetyl group tartrate monoglyceride and diester, citrate monoglyceride diester, glycerol lactate fatty acid ester, ten to the octadecanoyl lactate, stearoyl-2 lactoyl salt, alginate, and composition thereof, above-mentioned salt is selected from sodium salt, or potassium salt, or ammonium salt.

Optimal technical scheme 52. is according to the tablet of any one party case in optimal technical scheme 18 to 21 or 50, and wherein said sweller is selected from the following polymers that degree of neutralization that weight average molecular weight is greater than 100000 acidity and/or basic functionality is 30～100 % by mole: acrylate copolymer, poly-carbon number is C1～C4 alkyl acrylic, poly-hydroxyl carbon number is C1～C4 alkyl acrylic, acrylic acid-acrylate polymer, polyvinyl alcohol-acrylic block copolymers, the starch graft acrylic acid polymer, the cellulose graft acrylate copolymer, humic acids, polycarbophil, alginic acid, poly-aspartate, polyglutamic acid, poly-aspartic acid and poly-glutamic acid, polyamine or the poly-imines of mixing of mixing, polymine, polypropylene amine, polyethylenepolyamine, the polypropylene carbon number is C1～C4 alkylamine, poly-carbon number is C1～C4 alkyl allylamine, poly-carbon number is that C1～C4 alkyl propylene carbon number is C1～C4 alkylamine, poly-hydroxyl carbon number is C1～C4 alkyl allylamine, poly-hydroxyl carbon number is that C1～C4 alkyl propylene atomic number is C1～C4 alkylamine, aminopolysaccharide, chitin, chitosan, poly-asparagine, polyglutamine, polylysine, poly arginine, the poly-lysine that mixes mixes arginine and their mixture with gathering.

Optimal technical scheme 53. is according to the tablet of optimal technical scheme 52, and the acidity of wherein said polymer and/or the degree of neutralization of basic functionality are 40～100 % by mole (more preferably 50～100 % by mole).

Optimal technical scheme 54. is according to the tablet of any one in optimal technical scheme 1 to 53, and wherein said solid dispersion I～VI also contains active component.

Optimal technical scheme 55. is according to the tablet of any one in optimal technical scheme 1 to 54, wherein said solid coating particle and/or described solid dispersion particle have " shell-core structure ", in above-mentioned " shell-core structure ", " shell " can coat in " core " and/or " shell " wholly or in part can contain one or more " core ".

Optimal technical scheme 56. is according to the tablet of any one in optimal technical scheme 1 to 55, wherein said solid coating particle and/or described solid dispersion particle have " shell-core structure ", in above-mentioned " shell-core structure ", can also contain the component that comprises " shell " in " core " in less " core " and/or " shell " or less " shell-core structure " in " shell ".

Optimal technical scheme 57. is according to the tablet of any one in optimal technical scheme 1 to 56, wherein said solid coating particle and/or described solid dispersion particle have " shell-core structure ", and above-mentioned " shell-core structure " has shell/shell/three layers of cores, shell/core/three layers, shell or shell/core/shell/core four-layer structure.

Optimal technical scheme 58. is according to the tablet of any one in optimal technical scheme 1 to 57, wherein said solid coating particle and/or described solid dispersion particle have " shell-core structure ", in above-mentioned " shell-core structure ", " shell " preferably accounts for 0.5～50% of total volume.

Optimal technical scheme 59., according to the tablet of any one in optimal technical scheme 1 to 58, wherein also includes at least one medical additive.

Optimal technical scheme 60. is according to the tablet of any one in optimal technical scheme 1 to 59, the consumption of wherein said active components A 1 is 0.001%(wt./wt.) to 70%(wt./wt.) (more preferably 0.001%(wt./wt.) to 50%(wt./wt.), 0.001%(wt./wt. most preferably) to 50%(wt./wt.)), the consumption of described diluent B 1 is 5%(wt./wt.) to 95%(wt./wt.) (more preferably 10%(wt./wt.) to 90%(wt./wt.), 20%(wt./wt. most preferably) to 80%(wt./wt.)), the consumption of described fusible adhesion agent C1 is 1%(wt./wt.) to 70%(wt./wt.) (more preferably 5%(wt./wt.) to 50%(wt./wt.), 8%(wt./wt. most preferably) to 30%(wt./wt.)), above percentage by weight is based on the gross weight of tablet, and/or

The consumption of described diluent B 2 is 5%(wt./wt.) to 99%(wt./wt.) (more preferably 10%(wt./wt.) to 95%(wt./wt.), 30%(wt./wt. most preferably) to 92%(wt./wt.)), the consumption of described fusible adhesion agent C2 is 1%(wt./wt.) to 95%(wt./wt.) (more preferably 5%(wt./wt.) to 90%(wt./wt.), 8%(wt./wt. most preferably) to 70%(wt./wt.)), above percentage by weight is based on the gross weight of tablet.

Optimal technical scheme 61. is according to the tablet of any one in optimal technical scheme 1 to 60, medical additive E1 in wherein said fusible adhesion agent C1-1, and/or the surfactant E2 in described fusible adhesion agent C1-2, and/or the medical additive E2 in described fusible adhesion agent C1-5, and/or the medical additive E3 in described fusible adhesion agent C1-6 or described core core 1, and/or the medical additive E4 in described fusible adhesion agent C1-7 or described core core 2, and/or the active components A 2 in described fusible adhesion agent C2-1, and/or the ratio that the active components A 2 in described fusible adhesion agent C2-2 or described core core 3 account in the fusible adhesion agent at its place is 0.05(wt./wt.) to 0.95(wt./wt.) (preferably 0.15(wt./wt.) to 0.85(wt./wt.), more preferably 0.25(wt./wt.) to 0.75(wt./wt.), 0.35(wt./wt. most preferably) to 0.65(wt./wt.)), surfactant D 1 in described fusible adhesion agent C1-1, and/or the medicinal lipid additive D2 in described fusible adhesion agent C1-2, and/or the fusible saccharide D3 in described fusible adhesion agent C1-5, and/or the fusible outer thing D1 that covers in described fusible adhesion agent C1-6, and/or the fusible outer thing D2 that covers in described fusible adhesion agent C1-7, and/or the fusible binding agent D1 in described fusible adhesion agent C2-1, and/or fusible outer in described fusible adhesion agent C2-2 to cover the ratio that thing D3 accounts in the fusible adhesion agent at its place be 0.05(wt./wt.) to 0.95(wt./wt.) (preferably 0.15(wt./wt.) to 0.85(wt./wt.), more preferably 0.25(wt./wt.) to 0.75(wt./wt.), 0.35(wt./wt. most preferably) to 0.65(wt./wt.)), above part by weight all is based on the gross weight of fusible adhesion agent, and/or

Described fusible adhesion agent C1-3, and/or the ratio that the hydrophilic surfactant E21 in fusible adhesion agent C1-4 accounts in the fusible adhesion agent at its place is 0.01(wt./wt.) to 0.20(wt./wt.) (preferably 0.02(wt./wt.) to 0.15(wt./wt.), more preferably 0.03(wt./wt.) to 0.10(wt./wt.), 0.03(wt./wt. most preferably) to 0.10(wt./wt.)), lipophilic surfactant D11 in described fusible adhesion agent C1-3, and/or the ratio that in fusible adhesion agent C1-4, medicinal lipid additive D21 accounts in the fusible adhesion agent at its place is 0.80(wt./wt.) to 0.99(wt./wt.) (preferably 0.85(wt./wt.) to 0.98(wt./wt.), more preferably 0.90(wt./wt.) to 0.97(wt./wt.), 0.90(wt./wt. most preferably) to 0.97(wt./wt.)), above part by weight all is based on the gross weight of fusible adhesion agent.

Optimal technical scheme 62. is according to the tablet of any one in optimal technical scheme 2 to 60, medical additive E3 in wherein said fusible adhesion agent C1-10 or described core core 4, and/or the medical additive E4 in described fusible adhesion agent C1-11 or described core core 5, and/or the active components A 2 in described fusible adhesion agent C2-3, and/or the ratio that the active components A 2 in described fusible adhesion agent C2-4 or described core core 6 account in the fusible adhesion agent at its place is 0.05(wt./wt.) to 0.95(wt./wt.) (preferably 0.15(wt./wt.) to 0.85(wt./wt.), more preferably 0.25(wt./wt.) to 0.75(wt./wt.), 0.35(wt./wt. most preferably) to 0.65(wt./wt.)), the fusible outer thing D4 that covers in described fusible adhesion agent C1-10, and/or the fusible outer thing D5 that covers in described fusible adhesion agent C1-11, and/or the fusible binding agent D2 in described fusible adhesion agent C2-3, and/or fusible outer in described fusible adhesion agent C2-3 to cover the ratio that thing D6 accounts in the fusible adhesion agent at its place be 0.05(wt./wt.) to 0.95(wt./wt.) (preferably 0.15(wt./wt.) to 0.85(wt./wt.), more preferably 0.25(wt./wt.) to 0.75(wt./wt.), 0.35(wt./wt. most preferably) to 0.65(wt./wt.)), above part by weight all is based on the gross weight of fusible adhesion agent.

Optimal technical scheme 63. is according to the tablet of any one in optimal technical scheme 2 to 60, wherein said medical additive E1 and/or described surfactant E2 and/or described medical additive E2 are in the solid dispersion solid dispersion (I at its place, and/or II, and/or V) and/or the ratio accounted in fusible binding agent D2 be 0.005(wt./wt.) to 0.995(wt./wt.) (preferably 0.05(wt./wt.) to 0.95(wt./wt.), 0.15(wt./wt. more preferably) to 0.85(wt./wt.), more preferably 0.25(wt./wt.) to 0.75(wt./wt.), 0.35(wt./wt. most preferably) to 0.65(wt./wt.)), described fusible surfactant D 1 and/or described fusible medicinal lipid additive D2 and/or described fusible saccharide D3 are in the solid dispersion solid dispersion (I at its place, and/or II, and/or V) and/or the ratio accounted in fusible binding agent D2 be 0.005(wt./wt.) to 0.995(wt./wt.) (preferably 0.05(wt./wt.) to 0.95(wt./wt.), 0.15(wt./wt. more preferably) to 0.85(wt./wt.), more preferably 0.25(wt./wt.) to 0.75(wt./wt.), 0.35(wt./wt. most preferably) to 0.65(wt./wt.)), above part by weight all is based on the gross weight of this solid dispersion and/or fusible binding agent, and/or

Described hydrophilic surfactant E21 is in the solid dispersion (III at its place, and/or IV) and/or the ratio accounted in fusible binding agent D2 be 0.005(wt./wt.) to 0.25(wt./wt.) (preferably 0.01(wt./wt.) to 0.20(wt./wt.), 0.02(wt./wt. more preferably) to 0.15(wt./wt.), more preferably 0.03(wt./wt.) to 0.10(wt./wt.), 0.03(wt./wt. most preferably) to 0.10(wt./wt.)), described fusible lipophilic surfactant D11 and/or described medicinal lipid additive D21 are in the solid dispersion (III at its place, and/or IV) and/or the ratio accounted in fusible binding agent D2 be 0.75(wt./wt.) to 0.995(wt./wt.) (preferably 0.80(wt./wt.) to 0.99(wt./wt.), 0.85(wt./wt. more preferably) to 0.98(wt./wt.), more preferably 0.90(wt./wt.) to 0.97(wt./wt.), 0.90(wt./wt. most preferably) to 0.97(wt./wt.)), above part by weight all is based on the gross weight of this solid dispersion and/or fusible binding agent.

Optimal technical scheme 64. is according to the tablet of any one in optimal technical scheme 1 to 63, the balance meltage of wherein said active components A 2 in water (25 ℃ of temperature) (dissolubility in water at 25 ℃ of temperature) lower than 33mg/1ml (solvency/water) (preferably lower than 10mg/1ml (solvency/water), more preferably lower than 1mg/1ml (solvency/water), best lower than 0.1mg/1ml (solvency/water)).

The tablet the present invention relates to compare prepared by prior art tablet there are at least following one or more advantages:

-stronger mechanical performance, safeguard the integrity of tablet, improve accuracy and the ease of use of divided dose, prevent from or reduce tablet trickle or large crack, wearing and tearing, fragmentation occurring in the processes such as production, transportation, prevent that unsettled material is exposed in hostile environment again;-better drug-eluting performance, not only be conducive to the rapid stripping of medication medication preferably of contained water solublity, and be more conducive to the rapid stripping of the poor medication medication of contained water solublity;-better weatherability, can be at the higher temperature of tolerance in summer, and under higher temperature, tablet can not soften, and its tablet strength and disintegration time etc. can be not therefore and change (with respect to surfactant or the lipid additive of low melting point) yet;-better hydrophilic or drug dissolution, have dissolving preferably or dispersion or disintegrate or Release Performance (with respect to the medicine of lipid or lipotropy additive or large particle size dispersion);-better safety, low toxic and side effects, the surfactant of less consumption and can obtain above-mentioned advantage (with respect to the surfactant of higher proportion consumption) preferably;-better technique operability or Yi Hangxing, can produce in relatively low temperature or without under wet environment, energy-conservation, reduce production costs, be conducive to improve tablet (unsettled composition) stability (with respect to lipid additive or surfactant or the saccharide binding agent of higher melt).

Preferred embodiment

Below non-selective embodiment further described the preferred embodiment in the scope of the invention.These embodiment also can have many variations within the scope of the invention.

Embodiment 1 and reference examples thereof

[method for making] gets component 3～4, and heat fused mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 10nm); Above-mentioned powder mixes with the component 1～2,5～9 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.18t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～9, mix, cross 100 mesh sieves (levigate in case of necessity), mix, afterwards (other) by embodiment, with legal system, standby (illustrate: each " (other) afterwards " of reaching hereinafter refer to that (corresponding) content is compared with above (content as middle as " embodiment 1 method for making " herein) herein, take " this " as boundary (as " mixing " herein), content before boundary just be described (as herein " get component 1～9, mix, cross 100 mesh sieves (levigate in case of necessity) "), content behind boundary is identical (as be its content for " with the about 0.18t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp herein because of the content with corresponding above, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 5 minutes, being cooled to room temperature gets final product ", do not comprise different content before boundary), for simplicity, do not repeat this identical content.Hereinafter because of implication herewith, no longer explained).

Embodiment 2 and reference examples thereof

[embodiment 2-1 method for making] got component 1～3 and is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Get component 4～5, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder 2 (the dispersate mean diameter is 70～100nm approximately); Above-mentioned powder 1,2 mixes, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 2-2 method for making] got component 1～3 and is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Get component 4 and be dissolved in appropriate ethanol, add and be micronized to the approximately component 5 of 90～100 μ m of mean diameter, the dispersion liquid spray drying obtains solid coating powder 2; Afterwards (other) by embodiment 2-1 with method method for making (filling a prescription constant).

[reference examples method for making] component 1～3 is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Get component 4～5 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, mix, (other) are standby with legal system by embodiment afterwards.

Embodiment 3 and reference examples thereof

[embodiment 3-1 method for making] gets component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 100nm); Above-mentioned powder mixes with the component 1～2,5～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.28t/ pestle of tabletting pressure tabletting (sheet hardness 2.4kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 8 minutes, is cooled to room temperature and gets final product.

[embodiment 3-2 method for making] got component 3 and is dissolved in appropriate ethanol, adds component 4, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; (other) press embodiment 3-1 with the method method for making afterwards.

[embodiment 3-3 method for making] got component 4 and is dissolved in suitable quantity of water, under 0 ℃ of ambient temperature, be micronized to approximately component 3 spray coatings of 5～25 μ m of mean diameter with this solution to what suspend, afterwards the coated granule of above-mentioned suspension is sprayed into to liquid nitrogen or carbon dioxide solidifies coatings, shift subsequently this cured granulate to frozen drying equipment, reach dry (moisture in making coatings directly transfers gaseous state from solid-state to without liquid state) above-mentioned granule under vacuum state in temperature below 0 ℃ and obtain solid coating powder; Above-mentioned powder mixes with the component 1～2,5～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.28t/ pestle of tabletting pressure tabletting (sheet hardness 2.4kp, n=5), sheet is heated to 125 ℃ of temperature and is incubated 2 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 4 and reference examples thereof

[embodiment 4-1 method for making] gets component 4～5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder 1 (the dispersate mean diameter is not more than 100nm); Component 1～3 is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 2; Above-mentioned powder 1,2 mixes with the component 6～7 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 4-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 5, makes it to be micronized to approximately 70～100 μ m of mean diameter, and this dispersion liquid of spray drying obtains solid coating powder 1; Afterwards (other) by embodiment 4-1 with method method for making (filling a prescription constant).

[reference examples method for making] got component 1～3 and is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder; Get component 4～7 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned dispersion (/ body) powder, mix, (other) are standby with legal system by embodiment afterwards.

Embodiment 5 and reference examples thereof

The component 2 of 1,3 and three minutes amounts of [method for making] component is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Component 4～5 is dissolved in the aqueous solution of appropriate 80% ethanol altogether, in fluid bed, with above-mentioned solution, component 2 spray dryinges of the surplus that suspends is obtained to solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder 2; Above-mentioned powder 1,2 mixes, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

The component 2 of 1,3 and three minutes amounts of [reference examples method for making] component is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Get the component 2 of component 4～5 and surplus and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, mix, (other) are standby with legal system by embodiment afterwards.

Embodiment 6 and reference examples thereof

[embodiment 6-1,3 method for makings] get the component 5 that is micronized to 500 orders (mean diameter is 25 μ m approximately), add the component 4 melted, and mix, cooling, are crushed to 100～120 orders, obtain solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～3,6～9 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.6t/ pestle of tabletting pressure tabletting (sheet hardness 4kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 9 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 6-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; (other) press embodiment 6-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～9, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 6-1 and reference examples, embodiment 6-2 and reference examples thereof, embodiment 6-3 and reference examples thereof, except component 5, be followed successively by sodium caseinate, lauryl sulphate acid potassium, N α-lauroyl arginine ethyl ester hydrochlorate, other are all identical.

Embodiment 7 and reference examples thereof

[embodiment 7-1 method for making] component 3,4 heat fused, add the saturated aqueous solution of component 1, mixes, and treats after moisture evaporation coolingly, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 100nm); Above-mentioned powder mixes with the component 5～6 of crossing 100 mesh sieves (levigate in case of necessity), adds component 2,7, mixes, and in pack into suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 7-2 method for making] got component 3 and is dissolved in suitable quantity of water, adds component 4, and heating makes it fusing, and strong stirring makes it to be dispersed to the about 100nm of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,5～6 of crossing 100 mesh sieves (levigate in case of necessity), adds component 2,7, mix, afterwards (other) by embodiment 7-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1,3～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), add component 2,7 mix after (other) standby with legal system by embodiment.

Embodiment 8 and reference examples thereof

[embodiment 8-1 method for making] component 1,4～6 is dissolved in appropriate 85% alcohol water blend altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 2, mixes, and in pack into suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 8-2 method for making] got component 4,6 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, and in high-speed stirred, to its emulsifying, in emulsion, the mean diameter of particle is not more than 100nm, and emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 2, mix, afterwards (other) by embodiment 8-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1,3～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), add component 2 mix after (other) standby with legal system by embodiment.

Embodiment 9 and reference examples thereof

[embodiment 9-1 method for making] gets group 6 heat fused, adds component 7, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～5,8 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 0.11t/ pestle of tabletting pressure tabletting (sheet hardness 0.08kp, n=5), sheet is heated to temperature 60 C again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 9-2 method for making] got component 6,7 and is dissolved in appropriate ethanol, adds micronized component 1 (mean diameter is 5～25 μ m approximately), and the dispersion liquid spray drying obtains solid coating powder; It is even that above-mentioned powder and the component 2,3,4,5,8 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, and (other) press embodiment 9-1 with the method method for making afterwards.

[embodiment 9-3 method for making] gets component 6,7 heat fused, adds micronized component 2 (mean diameter is 5～25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; It is even that above-mentioned powder and the component 1,3,4,5,8 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, and (other) press embodiment 9-1 with the method method for making afterwards.

[embodiment 9-4 method for making] gets group 6 heat fused, adds micronized component 7 (mean diameter is 1～5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～5,8 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 0.11t/ pestle of tabletting pressure tabletting (sheet hardness 0.08kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 9-1 and reference examples, embodiment 9-2 and reference examples thereof, embodiment 9-3 and reference examples thereof, embodiment 9-4 and reference examples thereof, except component 7, be followed successively by PEG200, PEG200, PEG200, tetradecylic acid sodium lactate, other are all identical.

Embodiment 10 and reference examples thereof

[embodiment 10-1 method for making] component 1,3～4 is dissolved in altogether appropriate hot ethanol and obtains solution, in fluid bed, with above-mentioned solution, micronized component 2 (mean diameter is 50～100 μ m approximately) spray drying of 50% amount that suspends is obtained to solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; The component 2 of above-mentioned powder and surplus is mixed to even, and with the about 0.17t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 10-2 method for making] gets component 3,4 heat fused, and the component 1 that adds appropriate hot ethanol to dissolve, mix, and flings to ethanol, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder and component 2 are mixed to even, afterwards (other) by embodiment 10-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 11 and reference examples thereof

[embodiment 11-1 method for making] gets group 5 heat fused, adds component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 11-2 method for making] gets group 5 heat fused, adds component 4, adds the micronized component 2 (mean diameter is 5～25 μ m approximately) of 20% amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, after mixing (other) by embodiment 11-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 12 and reference examples thereof

[embodiment 12-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,3,7 of crossing 100 mesh sieves (levigate in case of necessity), add component 6, mix, with the about 0.5t/ pestle of tabletting pressure tabletting (sheet hardness 3.5kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 12-2 method for making] got component 5 and is dissolved in suitable quantity of water, under 0 ℃ of ambient temperature, be micronized to approximately component 4 spray coatings of 50～100 μ m of mean diameter with this solution to what suspend, afterwards the coated granule of above-mentioned suspension is sprayed into to liquid nitrogen or carbon dioxide solidifies the coatings of this granule, shift subsequently this cured granulate to frozen drying equipment, reach dry (moisture in making coatings directly transfers gaseous state from solid-state to without liquid state) above-mentioned granule under vacuum state in temperature below 0 ℃ and obtain solid coating powder; Above-mentioned powder mixes with the component 1,2,3,7 of crossing 100 mesh sieves (levigate in case of necessity), add component 6, mix, with the about 0.5t/ pestle of tabletting pressure tabletting (sheet hardness 3.5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 12-3 method for making] component 4,5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; (above-mentioned powder mixes with the component 1,2,3,7 of crossing 100 mesh sieves (levigate in case of necessity) afterwards, add component 6, mix, with the about 0.5t/ pestle of tabletting pressure tabletting (sheet hardness 3.5kp, n=5), sheet is heated to 118 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～5,7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 12-1 and reference examples, embodiment 12-2 and reference examples thereof, embodiment 12-3 and reference examples thereof, except component 4 is followed successively by poloxamer338, poloxamer338, glucuronic acid, other are all identical.

Embodiment 13 and reference examples thereof

[embodiment 13-1,3 method for makings] get component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), mix, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 140～170 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 13-2,4 method for makings] are got component 5 and are dissolved in suitable quantity of water, with this solution to be micronized to mean diameter approximately component 4 spray coatings of 60～100 μ m obtain solid coating powder; (other) press embodiment 13-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 13-1 and reference examples, embodiment 13-2 and reference examples thereof, embodiment 13-3 and reference examples thereof, embodiment 13-4 and reference examples (formula) thereof, except component 4, be followed successively by lactitol, lactitol, 2-HP-β-CD, 2-HP-β-CD, other are all identical.

Embodiment 14 and reference examples thereof

[method for making] component 1～3 is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 4,5, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 2; Pack into after above-mentioned powder 1,2 mixes in suitable bubble eye or tablet mould, then be heated to 55 ℃ of temperature and be incubated 5 minutes, be cooled to room temperature and get final product.

[reference examples method for making] component 1～3 is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 4～5 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, after mixing, (other) are standby with legal system by embodiment.

Embodiment 15 and reference examples thereof

[embodiment 15-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 8 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 15-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 100 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 15-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 16 and reference examples thereof

[method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 17 and reference examples thereof

[embodiment 17-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 17-2,3 method for makings] are got component 5 and are dissolved in suitable quantity of water, add component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 100nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; (other) press embodiment 17-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 17-1 and reference examples, embodiment 17-2 and reference examples thereof, embodiment 17-3 and reference examples thereof, except component 5, be followed successively by lauryl betaine, lauryl betaine, N-cetyl acyl Glycine sodium, other are all identical.

Embodiment 18 and reference examples thereof

[embodiment 18-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 18-2 method for making] got component 4,5 and is dissolved in appropriate ethanol, adds the micronized component 2 (mean diameter is 5～25 μ m approximately) of half amount, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 18-1 with method method for making (filling a prescription constant).

[embodiment 18-3 method for making] gets component 4,5 heat fused, adds component 1 (mean diameter is 1～5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; It is even that above-mentioned powder and the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 18-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 19 and reference examples thereof

[embodiment 19-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3,6 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 6 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 19-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 5 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 19-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 20 and reference examples thereof

Simulsol165 (self emulsifying glyceride, tristerin+PEG100 stearic acid, mp, 55-59 ℃)

[method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to temperature 70 C and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～2,4～7, component 3 is replaced by the mixed in equal amounts powder of composition and ratio identical with Simulsol165 (tristerin and PEG100 stearic acid etc.), mix, cross 100 mesh sieves (levigate in case of necessity), cross 100 mesh sieves (levigate in case of necessity), after mixing, (other) are standby with legal system by embodiment.

Embodiment 21 and reference examples thereof

[embodiment 21-1～3 method for makings] get the aqueous solution that component 3,4 is dissolved in appropriate 60% ethanol of temperature 70 C, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder mixes with the component 1,2,5 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 5 volatilizations are complete, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 21-1 and reference examples, embodiment 21-2 and reference examples thereof, embodiment 21-3 and reference examples (formula) thereof, except component 4, be followed successively by 2-HP-BETA-CD, ALANINE, the sweet peptide of Soviet Union's first, other are all identical.

Embodiment 22 and reference examples thereof

[embodiment 22-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to temperature 70 C again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 22-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, about 0.1～1 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; (other) press embodiment 22-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 22-1 and reference examples, embodiment 22-2 and reference examples thereof, except component 5 is followed successively by monocaprin, octadecyl trimethyl ammonium chloride, other are all identical.

Embodiment 23 and reference examples thereof

[embodiment 23-1～3 method for makings] get in the water of the temperature 70 C that component 5 is dissolved in 20 times of its weight at least; Get in 95% ethanol that component 4 is incorporated in 20 times of its weight at least, heating makes to melt, and stirs it is uniformly dispersed; Be mixed rear spraying or the lyophilization of above-mentioned two liquid obtains solid coating powder; Above-mentioned powder mixes with the component 1～3,6～7,9 of crossing 100 mesh sieves (levigate in case of necessity), add component 8, mix, with the about 5t/ pestle of tabletting pressure tabletting (sheet hardness 4kp, n=5), sheet is heated to temperature 70 C again and is incubated at least 5 hours under vacuum, until component 9 volatilizations are complete, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～9, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 23-1 and reference examples, embodiment 23-2 and reference examples thereof, embodiment 23-3 and reference examples (formula) thereof, except component 5 is followed successively by malt-base-alpha-cyclodextrin, sodium glutamate, alanyl glutamine, other are all identical.

Embodiment 24 and reference examples thereof

[embodiment 24-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 24-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, makes it to be micronized to approximately 5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 24-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 25 and reference examples thereof

[embodiment 25-1 method for making] component 4,5, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; The component 2 of component 1 and two minutes amounts is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 2; Above-mentioned powder 1,2 mixes with component 2 and the component 3 of crossing the surplus of 100 mesh sieves (levigate in case of necessity), mix, with the about 1.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.8kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 25-2 method for making] got component 5 and is dissolved in appropriate containing in the water of 60% ethanol, adds component 4, makes it to be micronized to approximately 1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder 1; (other) press embodiment 25-1 with the method method for making afterwards.

[embodiment 25-3 method for making] got component 5 and is dissolved in appropriate water, adds the component 4 of heat fused, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; The component 2 of component 1 and two minutes amounts is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 2; Above-mentioned powder 1,2 mixes with component 2 and the component 3 of crossing the surplus of 100 mesh sieves (levigate in case of necessity), mix, with the about 1.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.8kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

The component 2 of [reference examples method for making] component 1 and two minutes amounts is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned dispersion (/ body) powder mixes with component 2 and the component 3～5 of crossing the surplus of 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 25-1 and reference examples, embodiment 25-2 and reference examples thereof, embodiment 25-3 and reference examples thereof, except component 5, be followed successively by four sad season the eleventh of the twelve Earthly Branches tetrol ester, four sad season the eleventh of the twelve Earthly Branches tetrol ester, stearoyl propylene glycol ammonium succinates, other are all identical.

Embodiment 26 and reference examples thereof

[embodiment 26-1 method for making] gets component 3, heat fused, the component 1 that adds component 4 and dissolve by proper amount of acetone, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,5～9 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 26-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 3, and heating makes fusing, and in high-speed stirred, to its emulsifying, in emulsion, the mean diameter of particle is not more than 100nm, and emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,2,5～9 of crossing 100 mesh sieves (levigate in case of necessity), after mixing (other) by embodiment 26-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～9, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 27 and reference examples thereof

[embodiment 27-1 method for making] gets component 4 heat fused, adds component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 27-2 method for making] gets component 4 heat fused, adds component 5, adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of 20% amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 27-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 28 and reference examples thereof

[embodiment 28-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 28-2 method for making] gets component 5 heat fused, adds micronized component 4 (mean diameter is 50～100 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; (other) press embodiment 28-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 28-1 and reference examples, embodiment 28-2 and reference examples thereof, except component 4, be followed successively by PEG1000, cattle sulphur chenodeoxy cholic acid, other are all identical.

Embodiment 29 and reference examples thereof

[method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 30 and reference examples thereof

[embodiment 30-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 30-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds and is micronized to the approximately component 5 of 20～30 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 30-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 31 and reference examples thereof

[embodiment 31-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 31-2,3 method for makings] are got component 4,5 and are dissolved in suitable quantity of water, the dry solid dispersion powder that obtains of solution spray; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), mix, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 120～140 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 31-1 and reference examples, embodiment 31-2 and reference examples thereof, embodiment 31-3 and reference examples (formula) thereof, except component 4, be followed successively by Polyox (WSR N-80), linoleic acid sodium, galactosamine, other are all identical.

Embodiment 32 and reference examples thereof

[embodiment 32-1 method for making] gets component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～2 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 98 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 32-2 method for making] got component 3 and is dissolved in appropriate ethanol, adds component 4, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 32-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 33 and reference examples thereof

[embodiment 33-1 method for making] gets component 4 heat fused, adds by appropriate 50% alcohol-soluble component 1, adds component 5, be heated to its fusing, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 140 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 33-2～5 method for makings] are got component 4 and are dissolved in appropriate ethanol, add component 5, make it micronization, wherein embodiment 33-2 to mean diameter approximately 5～25 μ m, embodiment 33-3 to mean diameter approximately 1～5 μ m, embodiment 33-4 to mean diameter, approximately 0.6～1 μ m, embodiment 33-5 are to about 50～100 μ m of mean diameter, the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, (other) press embodiment 33-1 with the method method for making.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 33-1 and reference examples, embodiment 33-2 and reference examples thereof, embodiment 33-3 and reference examples thereof, embodiment 33-4 and reference examples thereof, embodiment 33-5 and reference examples (formula) thereof, except component 5, be followed successively by maltose, maltose, gamma-cyclodextrin, L-threonine, glycyl proline dipeptides, other are all identical.

Embodiment 34 and reference examples thereof

[embodiment 34-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 1 μ m) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to temperature 70 C again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 34-2～5 method for makings] are got component 4 and are dissolved in appropriate ethanol, add component 5, make it micronization, wherein embodiment 34-2 to mean diameter approximately 80～100 μ m, embodiment 34-3 to mean diameter approximately 1～5 μ m, embodiment 34-4 to mean diameter, approximately 0.3～1 μ m, embodiment 34-5 are to about 5～25 μ m of mean diameter, the dispersion liquid spray drying obtains solid coating powder; (other) press embodiment 34-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 34-1 and reference examples, embodiment 34-2 and reference examples thereof, embodiment 34-3 and reference examples thereof, embodiment 34-4 and reference examples thereof, embodiment 34-5 and reference examples (formula) thereof, except component 5, be followed successively by sucrose, sucrose, H-Ala-His-OH dipeptides, L-glycine-L-Trp-L-Phe-D-Arg tetrapeptide hydrochlorate, glucosulfone base-alpha-cyclodextrin, other are all identical.

Embodiment 35 and reference examples thereof

[embodiment 35-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[embodiment 35-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds component 5, makes it to be micronized to approximately 100～900nm of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 35-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 36 and reference examples thereof

[method for making] gets component 3,4, and heat fused adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with component 2, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to temperature 70 C again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 37 and reference examples thereof

NIKKOL Nikkomulese41 (containing the O/W emulsifying agent of behenyl alcohol, Natrulon H-10 five stearates, stearoyl dilactic acid sodium, fusing point is between 65～75 ℃)

[method for making] component 1 and component 3 are dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,4～7 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] component 1 and component 3 are dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 2,4,6,7, component 5 is by component and proportional quantity and NIKKOL Nikkomulese41(behenyl alcohol, Natrulon H-10 five stearates, stearoyl dilactic acid sodium) physical mixture of identical equivalent replaces, mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, after mixing, (other) are standby with legal system by embodiment.

Embodiment 38 and reference examples thereof

[embodiment 38-1 method for making] gets component 4, heat fused, add component 5 to reach the component 1 that has been micronized to 6000～10000 orders (1～2 μ m), mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (component 5 dispersate mean diameters are not more than 500nm) powder; Above-mentioned powder mixes with the component 2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 126 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[embodiment 38-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, about 5～25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), after mixing (other) by embodiment 38-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 39 and reference examples thereof

[method for making] component 1 and component 3 are dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 4,5, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 2; Above-mentioned powder 1,2 mixes with component 2, adds component 6, mixes, and with the about 1.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.8kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1 and component 3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Above-mentioned powder 1 mixes with the component 2,4～5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) are standby with legal system by embodiment afterwards.

Embodiment 40 and reference examples thereof

(from RoquetteAmerican, the spray drying solid that contains 15% corn starch and 85% alpha-lactose monohydrate of Inc.)

[method for making] gets component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with component 1 and the component 2 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 25 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 41 and reference examples thereof

100 (from Meggle excipients& The spray drying solid that contains 75% alpha-lactose monohydrate and 25% microcrystalline Cellulose of technology)

[embodiment 41-1 method for making] component 1,3～4 is dissolved in altogether appropriate hot ethanol and obtains solution, and above-mentioned solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder and component 2 mix, and in pack into after mixing suitable bubble eye or tablet mould, then are heated to 80 ℃ of temperature and are incubated 25 minutes, are cooled to room temperature and get final product.

[embodiment 41-2 method for making] gets component 3, and heat fused adds the aqueous solution of (with water-soluble in right amount) component 4, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is 0.2～2 μ m approximately) powder; Above-mentioned powder and component 1 (crossing 100 mesh sieves (levigate in case of necessity)), 2 mix, and in pack into after mixing suitable bubble eye or tablet mould, then are heated to 100 ℃ of temperature and are incubated 15 minutes, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: be followed successively by PEG600, N1 except component 4 in embodiment 41-1 and reference examples, embodiment 41-2 and reference examples thereof, N3-bis-(N-myristoyl lysine phosphate)-1, outside the 3-propane diamine, other are all identical.

Embodiment 42 and reference examples thereof

The material of the common drying that Advantose FS95Fructose(is 95% fructose and 5% starch).

[method for making] gets component 4, and heat fused adds component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with component 1,2 and the component 3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 95 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,2,4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 3,5, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 43 and reference examples thereof

[embodiment 43-1 method for making] gets component 5, heat fused, add the component 1 of dissolving by proper amount of acetone, mix, add again component 4 heating to make it fusing, mix, fling to after solvent cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with component 3 and the component 2,6 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 30 minutes, is cooled to room temperature and gets final product.

[embodiment 43-2,3 method for makings] are got component 4 and are dissolved in suitable quantity of water, add and are micronized to the approximately component 5 of 1～5 μ m of mean diameter, mix rear dispersion liquid spray drying and obtain solid coating powder; Above-mentioned powder and the component 3 of crossing 100 mesh sieves (levigate in case of necessity), component 1 and the component 2,6 of crossing 200 mesh sieves (levigate in case of necessity) are mixed, after mixing, pack in suitable bubble eye or tablet mould, be heated to again 130～140 ℃ of temperature and be incubated 10 minutes, being cooled to room temperature and getting final product.

[reference examples method for making] gets component 3～5, crosses 100 mesh sieves (levigate in case of necessity), and component 1 is crossed 200 mesh sieves (levigate in case of necessity), mixes, and adds component 2,6, mixes, and (other) are standby with legal system by embodiment afterwards.

Illustrate: in embodiment 43-1 and reference examples, embodiment 43-2 and reference examples thereof, embodiment 43-3 and reference examples (formula) thereof, except component 5 is followed successively by PEG2500, Glycodeoxrycholic acid, potassium hydrogen tartrate, other are all identical.

Embodiment 44 and reference examples thereof

[method for making] gets component 4, and heat fused adds component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to temperature 70 C again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 45 and reference examples thereof

[embodiment 45-1 method for making] gets component 4,5, heat fused, add the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[embodiment 45-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 5, and heating makes it fusing, in high-speed stirred to its emulsifying, about 1～5 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves, after mixing (other) by embodiment 45-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 46 and reference examples thereof

t, the maltodextrin of Roquette American Inc. and spray-dired glucose

[embodiment 46-1 method for making] gets component 3, and heat fused, add component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 5 μ m) powder; Above-mentioned powder mixes with component 1 and the component 2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 46-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 3, and heating makes fusing, and in high-speed stirred, to its emulsifying, in emulsion, the mean diameter of particle is not more than 100nm, and emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 46-1 with method method for making (filling a prescription constant)

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 47 and reference examples thereof

MANNOGEM EZ

spray-dired mannitol from SPIPharma.Inc.

[embodiment 47-1 method for making] gets component 5, and heat fused, add component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 1 μ m) powder; Above-mentioned powder mixes with component 1,3 and the component 2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 47-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, in high-speed stirred to its emulsifying, about 1～25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 47-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1,3～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 48 and reference examples thereof

[embodiment 48-1 method for making] gets component 1,4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 30 minutes, is cooled to room temperature and gets final product.

[embodiment 48-2～5 method for makings] are got component 4 and are dissolved in appropriate ethanol-water (1: 1), with this liquid, to being suspended in micronized component 5 in fluid bed (wherein embodiment 48-2 be micronized to mean diameter approximately 80～100 μ m, embodiment 48-3 are micronized to mean diameter approximately 1～5 μ m, embodiment 48-4 are micronized to mean diameter approximately 1～5 μ m, embodiment 48-5 are micronized to approximately 5～25 μ m of mean diameter) spray drying, obtain solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves, and after mixing, (other) press embodiment 48-1 with the method method for making.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 48-1 and reference examples, embodiment 48-2 and reference examples thereof, embodiment 48-3 and reference examples thereof, embodiment 48-4 and reference examples thereof, embodiment 48-5 and reference examples (formula) thereof, except component 5, be followed successively by mannitol, mannitol, bad-cheese-Se-methyl-sweet-paddy six peptides, (D-) leucine, TM-β-CD, other are all identical.

Embodiment 49 and reference examples thereof

[embodiment 49-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 49-2 method for making] got component 5 and is dissolved in appropriate ethanol, adds component 4, makes it to be micronized to approximately 50～100nm of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 49-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 50 and reference examples thereof

[embodiment 50-1 method for making] gets component 4,5, heat fused, add the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 98 ℃ of temperature again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[embodiment 50-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, and in high-speed stirred, to its emulsifying, in emulsion, the mean diameter of particle is not more than 1 μ m, and this emulsion frozen drying obtains solid coating powder; It is even that above-mentioned powder and the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 50-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 51 and reference examples thereof

[embodiment 51-1 method for making] gets component 4,5,6, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 25 μ m) powder 1; Above-mentioned powder 1 mixes with the component 1,2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[embodiment 51-2 method for making] got component 5,6 and is dissolved in appropriate ethanol-water (1: 1), with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3,4 of crossing 100 mesh sieves, mix, afterwards (other) by embodiment 51-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 52 and reference examples thereof

[embodiment 52-1 method for making] gets component 4, and heat fused adds component 5 and by appropriate alcohol-soluble component 1, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 52-2 method for making] gets component 4 heat fused, adds component 5, adds micronized component 2 (mean diameter is 5～25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, after mixing (other) by embodiment 52-1 with method method for making (filling a prescription constant).

[embodiment 52-3 method for making] gets component 4, and heat fused adds component 5 to mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, and it is standby with legal system that after mixing, (other) press embodiment 52-1.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 8, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 53 and reference examples thereof

[embodiment 53-1 method for making] component 1,4,5 is dissolved in appropriate hot water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 110 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 53-2 method for making] got component 1 and 4 and is dissolved in appropriate hot water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 5 spray dryinges of 90～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 53-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 54 and reference examples thereof

The component 5 of [embodiment 54-1 method for making] component 1 and four minutes amounts is dissolved in appropriate ethanol altogether, with gained solution in fluid bed to suspend be micronized to mean diameter approximately component 2 spray dryinges of 80～100 μ m obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) solid coating powder 1; Get 5 of component 4 and surplus, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 2; Above-mentioned powder 1,2 has been crossed the component 3 of 100 mesh sieves (levigate in case of necessity) and has been mixed, and adds component 6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 30 minutes, is cooled to room temperature and gets final product.

[embodiment 54-2 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; Above-mentioned powder 1 has been crossed the component 1,2,3 of 100 mesh sieves (levigate in case of necessity) and has been mixed, and adds component 6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 30 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 55 and reference examples thereof

[embodiment 55-1 method for making] gets component 3, and heat fused adds by appropriate water-soluble component 1,4, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to temperature 70 C and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 55-2 method for making] got component 3,4 and is dissolved in suitable quantity of water, and solution spray or lyophilization obtain solid and disperse or the coating powder; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to temperature 70 C and is incubated 20 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 56 and reference examples thereof

[embodiment 56-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 96 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[embodiment 56-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 100 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves, mix, afterwards (other) by embodiment 56-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 57 and reference examples thereof

[embodiment 57-1 method for making] gets component 6, and heat fused adds component 7 to mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100 μ m) powder 1; Above-mentioned powder mixes with the component 1～5 of crossing 100 mesh sieves, adds component 8, mixes, and with the about 1.9t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 116 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 57-2 method for making] got component 7 and is dissolved in suitable quantity of water, adds component 6, and heating makes fusing, in high-speed stirred to its emulsifying, about 5～25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder 1; Afterwards (other) by embodiment 57-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 8, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 58 and reference examples thereof

[embodiment 58-1～5 method for makings] get component 4, and heat fused adds by appropriate water-soluble component 5, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Illustrate: in embodiment 58-1 and reference examples, embodiment 58-2 and reference examples thereof, embodiment 58-3 and reference examples thereof, embodiment 58-4 and reference examples thereof, embodiment 58-5 and reference examples (formula) (formula) thereof, except component 5, be followed successively by erythritol, Calcium peptide, anserine, 3-hydroxyl butyl-gamma-cyclodextrin, L-hydroxyproline, other are all identical.

Embodiment 59 and reference examples thereof

[embodiment 59-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is 60～100nm approximately) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 59-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 60～100nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 59-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 60 and reference examples thereof

[embodiment 60-1 method for making] gets component 3, heat fused, the component 1 that adds component 4 and dissolve by proper amount of acetone, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 135 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 60-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 3, and heating makes fusing, in high-speed stirred to its emulsifying, the about 60～100nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), after mixing (other) by embodiment 60-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 61 and reference examples thereof

[embodiment 61-1 method for making] gets component 4, and heat fused adds component 5,6 and by appropriate alcohol-soluble component 1, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3,7～9 of crossing 100 mesh sieves (levigate in case of necessity), after mixing with the about 0.4t/ pestle of tabletting pressure tabletting (sheet hardness 2.8kp, n=5), sheet is heated to 110 ℃ of temperature again and is incubated at least 1 hour under vacuum, until component 9 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 61-2 method for making] got component 6 and is dissolved in suitable quantity of water, adds component 4,5, and heating makes fusing, in high-speed stirred to its emulsifying, the about 10～60nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～3,7～9 of crossing 100 mesh sieves (levigate in case of necessity), after mixing (other) by embodiment 61-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～9, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 62 and reference examples thereof

The component 1,4 that [embodiment 62-1 method for making] dissolves with appropriate 95% hot alcohol, add the component 5 with appropriate hot water dissolving, mixes, and spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 2～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), after mixing with the about 0.4t/ pestle of tabletting pressure tabletting (sheet hardness 2.8kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated at least 1 hour under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 62-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, the about 10～60nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), after mixing (other) by embodiment 62-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 63 and reference examples thereof

[method for making] gets component 3, and heat fused adds component 4, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with component 1,2, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2,4, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 64 and reference examples thereof

[method for making] gets component 4, and heat fused adds component 5,6, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 1～3,7～9 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to temperature 70 C and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～9, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 65 and reference examples thereof

[embodiment 65-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 65-2 method for making] gets component 4 heat fused, adds component 5, adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of half amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 65-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 66 and reference examples thereof

[embodiment 66-1 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is 1～5 μ m approximately) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 8 minutes, is cooled to room temperature and gets final product.

[embodiment 66-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, about 1～5 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 66-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 67 and reference examples thereof

[embodiment 67-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; Above-mentioned powder 1 is packed into after mixing with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity) in suitable bubble or tablet mould, then is heated to temperature 70 C and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 67-2 method for making] got component 4,5 and is dissolved in appropriate ethanol, adds the component 2 of half amount, makes it micronized (mean diameter is 1～5 μ m approximately), and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 67-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5 mixing, crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 68 and reference examples thereof

[method for making] gets component 3, and heat fused adds component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～2 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 1.8t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 40 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 69 and reference examples thereof

[method for making] gets component 3, and heat fused adds component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～2 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 1.8t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 20 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 70 and reference examples thereof

[embodiment 70-1 method for making] component 1,4,5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization become solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 170 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 70-2 method for making] component 4,5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization become solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 170 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 70-3,4 method for makings] are got component 4 and are dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 5 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, mixes, and (other) press embodiment 70-1 with the method method for making afterwards.

[embodiment 70-5 method for making] got component 4,5 and is dissolved in suitable quantity of water, adds micronized component 2 (mean diameter is 0.5～1 μ m approximately), and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), adds component 8, mixes, and (other) press embodiment 70-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), adds component 8, mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 70-1 and reference examples, embodiment 70-2 and reference examples thereof, embodiment 70-3 and reference examples thereof, embodiment 70-4 and reference examples thereof, embodiment 70-5 and reference examples (formula) thereof, except component 5, be followed successively by sodium lauroyl lactylate, sodium lauroyl lactylate, sucrose, threonine-methionine-glycine tripeptide, threonine-methionine-glycine tripeptide, other are all identical.

Embodiment 71 and reference examples thereof

[embodiment 71-1 method for making] component 1 is dissolved in appropriate ethanol, adds the component 3,4 melted, and mixes, cooling after ethanol is evaporated completely, and is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 2,5～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 78 ℃ of temperature again and is incubated 1 minute, is cooled to room temperature and gets final product.

[embodiment 71-2 method for making] gets component 3,4 heat fused, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 100nm); It is even that above-mentioned powder and the component 1,2,5～7 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 71-1 with method method for making (filling a prescription constant).

[embodiment 71-3 method for making] got component 3 and is dissolved in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4～7 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 71-1 with method method for making (filling a prescription constant).

[embodiment 71-4 method for making] got component 4 and is dissolved in suitable quantity of water, under 0 ℃ of ambient temperature, be micronized to approximately component 3 spray coatings of 1～5 μ m of mean diameter with this solution to what suspend, afterwards the coated granule of above-mentioned suspension is sprayed into to liquid nitrogen or carbon dioxide solidifies the coatings of this granule, shift subsequently this cured granulate to frozen drying equipment, reach dry (moisture in making coatings directly transfers gaseous state from solid-state to without liquid state) above-mentioned granule under vacuum state in temperature below 0 ℃ and obtain solid coating powder; Above-mentioned powder mixes with the component 1～2,5～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 105 ℃ of temperature again and is incubated 2 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 71-1 and reference examples, embodiment 71-2 and reference examples (formula) thereof, embodiment 71-3 and reference examples (formula) thereof, embodiment 71-4 and reference examples (formula) thereof, except component 4 is followed successively by behenic acid, behenic acid, behenic acid, 1,2,3,4,5-pentanepentol, other are all identical.

Embodiment 72 and reference examples thereof

[embodiment 72-1 method for making] gets component 4,5 heat fused, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 2 minutes, is cooled to room temperature and gets final product.

[embodiment 72-2 method for making] got component 4 and is dissolved in or is scattered in suitable quantity of water, adds the component 2 of half amount, makes it to be micronized to approximately 50～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 72-1 with method method for making (filling a prescription constant).

[embodiment 72-3 method for making] gets component 4 heat fused, adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of half amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 72-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment afterwards.

Embodiment 73 and reference examples thereof

[embodiment 73-1 method for making] gets component 4～5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 73-2 method for making] component 4,5 is dissolved in or is scattered in suitable quantity of water, and solution spray or lyophilization become solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120～140 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: be followed successively by poly(ethylene oxide) (molecular weight 200,000), D-2-deoxyribose and component 5 except component 4 and be followed successively by glycerol list (meat) myristate, chitin in embodiment 73-1 and reference examples, embodiment 73-2 and reference examples (formula) thereof, other are all identical.

Embodiment 74 and reference examples thereof

[embodiment 74-1 method for making] gets component 4～5, and heat fused adds and is micronized to the approximately component 2 of 60～100 μ m of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,3,6 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 6 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 74-2 method for making] got component 4,5 and is dissolved in appropriate ethanol-water (1: 1), with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of half amount of 5～25 μ m obtain solid coating powder; Above-mentioned powder mixes with crossing the component 1,3,6 of 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, and (other) press embodiment 74-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 74-1 and reference examples, embodiment 74-2 and reference examples (formula) thereof, except component 2, be followed successively by sodium oxybate, Umami flavor peptides, other are all identical.

Embodiment 75 and reference examples thereof

[embodiment 75-1 method for making] component 1,4,5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and in pack into suitable bubble eye or tablet mould, then is heated to 170 ℃ of temperature and is incubated 45 minutes, is cooled to room temperature and gets final product.

[embodiment 75-2 method for making] component 4,5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 75-1 with the method method for making afterwards.

[embodiment 75-3 method for making] got component 4 and is dissolved in suitable quantity of water, adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of half amount, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5,6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, in pack into suitable bubble or tablet mould, then is heated to 130 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 75-4 method for making] gets component 4 heat fused, adds the micronized component 5 (mean diameter is 5～25 μ m approximately) of half amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; The component 5 of above-mentioned powder and the component 1,2,3,6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, and (other) press embodiment 75-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, standby with legal system by embodiment after mixing.

Illustrate: in embodiment 75-1 and reference examples, embodiment 75-2 and reference examples thereof, embodiment 75-3 and reference examples thereof, embodiment 75-4 and reference examples (formula) thereof, except component 5 is followed successively by hydroxyl isomaltulose, hydroxyl isomaltulose, Calcium peptide, Calcium peptide, other are all identical.

Embodiment 76 and reference examples thereof

[embodiment 76-1 method for making] component 3 heat fused, add component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～2,5～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.3t/ pestle of tabletting pressure tabletting (sheet hardness 2.3kp, n=5), sheet is heated to 90 ℃ of temperature and is incubated 7 minutes, is cooled to room temperature and gets final product.

[embodiment 76-2 method for making] component 3 heat fused, add component 4, add half amount and be micronized to the approximately component 2 of 5～25 μ m of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (decentralized photo or continuous phase mean diameter are not more than 10nm) powder; Above-mentioned powder mixes with the component 1,5～7 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, afterwards (other) by embodiment 76-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 77 and reference examples thereof

[embodiment 77-1 method for making] gets component 5, and heat fused adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of half amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder is with the component 1,3,4,6 of 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus mix excessively, with the about 0.28t/ pestle of tabletting pressure tabletting (sheet hardness 2.3kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 77-2 method for making] got component 6 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, in high-speed stirred to its emulsifying, the about 25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～4 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.28t/ pestle of tabletting pressure tabletting (sheet hardness 2.3kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 78 and reference examples thereof

[embodiment 78-1 method for making] gets component 4,5, heat fused becomes the consolute thing, component 1 use suitable quantity of water is dissolved near saturated solution, add above-mentioned consolute thing, mix, Deng cooling after moisture evaporation, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.6kp, n=5), sheet is heated to 130 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 78-2,5～6 method for makings] are got component 4,5 and are dissolved in suitable quantity of water, and solution spray or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 78-1 with the method method for making afterwards.

[embodiment 78-3 method for making] got component 4 and is dissolved in appropriate ethanol, adds component 2, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 78-1 with the method method for making afterwards.

[embodiment 78-4 method for making] gets component 4, and heat fused adds and is micronized to the approximately component 2 of 5～25 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 78-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 78-1 and reference examples, embodiment 78-2 and reference examples thereof, embodiment 78-3 and reference examples thereof, embodiment 78-4 and reference examples thereof, embodiment 78-5 and reference examples thereof, embodiment 78-6 and reference examples (formula) thereof, except component 5, be followed successively by galactose, galactose, galactose, galactose, HBe-β-CD, Miraculin (changing the flavor glycoprotein), other are all identical.

Embodiment 79 and reference examples thereof

[embodiment 79-1 method for making] heat fused component 5,6, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) coating powder; Above-mentioned powder mixes with the component 1～4 of crossing 100 mesh sieves (levigate in case of necessity), adds component 7, mixes, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.6kp, n=5), sheet is heated to 110 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 79-2 method for making] got component 5 and is dissolved in appropriate ethanol, adds component 6, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1～4 of crossing 100 mesh sieves (levigate in case of necessity), adds component 7, mix, afterwards (other) by embodiment 79-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 80 and reference examples thereof

[embodiment 80-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 6 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 80-2 method for making] got component 4,5 and is dissolved in appropriate ethanol, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of half amount of 90～100 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3,6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 80-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 81 and reference examples thereof

[embodiment 81-1 method for making] component 1,4,5 is dissolved in appropriate 80% ethanol, and after solution, spraying or lyophilization, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 0.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.7kp, n=5), sheet is heated to 150 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 81-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds component 2, makes it to be micronized to approximately 80～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 81-1 with the method method for making afterwards.

[embodiment 81-3～5 method for makings] are got component 4,5 and are dissolved in suitable quantity of water, the dry solid coating powder (the dispersate mean diameter is not more than 10nm) that obtains of solution spray; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 81-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 81-1 and reference examples, embodiment 81-2 and reference examples thereof, embodiment 81-3 and reference examples thereof, embodiment 81-4 and reference examples thereof, embodiment 81-5 and reference examples (formula) thereof, except component 5, be followed successively by glucose, glucose, glucose, malt sugar group-beta-cyclodextrin base-glucose, threonine-isoleucine-arginine monohydrochloride, other are all identical.

Embodiment 82 and reference examples thereof

[embodiment 82-1,2 method for makings] get component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes, adds component 5 with the component 1～2 of crossing 100 mesh sieves (levigate in case of necessity), mix, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 82-3 method for making] got component 3,4 and is dissolved in appropriate ethanol, adds component 2, makes it to be micronized to approximately 50～100 μ m of mean diameter, and this dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5 to mix, afterwards (other) by embodiment 82-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 5, mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 82-1 and reference examples, embodiment 82-2 and reference examples thereof, embodiment 82-3 and reference examples (formula) thereof, except component 2, be followed successively by kaolin, holothurian collagen peptide, holothurian collagen peptide, other are all identical.

Embodiment 83 and reference examples thereof

[embodiment 83-1 method for making] component 1,4,5 is dissolved in suitable quantity of water, and spray drying after solution obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3,6 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and packs in suitable bubble eye or tablet mould, is heated to 170 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 83-2 method for making] component 4,5 is dissolved in suitable quantity of water, and spray drying after solution obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and (other) press embodiment 83-1 with the method method for making afterwards.

[embodiment 83-3 method for making] got component 4 and is dissolved in suitable quantity of water, adds and is micronized to the approximately component 2 of 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; It is even that above-mentioned powder and the component 1,3,5,6 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, and (other) press embodiment 83-1 with the method method for making afterwards.

[embodiment 83-4 method for making] component 4,5 is dissolved in suitable quantity of water, and spray drying after solution obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and packs in suitable bubble eye or tablet mould, is heated to 150 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 83-1 and reference examples, embodiment 83-2 and reference examples thereof, embodiment 83-3 and reference examples thereof, embodiment 83-4 and reference examples (formula) thereof, except component 5 is followed successively by verbascose, verbascose, verbascose, L-PROLINE, other are all identical.

Embodiment 84 and reference examples thereof

[embodiment 84-1 method for making] component 1,4,5 is dissolved in appropriate 95% ethanol, and spray drying after solution obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 100 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 84-2 method for making] got component 4,5 and is dissolved in suitable quantity of water, with this solution to be micronized to mean diameter approximately component 1 spray coating of 70～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 84-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 85 and reference examples thereof

[embodiment 85-1 method for making] gets component 6,7, and heat fused, fully mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes, adds 8 to mix with the component 1～5 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 85-2 method for making] got component 6,7 and is dissolved in or is scattered in appropriate hot water, adds the component 2 of half amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,4,5,8 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 85-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 8, mixes, standby with legal system by embodiment afterwards.

Embodiment 86 and reference examples thereof

[method for making] gets component 3,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 1,2,4 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 87 and reference examples thereof

[embodiment 87-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 87-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, in high-speed stirred to its emulsifying, the about 50～100nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 87-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, standby with legal system by embodiment afterwards.

Embodiment 88 and reference examples thereof

[embodiment 88-1 method for making] component 1,2 is dissolved in the aqueous solution of appropriate 10% ethanol, and spray drying after solution obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 5, heat fused, add 6, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 2; Above-mentioned powder 1,2 mixes with the component 3,4 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to temperature 70 C and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 88-2 method for making] gets component 5,6 heat fused, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; It is even that above-mentioned powder and the component 1～4 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 88-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 89 and reference examples thereof

[embodiment 89-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 96 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 89-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, in high-speed stirred to its emulsifying, about 5～25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 89-1 with method method for making (filling a prescription constant).

[embodiment 89-3 method for making] gets component 4 heat fused, adds the micronized component 2 (mean diameter is 50～100 μ m approximately) of half amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 89-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 90 and reference examples thereof

[embodiment 90-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), after mixing with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 90-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder and the component 1,3,5～7 of crossing 100 mesh sieves (levigate in case of necessity) be mixed to even after, (other) press embodiment 90-1 with the method method for making afterwards.

[embodiment 90-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 5 spray dryinges of 90～100 μ m obtain solid coating powder; It is even that above-mentioned powder and the component 1,2,3,6～7 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, and (other) press the same legal system of embodiment 90-1 afterwards.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 90-1 and reference examples, embodiment 90-2 and reference examples thereof, embodiment 90-3 and reference examples (formula) thereof, except component 5 is followed successively by Perseitol, Perseitol, galactosyl-gamma-cyclodextrin, other are all identical.

Embodiment 91 and reference examples thereof

[embodiment 91-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 25 μ m) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 91-2 method for making] got component 5 and is dissolved in suitable quantity of water, under 0 ℃ of ambient temperature, be micronized to approximately component 4 spray coatings of 5～25 μ m of mean diameter with this solution to what suspend, afterwards the coated granule of above-mentioned suspension is sprayed into to liquid nitrogen or carbon dioxide solidifies the coatings of this granule, shift subsequently this cured granulate to frozen drying equipment, reach dry (moisture in making coatings directly transfers gaseous state from solid-state to without liquid state) above-mentioned granule under vacuum state in temperature below 0 ℃ and obtain solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 91-3 method for making] got component 4,5 and is dissolved in appropriate 90% ethanol, and this liquid spray drying in fluid bed obtains solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 91-1 and reference examples, embodiment 91-2 and reference examples (formula) thereof, embodiment 91-3 and reference examples (formula) thereof, except component 5, be followed successively by rhamnose, rhamnose, 3-HP-β-CD, other are all identical.

Embodiment 92 and reference examples thereof

[embodiment 92-1 method for making] gets component 5, and heat fused adds micronized component 2,6 (mean diameter is 1～5 μ m approximately), mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 5 μ m) powder; Above-mentioned powder mixes with the component 1,3～4 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 92-2 method for making] got component 6 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, in high-speed stirred to its emulsifying, about 5～25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; It is even that above-mentioned powder and the component 1～4 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 92-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 93 and reference examples thereof

[embodiment 93-1 method for making] gets component 4, heat fused, add and be micronized to mean diameter approximately component 2 and the component 5 of 25 μ m, mixes, cooling, be crushed to 100～120 orders and obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 93-2 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders and obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 94 and reference examples thereof

[embodiment 94-1 method for making] gets component 4, and heat fused adds and is micronized to mean diameter approximately component 2 and the component 5 of 30% amount of 5 μ m, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) coating powder; Above-mentioned powder is with the component 1,3 of 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus are mixed excessively, after mixing with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 94-2 method for making] gets component 4, and heat fused, add component 5, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 95 and reference examples thereof

[embodiment 95-1 method for making] gets component 3, and heat fused, add component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～2 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5, mixes, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 95-2 method for making] gets component 3,4 heat fused, adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of 10% amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 5, after mixing (other) by embodiment 95-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 5, mixes, standby with legal system by embodiment afterwards.

Embodiment 96 and reference examples thereof

[embodiment 96-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; Above-mentioned powder 1 mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 100 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 96-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 35% amount of 70～100 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 96-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 97 and reference examples thereof

[embodiment 97-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 100 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 97-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 5, and heating makes fusing, in high-speed stirred to its emulsifying, about 1～5 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 97-1 with method method for making (filling a prescription constant).

[embodiment 97-3 method for making] got component 4 and is dissolved in suitable quantity of water, adds the component 2 of 1/3rd amounts, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 97-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 98 and reference examples thereof

[embodiment 98-1 method for making] component 4,5 heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.25t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 155 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 98-2 method for making] got component 5 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 4 spray dryinges of 90～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 98-1 with method method for making (filling a prescription constant).

[embodiment 98-3 method for making] got component 5 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder and the component 1,3～4,6～8 of crossing 100 mesh sieves (levigate in case of necessity) and be mixed to evenly, (other) press embodiment 98-1 with the method method for making afterwards.

[embodiment 98-4 method for making] got component 4,5 and is dissolved in suitable quantity of water, and this liquid spray drying in fluid bed obtains solid coating powder; Above-mentioned powder and the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity) and be mixed to evenly, (other) press embodiment 98-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 98-1 and reference examples, embodiment 98-2 and reference examples thereof, embodiment 98-3 and reference examples thereof, embodiment 98-4 and reference examples (formula) thereof, except component 5 is followed successively by maltose, maltose, maltose, D-phenylalanine, other are all identical.

Embodiment 99 and reference examples thereof

[embodiment 99-1 method for making] got component 1,3,4 and is dissolved in appropriate water, spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution; Above-mentioned powder mixes with the component 2,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 135 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 99-2 method for making] got component 3,4 and is dissolved in suitable quantity of water, and this liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,2,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, and (other) press embodiment 99-1 with the method method for making afterwards.

[embodiment 99-3 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 4 spray dryinges of 1～5 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,2,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 99-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 99-1 and reference examples, embodiment 99-2 and reference examples thereof, embodiment 99-3 and reference examples (formula) thereof, except component 4 is followed successively by altrose, altrose, leucine, other are all identical.

Embodiment 100 and reference examples thereof

[embodiment 100-1 method for making] gets component 3,4, and heat fused adds and is micronized to the approximately component 1 of 50～90 μ m of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100 μ m) powder; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 35 minutes, is cooled to room temperature and gets final product.

[embodiment 100-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 3, and heating makes fusing, in high-speed stirred to its emulsifying, the about 60～100nm of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 100-1 with method method for making (filling a prescription constant).

[embodiment 100-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 100-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 101 and reference examples thereof

[embodiment 101-1 method for making] gets the aqueous solution that component 1,3,4 is dissolved in appropriate 85% ethanol, spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 100nm) powder that obtains of solution; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 95 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 101-2 method for making] gets component 3, and heat fused adds the component 1 with the aqueous solution dissolving of appropriate 85% ethanol, mix, fling to solvent, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; It is even that above-mentioned powder and the component 2,4 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 101-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 102 and reference examples thereof

[embodiment 102-1 method for making] got component 1,4～6 and is dissolved in 95% appropriate ethanol-ether (2:8), spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 76 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 102-2 method for making] got component 4～6 and is dissolved in 95% appropriate ethanol-ether (2:8), spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 76 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 102-3 method for making] got component 5,6 and is dissolved in or is scattered in appropriate ethanol-water (1: 1), with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 50% amount of 60～100 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3,4 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 102-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 103 and reference examples thereof

[embodiment 103-1 method for making] got component 3 and is dissolved in appropriate ether, and component 4 is dissolved in appropriate 95% ethanol, and two liquid mix, and mixes spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 100nm) powder that obtains of rear solution; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 95 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 103-2 method for making] got component 4 and is dissolved in suitable quantity of water, then adds component 3, and heating makes fusing, in high-speed stirred to its emulsifying, the about 1 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; Afterwards (other) by embodiment 103-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment afterwards.

Embodiment 104 and reference examples thereof

[embodiment 104-1 method for making] got component 1,3,4 and is dissolved in appropriate 95% ethanol, spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.25t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 104-2 method for making] got component 3,4 and is dissolved in appropriate 95% ethanol, adds the micronized component 2 (mean diameter is 40～100 μ m approximately) of half amount, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 104-1 with method method for making (filling a prescription constant).

[embodiment 104-3 method for making] got component 3,4 and is dissolved in appropriate 95% ethanol, and solution spray is dry that solid disperses or coating powder (the dispersate mean diameter is not more than 10nm); It is even that above-mentioned powder and the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 104-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment afterwards.

Embodiment 105 and reference examples thereof

[embodiment 105-1 method for making] gets component 5,6, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 1～4,7 of crossing 100 mesh sieves (levigate in case of necessity), add component 8, after mixing with the about 0.27t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to temperature 70 C again and is incubated 40 minutes, is cooled to room temperature and gets final product.

[embodiment 105-2 method for making] gets component 5,6, heat fused, and what add 30% amount is micronized to the approximately component 2 of 5～25 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1,3～4,7 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 8, mix, afterwards (other) by embodiment 105-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 8, standby with legal system by embodiment after mixing.

Embodiment 106 and reference examples thereof

[embodiment 106-1 method for making] gets component 5, and heat fused, add component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 4 minutes, is cooled to room temperature and gets final product.

[embodiment 106-2 method for making] gets component 5, and heat fused, add component 4, mixes, and what add 30% amount is micronized to the approximately component 2 of 30～60 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 8, mix, afterwards (other) by embodiment 106-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 107 and reference examples thereof

[embodiment 107-1 method for making] gets component 3, and heat fused, add component 4, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～2,5 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 107-2 method for making] got component 3,4 and is dissolved in suitable quantity of water, spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution; Above-mentioned powder mixes with the component 1,2,5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 130～140 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes (embodiment 107-1 component 4 first absorbs by component 2), crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 107-1 and reference examples, embodiment 107-2 and reference examples (formula) thereof, except component 3 is followed successively by lacceroic acid, 1,2,3,4,5-pentanepentol and component 4, be followed successively by PEG-200 Oleum Ricini, glucosamine, other are all identical.

Embodiment 108 and reference examples thereof

[embodiment 108-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 110 ℃ of temperature and is incubated 30 minutes, is cooled to room temperature and gets final product.

[embodiment 108-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 5 spray dryinges of 90～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 108-1 with method method for making (filling a prescription constant).

[embodiment 108-3 method for making] got component 5 and is dissolved in suitable quantity of water, under 0 ℃ of ambient temperature, be micronized to approximately component 4 spray coatings of 1～5 μ m of mean diameter with this solution to what suspend, afterwards the coated granule of above-mentioned suspension is sprayed into to liquid nitrogen or carbon dioxide solidifies the coatings of this granule, shift subsequently this cured granulate to frozen drying equipment, reach dry (moisture in making coatings directly transfers gaseous state from solid-state to without liquid state) above-mentioned granule under vacuum state in temperature below 0 ℃ and obtain solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 125 ℃ of temperature and is incubated 1 minute, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 109 and reference examples thereof

[embodiment 109-1 method for making] component 1～2 is dissolved in appropriate hot water, adds component 3, and after the abundant swelling of component 3, solution mixes rear spray drying, obtains solid dispersion (/ body) powder 1; Get component 4,5, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 2; Above-mentioned powder 1,2 mixes, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to 70～90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 109-2 method for making] component 1～2 is dissolved in or is scattered in appropriate hot water, adds component 3, and after the abundant swelling of component 3, solution mixes rear spray drying, obtains solid dispersion (/ body) powder 1; Component 4 is dissolved in appropriate hot alcohol, adds and is micronized to the approximately component 5 of 1～5 μ m of mean diameter, and dispersion liquid mixes rear spray drying and obtains solid coating (/ body) powder 2; Above-mentioned powder 1,2 mixes, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to 70～90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] component 1～2 is dissolved in suitable quantity of water, adds component 3, and after the abundant swelling of component 3, solution mixes rear spray drying and obtains solid dispersion (/ body) powder 1; Get component 4～5, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, mix, standby with legal system by embodiment after mixing.

Illustrate: in embodiment 109-1 and reference examples, embodiment 109-2 and reference examples (formula) thereof, except component 5 is followed successively by lauroyl sarcosine, poly-aspartate, other are all identical.

Embodiment 110 and reference examples thereof

[embodiment 110-1 method for making] gets component 4,5 heat fused, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.7t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 110-2～3 method for makings] are got component 4,5 and are dissolved in appropriate hot alcohol-water (9: 1) liquid, and solution spray or lyophilization obtain solid coating or solid dispersion powder; (other) press embodiment 110-1 with the method method for making afterwards.

[embodiment 110-4 method for making] gets component 4 heat fused, adds and is micronized to the approximately component 5 of 15～25 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; (other) press embodiment 110-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 110-1 and reference examples, embodiment 110-2 and reference examples thereof, embodiment 110-3 and reference examples thereof, embodiment 110-4 and reference examples (formula) thereof, except component 4, be followed successively by palmityl alcohol, palmityl alcohol, 3-HP-β-CD, palmityl alcohol, component 5 is followed successively by outside stearoylglycine, stearoylglycine, stearoylglycine, laureth-6 carboxylic acid sodium, and other are all identical.

Embodiment 111 and reference examples thereof

[embodiment 111-1 method for making] gets component 3,4, and heating makes it fusing, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～2,5～6 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.7t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 6 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 111-2 method for making] got component 3 and is dissolved in suitable quantity of water, adds component 4, and heating makes fusing, in high-speed stirred to its emulsifying, about 5～25 μ m of the mean diameter of particle in emulsion, emulsion spraying or lyophilization obtain solid coating powder; (other) press embodiment 111-1 with the method method for making afterwards.

[embodiment 111-3 method for making] got component 3 and is dissolved in appropriate ethanol, adds the component 2 of half amount, makes it micronized to about 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4,5,6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, and (other) press embodiment 111-1 with the method method for making afterwards.

[embodiment 111-4,5 method for makings] are got component 3,4 and are dissolved in suitable quantity of water, and solution spray or lyophilization obtain solid coating powder; (other) press embodiment 111-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 111-1 and reference examples, embodiment 111-2 and reference examples thereof, embodiment 111-3 and reference examples thereof, embodiment 111-4 and reference examples thereof, embodiment 111-5 and reference examples (formula) thereof, except component 4, be followed successively by lignoceric acid, lignoceric acid, sulphur butyl (ether)-beta-schardinger dextrin-sodium salt, sulphur butyl (ether)-beta-schardinger dextrin-sodium salt, Rhizoma Curculiginis sweet protein, other are all identical.

Embodiment 112 and reference examples thereof

[embodiment 112-1 method for making] gets component 3,4, and heat fused adds and is micronized to the approximately component 1 of 1 μ m of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with component 2, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 112-2 method for making] got component 3,4 and is dissolved in appropriate ethanol, and solution spray or lyophilization obtain solid coating or solid dispersion powder; Above-mentioned powder and component 2, the component 1 of crossing 100 mesh sieves (levigate in case of necessity) mix, afterwards (other) by embodiment 112-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, standby with legal system by embodiment after mixing.

Embodiment 113 and reference examples thereof

[embodiment 113-1 method for making] got and added the component 4,5 melted, and mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 113-2 method for making] got component 4,5 and is dissolved in appropriate ethanol, adds component 2, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 113-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 114 and reference examples thereof

[embodiment 114-1 method for making] gets component 4,5, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 100～120 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 114-2 method for making] gets component 4, and heat fused adds and is micronized to the approximately component 5 of 1～5 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80～100 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 114-3 method for making] got component 4 and is dissolved in suitable quantity of water, adds the aqueous colloidal (dispersate mean diameter 30～600nm) of component 5, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 114-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 114-1 and reference examples, embodiment 114-2 and reference examples thereof, embodiment 114-3 and reference examples (formula) thereof, except component 4 is followed successively by Brazil wax, Brazil wax, PEG-20 glyceryl stearate and component 5, be followed successively by PEG-20 sorbitan trioleate, N; outside N-oleoyl N-methyltaurine sodium, hydrated ferric oxide., other are all identical.

Embodiment 115 and reference examples thereof

[embodiment 115-1 method for making] gets component 4 heat fused, add component 5, add again and be micronized to the approximately about component 2 of 25 μ m of mean diameter of the component 1 of 1～5 μ m and half amount of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 3 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 6, mixes, with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 115-2 method for making] got component 4,5 and is dissolved in appropriate 95% ethanol, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of half amount of 25 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3,6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 115-1 with method method for making (filling a prescription constant).

[embodiment 115-3 method for making] got component 4,5 and is dissolved in appropriate 95% ethanol, and this liquid spray drying obtains solid coating powder; It is even that above-mentioned powder and the component 1～3,6 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 115-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 116 and reference examples thereof

[embodiment 116-1 method for making] gets component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 115 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 116-2 method for making] gets component 3 heat fused, adds the micronized component 2 (mean diameter is 1～5 μ m approximately) of half amount, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; The component 2 of above-mentioned powder and the component 1,4 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, and (other) press embodiment 116-1 with the method method for making afterwards.

[embodiment 116-3 method for making] got component 3,4 and is dissolved in or is scattered in appropriate hot water, mixes, and aforesaid liquid spraying or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 115 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 116-1 and reference examples, embodiment 116-2 and reference examples thereof, embodiment 116-3 and reference examples (formula) thereof, except component 4, be followed successively by cholesterol cetylate, cholesterol cetylate, glucosyl group-malt-base-gamma-cyclodextrin, other are all identical.

Embodiment 117 and reference examples thereof

[embodiment 117-1 method for making] gets component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1,2,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1kp, n=5), sheet is heated to 150 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 117-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 4 spray dryinges of 5～25 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1～2,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 117-1 with the method method for making afterwards.

[embodiment 117-3,4 method for makings] are got component 3 and are dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 4 spray dryinges of 1～5 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1～2,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 117-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 117-1 and reference examples, embodiment 117-2 and reference examples thereof, embodiment 117-3 and reference examples thereof, embodiment 117-4 and reference examples (formula) thereof, except component 4, be followed successively by melezitose, melezitose, sodium lauryl sulfate, hydrophilic peanut protein polypeptide, other are all identical.

Embodiment 118 and reference examples thereof

The solid rapid dispersion form of the maltodextrin of Grain Processing Corp. and corn syrup.

[embodiment 118-1 method for making] gets component 3,4, and heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 95 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 118-2 method for making] got component 3 and is dissolved in suitable quantity of water, adds component 4, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 118-1 with the method method for making afterwards.

[embodiment 118-3 method for making] got component 3,4 and is dissolved in appropriate hot water, and solution spray or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 118-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 118-1 and reference examples, embodiment 118-2 and reference examples thereof, embodiment 118-3 and reference examples (formula) thereof, except component 4, be followed successively by single Cera Flava acid glyceride, single Cera Flava acid glyceride, L-glutaminate, other are all identical.

Embodiment 119 and reference examples thereof

[embodiment 119-1 method for making] gets component 4,5, and heat fused adds and is micronized to the approximately component 1 of 1 μ m of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder and the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), add component 6, mixes, and in pack into after mixing suitable bubble or tablet mould, then is heated to 135 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 119-2 method for making] got component 4,5 and is dissolved in appropriate hot water, and solution spray or lyophilization obtain solid coating powder; Above-mentioned powder mixes with the component 1～3,6 of crossing 100 mesh sieves (levigate in case of necessity), and (other) press embodiment 119-1 with the method method for making afterwards.

[embodiment 119-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 5 spray dryinges of 5～25 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 119-1 with the method method for making afterwards.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 119-1 and reference examples, embodiment 119-2 and reference examples thereof, embodiment 119-3 and reference examples (formula) thereof, except component 5, be followed successively by Sorbitol, Sorbitol, Purified Water dissolubility liver peptide, other are all identical.

Embodiment 120 and reference examples thereof

[embodiment 120-1 method for making] component 4～5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 120-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds micronized component 5 (mean diameter is 5～25 μ m approximately), and the dispersion liquid spray drying obtains solid coating powder; It is even that above-mentioned powder and the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity) are mixed to, afterwards (other) by embodiment 120-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 121 and reference examples thereof

[embodiment 121-1 method for making] component 1,3～4 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 150～160 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 121-2,3 method for makings] component 3～4 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 150～160 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 121-4 method for making] component 3 is dissolved in suitable quantity of water, adds the aqueous colloidal dispersion (dispersate mean diameter 100～1000nm) of aluminium hydroxide, disperses spraying or lyophilization to obtain solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 150～160 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 121-1 and reference examples, embodiment 121-2 and reference examples thereof, embodiment 121-3 and reference examples thereof, embodiment 121-4 and reference examples thereof, except component 3 is followed successively by meglumine, meglumine, sodium phosphate, aluminium hydroxide, other are all identical.

Embodiment 122 and reference examples thereof

[embodiment 122-1 method for making] component 1,4～5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and in pack into suitable bubble eye or tablet mould, then is heated to 140 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 122-2 method for making] component 4～5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and in pack into suitable bubble eye or tablet mould, then is heated to 140 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 122-3 method for making] gets component 5 heat fused, adds micronized component 4 (mean diameter is 30～100 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; It is even that above-mentioned powder and the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity) and component 6 are mixed to, and (other) press embodiment 122-2 with the method method for making afterwards.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6 to mix afterwards standby with legal system by embodiment.

Illustrate: in embodiment 122-1 and reference examples, embodiment 122-2 and reference examples thereof, embodiment 122-3 and reference examples thereof, except component 4, be followed successively by alanine-Men days propylhomoserin dipeptides, alanine-Men days propylhomoserin dipeptides, tartaric acid, other are all identical.

Embodiment 123 and reference examples thereof

[embodiment 123-1 method for making] got and is micronized to the approximately component 1,5 of 100 μ m of mean diameter, adds the component 4 melted, and mixes, cooling, is crushed to 100～120 orders, obtains solid coating powder; Above-mentioned powder mixes with the component 2～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), with the about 1t/ pestle of tabletting pressure tabletting (sheet hardness 7kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 8 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 123-2 method for making] got and is micronized to the approximately component 5 of 100 μ m of mean diameter, adds the component 4 melted, and mixes, cooling, is crushed to 100～120 orders, obtains solid coating powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), with the about 1t/ pestle of tabletting pressure tabletting (sheet hardness 7kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 8 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 123-3 method for making] component 4～5 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), with the about 1t/ pestle of tabletting pressure tabletting (sheet hardness 7kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 8 volatilizations are complete, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 123-1 and reference examples, embodiment 123-2 and reference examples thereof, embodiment 123-3 and reference examples thereof, except component 5 is followed successively by glucosaccharic acid, glucosaccharic acid, maleic acid, other are all identical.

Embodiment 124 and reference examples thereof

[embodiment 124-1 method for making] gets component 2,5,6, and heat fused adds and is micronized to the approximately component 1 of 25 μ m of mean diameter, mix, cooling, be crushed to 100～120 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) coating powder; Above-mentioned powder mixes with the component 3,4 of crossing 100 mesh sieves (levigate in case of necessity), adds component 7, mixes, with the about 0.11t/ pestle of tabletting pressure tabletting (sheet hardness 0.08kp, n=5), sheet is heated to 110 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 124-2,3 method for makings] component 2,5,6 is dissolved in or is scattered in appropriate hot water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,3,4 of crossing 100 mesh sieves (levigate in case of necessity), adds component 7, mixes, with the about 0.11t/ pestle of tabletting pressure tabletting (sheet hardness 0.08kp, n=5), sheet is heated to 110 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 7, standby with legal system by embodiment after mixing.

Illustrate: in embodiment 124-1 and reference examples, embodiment 124-2 and reference examples thereof, embodiment 124-3 and reference examples thereof, except component 2, be followed successively by citric acid monohydrate, citric acid monohydrate, potassium acid sulfate, other are all identical.

Embodiment 125 and reference examples thereof

[embodiment 125-1 method for making] component 1,4～5 is dissolved in suitable quantity of water obtaining solution altogether, in fluid bed with above-mentioned solution to 2/3rds amounts of suspension be micronized to mean diameter approximately component 2 spray dryinges of 100 μ m obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) coating powder; Above-mentioned powder mixes with the component 3,6～9 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, in pack into after mixing suitable bubble or tablet mould, then is heated to 80～90 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 125-2 method for making] component 1,4～5 is dissolved in altogether in suitable quantity of water and obtains solution, spray-dried solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of above-mentioned solution; Above-mentioned powder mixes with the component 2,3,6～9 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80～90 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 125-3,4 method for makings] component 4,5 is dissolved in or is scattered in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6～9 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80～90 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～9 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 125-1 and reference examples, embodiment 125-2 and reference examples thereof, embodiment 125-3 and reference examples thereof, embodiment 125-4 and reference examples thereof, except component 4, be followed successively by sweet-paddy dipeptides, sweet-paddy dipeptides, sweet-paddy dipeptides, ascorbic acid, other are all identical.

Embodiment 126 and reference examples thereof

[embodiment 126-1 method for making] component 1,4～5 is dissolved in suitable quantity of water altogether, and spray drying obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 2,3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 126-2,3 method for makings] component 4～5 is dissolved in suitable quantity of water altogether, and spray drying obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 126-4 method for making] got component 4 and is dissolved in appropriate ethanol-water (1: 1), adds and is micronized to the approximately component 5 of 1～5 μ m of mean diameter, and this liquid spray drying in fluid bed obtains solid coating powder; Above-mentioned powder mixes with the component 1～3,6～7 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and presses afterwards embodiment 126-1 with the method method for making.

[reference examples method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 126-1 and reference examples, embodiment 126-2 and reference examples thereof, embodiment 126-3 and contrast thereof, embodiment 126-4 and reference examples example thereof, except component 5, be followed successively by smart ammonia essence, smart ammonia essence, (de-acetyl) oligochitosan, magnesium hydroxide, other are all identical.

Embodiment 127 and reference examples thereof

[embodiment 127-1,2 method for makings] component 5～6 is dissolved in suitable quantity of water altogether, dry solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution spray; Above-mentioned powder mixes with the component 1～4,7 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80～110 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: in embodiment 127-1 and reference examples, embodiment 127-2 and reference examples thereof, except component 6 is followed successively by sodium carbonate, trehalosamine, other are all identical.

Embodiment 128 and reference examples thereof

[embodiment 128-1 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 4, makes it to be micronized to approximately 0.5～5 μ m of mean diameter, and this liquid spray drying in fluid bed obtains solid coating powder; Above-mentioned powder and component 2, the component 1,6 of crossing the component 3 of 100 mesh sieves (levigate in case of necessity) and crossing 200 mesh sieves (levigate in case of necessity) are mixed, after mixing, pack in suitable bubble eye or tablet mould, sheet is heated to 70～100 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 128-2 method for making] component 4～5 is dissolved in suitable quantity of water altogether, dry solid dispersion (/ body) (the dispersate mean diameter the is not more than 10nm) powder that obtains of solution spray; Press afterwards embodiment 128-1 with the method method for making.

[reference examples method for making] gets component 1～6, and component 3 has been crossed 100 mesh sieves (levigate in case of necessity), and component 1,6 has been crossed 200 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Illustrate: in embodiment 128-1 and reference examples, embodiment 128-2 and reference examples thereof, except component 4 is followed successively by zinc oxide, sodium dihydrogen phosphate, other are all identical.

Embodiment 129 and reference examples thereof

[method for making] component 1,4～5 is dissolved in the aqueous solution of appropriate hot 70% ethanol altogether, and above-mentioned solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder and component 2, the component 3 of crossing 100 mesh sieves (levigate in case of necessity) mix, and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to temperature 70 C and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 130 and reference examples thereof

[embodiment 130-1,2 method for makings] component 3～4 is dissolved in altogether in suitable quantity of water and obtains solution, and above-mentioned solution spray or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 125～135 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Illustrate: be followed successively by meglumine, 1 except component 4 in embodiment 130-1 and reference examples, embodiment 130-2 and reference examples thereof, outside 2-bis-(lauroyl)-3-(N-acetyl group arginyl) glycerinate salt, other are all identical.

Embodiment 131 and reference examples thereof

[component 1 formula/sheet]: bark of Ramulus et folium taxi cuspidatae 50g Radix Ginseng Rubra 0.166g Radix Glycyrrhizae 0.500g

[embodiment 131-1 method for making] 1), preparation contains the solid dispersion (/ body) of component 1: above three flavor medical materials, bark of Ramulus et folium taxi cuspidatae is pulverized, cross 20 mesh sieves, according to the method under fluid extract and extractum item (appendix I O of Chinese Pharmacopoeia version in 2000), make solvent with 95% ethanol, flood after 48 hours, percolation slowly, the collection liquid of filtering, 40 ℃ of decompression recycling ethanols are to dry, add water and dichloromethane, fully be uniformly mixed, separate and collect dichloromethane solution after standing 4 hours, water liquid is used dichloromethane extraction 3 times again, merge dichloromethane solution each time, filter, the reclaim under reduced pressure dichloromethane is to dry, ethyl acetate-methanol for residue (3: 1) mixed solution dissolves, adding kieselguhr mixes thoroughly, removal of solvent under reduced pressure, pack in the percolation bucket, first use the normal hexane percolation, continue and use the dichloromethane percolation, collect the dichloromethane percolate, the reclaim under reduced pressure dichloromethane is to dry, residue dissolves with ethyl acetate, according to column chromatography (appendix VI C of Chinese Pharmacopoeia version in 2000), take silica gel as absorbent, n-hexane-acetone (75: 25) is eluant, eluting, the eluent that collection contains paclitaxel, decompression and solvent recovery is to doing to obtain dry extract (I), be crushed to approximately 80 orders, Radix Glycyrrhizae, red ginseng powder are broken into coarse powder, according to the method (appendix I O of Chinese Pharmacopoeia version in 2000) under fluid extract and extractum item, with 70% ethanol, make solvent, flood after 48 hours, slowly percolation, collect percolate, filter, filtrate is reclaimed solvent to doing to obtain dry extract (II), above-mentioned dry extract (I) dissolves with appropriate ethyl acetate, appropriate 80% dissolve with ethanol for above-mentioned dry extract (II), after above-mentioned two solution mix, add component 3 (Natrulon H-10 distearate) and component 4 (Capmul MCM C10) to dissolve, after mixing, solution spray or lyophilization obtain dry extract (III) (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm),

2), get component 2, component 5～7 80 mesh sieves excessively, add above-mentioned dry extract (III), mix, (divided dose of medicine shown in pressing (is every and contains Chinese medicine extract 167mg, or sheet weight=medicine (Chinese medicine extract) divided dose/medicine (Chinese medicine extract) accounts for the ratio that sheet is heavy, following examples herewith, no longer repeat)) be sub-packed in suitable bubble eye or tablet mould, be cooled to room temperature after being heated to 120 ℃ of temperature and being incubated 20 minutes and get final product.

[embodiment 131-2 method for making] 1), make dry dry extract (I) powder and dry extract (II) by embodiment 131-1 method for making 1;

2), be taken into component 3 (Natrulon H-10 distearate) and appropriate 80% dissolve with ethanol for component 4 (Capmul MCM C10), after mixing, solution spray or lyophilization obtain solid dispersion (/ body) powder (wherein the dispersate mean diameter is not more than 10nm);

3), get component 2, component 5～7 and dry extract (I) powder and dry extract (II) and cross 80 mesh sieves (pulverizing in case of necessity), add above-mentioned solid dispersion (/ body) powder, mix, standby with legal system by embodiment 131-1 afterwards.

[embodiment 131-1,2 reference examples method for makings] get dry extract (I), dry extract (II), component 2～7 80 mesh sieves excessively, mix, standby with legal system by embodiment afterwards.

Embodiment 131-3 and reference examples thereof

Except changing into component 4 Capmul MCM C10s in embodiment 131-1 and reference examples formula (and their method for making) thereof with the component 3 Natrulon H-10 distearates of its equivalent, (be that component 4 is removed, component 3 amounts increase to 17% by 12% liter), other comprise that method for making is all constant.

Every of this product contains bark of Ramulus et folium taxi cuspidatae in paclitaxel (C47H51No14), should be 4.5mg～5.5mg.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-10935(ZD-0935)-2002 is definite.)

Embodiment 132 and reference examples thereof

[component 1 formula/sheet]: fresh asparagus 15g

[embodiment 132-1 method for making] 1), get new fresh asparagus, clean, squeeze juice, juice is crossed 100 mesh sieves and is filtered, and gets filtrate, is spray dried to dry extract and obtains component 1; 2), component 3,4 heat fused, mix, cooling, pulverized 80 mesh sieves and obtained solid dispersion (/ body) (the dispersate mean diameter is not more than 1 μ m) powder; 3), get component 1～2, component 5 80 orders excessively, with above-mentioned solid dispersion (/ body) powder, mix, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.8kp, n=5), sheet is cooled to room temperature after being heated to 100 ℃ of temperature again and being incubated 5 minutes and gets final product.

[embodiment 132-1 reference examples method for making] got component 1～5 and crossed 80 mesh sieves, mixes, standby with legal system by embodiment afterwards.

Embodiment 132-2 and reference examples thereof

[formula], except component 4 in embodiment 132-1 and reference examples formula thereof being changed into to the component 3 (be that component 4 is removed, component 3 amounts increase to 10% by 6% liter) with its equivalent, other are all constant.

[embodiment 132-2 method for making] embodiment 132-1 is with the standby component 1 of legal system; 2), get component 3 heat fused, add said components 1, mix, cooling, pulverized 80 mesh sieves and obtained solid dispersion (/ body) (the dispersate mean diameter is not more than 1 μ m) powder; 3), get component 2, component 4 (Pulvis Talci) and cross 80 orders, with above-mentioned solid dispersion (/ body) powder, mix, it is standby with legal system that (other) press embodiment 132-1 afterwards.

[reference examples 132-2 method for making] got each component of embodiment and crossed 80 mesh sieves, mixes, standby with legal system by embodiment afterwards.

Every of this product contains total amino acids in glutamic acid (C5H9No4), must not be less than 6.0mg.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-10614(ZD-0614)-2002 is definite.)

Embodiment 133 and reference examples thereof

[component 1 formula/sheet]: Cornu Cervi Pantotrichum 0.036g Radix Polygoni Multiflori Preparata 0.750g Herba Epimedii 0.600g rhizoma Zingiberis 0.150g Radix Glycyrrhizae 0.075g Fructus Jujubae 0.150g

[embodiment 133-1 method for making] 1), preparation contains the solid dispersion (/ body) of component 1: above 6 flavor Chinese medicines, get Radix Polygoni Multiflori Preparata, Herba Epimedii, Rhizoma Zingiberis, Radix Glycyrrhizae, Fructus Jujubae, decoct with water secondary, each 2 hours, gradation filters, merging filtrate, it is 1.25～1.32(50 ℃ that filtrate is concentrated into relative density) extractum, add ethanol and make containing the alcohol amount to 50～55%, standing 24 hours, filter, reclaim ethanol, be concentrated into former extractum amount, adding ethanol makes containing the alcohol amount to 60～65%, standing 24 hours, filter filtrate for later use, Cornu Cervi Pantotrichum decocts with water five times, first, secondary each 4 hours, the 3rd, four times each 3 hours, the 5th time 2 hours, gradation filters, merging filtrate and to be concentrated into relative density be 1.20～1.25(70 ℃) extractum, add Cera Flava, standingly solidify fully to the wax layer, except the dewax layer, filter, add 80% ethanol 0.050ml, standing 48 hours, filter, filtrate recycling ethanol, being concentrated into relative density is 1.12～1.17(60 ℃) extractum, add 80% ethanol 0.070ml, stir evenly, standing 24 hours, filter, filtrate recovery section ethanol and above-mentioned filtrate merge, add the component 4 of half amount to dissolve, add component 2 to dissolve, mix, spray drying obtains dry extract (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm).

2), the component of second half amount 4 and the component 5 that adds fusing, mix, be crushed to 60～80 orders after cooling to obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm);

3), get component 3,6,7 and cross 80 mesh sieves, add above-mentioned dry extract and solid dispersion (/ body), mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is cooled to room temperature after being heated to 130 ℃ of temperature again and being incubated 2 minutes and gets final product.

[embodiment 133-2 method for making] 1), do not add component 4 and 2 other by embodiment 133-1 method for making 1 with the standby component 1 of legal system.

2), get component 4 and the component 5 that adds fusing, mix, be crushed to 60～80 orders after cooling to obtain solid dispersion (/ body) powder (the dispersate mean diameter is not more than 10nm);

3), get component 1～3,6～7 and cross 80 mesh sieves, add above-mentioned solid dispersion (/ body) powder, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is cooled to room temperature after being heated to 130 ℃ of temperature again and being incubated 2 minutes and gets final product.

Do not add component 4 during [reference examples method for making] component 1 preparation and 2 other are standby with legal system by embodiment; Get component 1～7 and cross 80 mesh sieves, mix, standby with legal system by embodiment afterwards.

Every of this product contains Radix Polygoni Multiflori Preparata with 2,3,5,4'-tetrahydroxystilbene-2-O-β-D glucoside (C ₂₀h ₂₂o ₉) meter, must not be less than 2.0mg.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-11154(ZD-1154)-2002 is definite.)

Embodiment 134 and reference examples thereof

[embodiment 134-1 method for making] 1), get component 3 heat fused, add micronized component 1 (mean diameter is 5～25 μ m approximately), mix, cooling rear pulverizing, cross 100 mesh sieves and obtain solid dispersion (/ body) powder (the dispersate mean diameter is not more than 25 μ m) powder; Above-mentioned powder mixes with the component 2,4～7 of crossing 80 mesh sieves, after mixing, with the about 1t/ pestle of tabletting pressure tabletting (sheet hardness 8kp, n=5), sheet is heated to 90 ℃ of insulations of temperature at least 3 hours again under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 134-2 method for making] got component 3 and is dissolved in appropriate ethanol-water (1: 1), with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 40～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 134-1 with method method for making (filling a prescription constant).

[reference examples method for making] got component 1～7 and crossed 80 mesh sieves, mixes, and presses afterwards embodiment with the standby reference examples of legal system.

Every of this product containing total flavonoids must not be less than 19.2mg, terpene lactone must not be less than 4.8mg.(component 1 meets China national Drug Administration standard (trying): WS-11490(ZD-1490)-2002 regulations.)

Embodiment 135 and reference examples thereof

[component 1 formula/sheet]: folium Eucommiae 6g

[method for making] 1), preparation contains the solid dispersion (/ body) of component 1: get Folium Eucommiae, decoct with water three times, 1 hour for the first time, second, third time each 45 minutes, collecting decoction, filter, it is 1.15～1.20(80 ℃ that filtrate decompression is concentrated into relative density) extractum, adding 5 times of amount ethanol stirs evenly, standing over night, filter, and filtrate is concentrated in right amount, add the component 5 of 2/3rds amounts to dissolve, spray drying obtains dry extract (in solid dispersion (/ body) powder, the dispersate mean diameter is not more than 10nm);

2), component 4 heat fused, add the component 5 of 1/3rd amounts, mix, cooling rear pulverizing, cross 80 mesh sieves, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 10nm) powder;

3), get component 2,3, cross 80 mesh sieves, add above-mentioned dry extract, solid dispersion (/ body) powder, mix, with the about 0.35t/ pestle of tabletting pressure tabletting (sheet hardness 3kp, n=5), sheet is heated to 55 ℃ of temperature again and is incubated 1 minute, is cooled to room temperature and gets final product.

[reference examples method for making] component 1 is standby with legal system by embodiment method for making 1 by other; Get the component 5 of component 1～4 and surplus (1/3rd amounts) and mix, cross 80 mesh sieves, mix, standby with legal system by embodiment afterwards.

Every of this product contains Folium Eucommiae with chlorogenic acid (C ₁₆h ₁₈o ₉) meter, must not be less than 0.50mg.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-10233(ZD-0233) 2002 is definite.)

Embodiment 136 and reference examples thereof

[component 1 formula/sheet]: herba Leonuri 1.25g

[method for making] 1), get Herba Leonuri, chopping, decoct with water secondary, each 2 hours, collecting decoction, filtered, filtrate is concentrated into the above extractum of the hydrochloric stachydrine 20mg of every 1g, with ethanol extraction three times, decompression recycling ethanol is to the dry dry extract that to obtain;

2), component 1 (above-mentioned dry extract), 2,3 water-soluble, spray drying must be containing solid dispersion (/ body) powder (the dispersate mean diameter the is not more than 10nm) powder of dry extract;

3), component 5 heat fused, add component 4, mix, cooling rear pulverizing, cross 80 mesh sieves and obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder;

4), get the thing that makes of method for making 2 and 3, add component 6, in pack into after mixing suitable bubble eye or tablet mould, be heated to 90 ℃ and be incubated 5 minutes after cooling, obtain.

[reference examples method for making] by embodiment method for making 1,2 with standby solid dispersion (/ body) powder (the dispersate mean diameter the is not more than 10nm) powder containing component 1,2,3 of legal system; Get component 4～6 and mix, cross 80 mesh sieves, add solid dispersion (/ body) powder, standby with legal system by embodiment after mixing.

Every of this product contains Herba Leonuri with stachydrine hydrochloride (C ₇h ₁₃nO ₂hCL) meter, should be 13.5mg～16.5mg.(component 1 formula and method for making 1 thereof: determine according to China national Drug Administration standard (trying): WS-11277 (ZD-1277)-2002.)

Embodiment 137 and reference examples thereof

[component 1 formula/sheet]: folium Caryophylli 1.1168g

[embodiment 137-1 method for making] 1), preparation contains the solid dispersion (/ body) of component 1: get Folium Caryophylli, decoct with water secondary, 2 hours for the first time, 1 hour for the second time, collecting decoction, filter, and Lv Ye Nong Shrink is to appropriate, add the component 3 of 40% amount to dissolve, mix rear spray drying and obtain dry extract (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm);

2), component 4 heat fused, add the i.e. component 3 of 60% amount of surplus, mix, cooling rear pulverizing, mistake 100 mesh sieves, obtain solid dispersion (/ body) powder (the dispersate mean diameter is not more than 10nm) powder; 3), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract, solid dispersion (/ body) powder, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 3 minutes, is cooled to room temperature and gets final product.

[embodiment 137-2 method for making] 1), get Folium Caryophylli, decoct with water secondary, 2 hours for the first time, 1 hour for the second time, collecting decoction, filtered, Lv Ye Nong Shrink is to appropriate, spray drying obtains dry extract;

2), component 4 heat fused, add component 3, mix, cooling rear pulverizing, cross 100 mesh sieves, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 10nm) powder;

3), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract, solid dispersion (/ body) powder, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 3 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] prepares the dry extract powder of component 1 by embodiment 137-2 method for making 1 same procedure; Separately get component 2～5, cross 80 mesh sieves; Mix above-mentioned each component, standby with legal system by embodiment afterwards.

Every of this product contains Folium Caryophylli with protocatechuic acid (C ₇h ₆o ₄) meter, must not be less than 0.20mg.(component 1 formula and method for making 1 thereof: determine according to China national Drug Administration standard (trying): WS-10679 (ZD-0679)-2002.)

Embodiment 138 and reference examples thereof

[component 1 formula/sheet]: herba Andrographis 1g

[embodiment 138-1 method for making] 1), preparation contains the solid dispersion (/ body) of component 1: get Herba Andrographis, be ground into coarse powder, with 80% alcohol reflux secondary, each 2 hours, merge extractive liquid,, filter, and filtrate adds component 3,4 to dissolve (being heated to 65 ℃), mix, spray drying obtains dry extract (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm);

2), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 138-2 method for making] 1), get Herba Andrographis, be ground into coarse powder, with 80% alcohol reflux secondary, each 2 hours, merge extractive liquid,, filtered, the filtrate spray drying obtains dry extract;

2), get component 3,4 use 80% ethanol (heating) dissolvings, dry solid dispersion (/ body) (wherein the dispersate mean diameter the is not more than 10nm) powder that obtains of solution spray;

3), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract and solid dispersion (/ body) powder, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 138-1,2 reference examples method for makings] prepare component 1 by embodiment 138-2 method for making 1 same procedure; Separately get component 2～5, mix, cross 80 mesh sieves, add component 1, mix, standby with legal system by embodiment afterwards.

Embodiment 138-3 and reference examples thereof

Except the component 3 (be that component 4 is removed, component 3 amounts increase to 23% by 8% liter) the middle component 4 of embodiment 138-1 and reference examples formula (and their method for making) thereof changed into its equivalent, other comprise that method for making is all constant.

Every of this product contains Herba Andrographis with andrographolide (C ₂₀h ₃₀o ₅) meter, must not be less than 2.1mg.(component 1 formula and method for making 1 thereof: determine according to China national Drug Administration standard (trying): WS-11355 (ZD-1355)-2002.)

Embodiment 139 and reference examples thereof

[component 1 formula/sheet]: flos wikstroemiae chamaedaphnes (Flos et follium wikstroemiae chamaedaphnis) 2g

[embodiment 139-1 method for making] 1), preparation contains the solid dispersion (/ body) of component 1: get Flos wikstroemiae chamaedaphnes (Flos et follium wikstroemiae chamaedaphnis), decoct with water secondary, each 1.5 hours, collecting decoction, filter, filtrate is concentrated in right amount, adds component 3 and 4 to dissolve, mix, spray drying obtains dry extract (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm);

2), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract, mix, with the about 0.11t/ pestle of tabletting pressure tabletting (sheet hardness 1kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 139-2 method for making] 1), get Flos wikstroemiae chamaedaphnes (Flos et follium wikstroemiae chamaedaphnis), decoct with water secondary, each 1.5 hours, collecting decoction, filtered, filtrate be concentrated into appropriate after spray drying obtain dry extract;

2), get component 3,4 use suitable quantity of water dissolvings, dry solid dispersion (/ body) (wherein the dispersate mean diameter the is not more than 10nm) powder that obtains of solution spray;

3), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract and solid dispersion (/ body) powder, mix, with the about 0.11t/ pestle of tabletting pressure tabletting (sheet hardness 1kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 139-1,2 reference examples method for makings] prepare component 1 by EXAMPLE Example 139-2 method for making 1 same procedure; Separately get component 2～5, cross 80 mesh sieves, add component 1, mix, standby with legal system by embodiment afterwards.

Embodiment 139-3 and reference examples thereof

Except the component 3 (be that component 4 is removed, component 3 amounts increase to 33% by 18% liter) the middle component 4 of embodiment 139-1 and reference examples formula (and their method for making) thereof changed into its equivalent, other comprise that method for making is all constant.

Embodiment 139-4 and reference examples thereof

Except the component 4 (be that component 3 is removed, component 4 amounts increase to 33% by 15% liter) the middle component 3 of embodiment 139-1 and reference examples formula (and their method for making) thereof changed into its equivalent, other comprise that method for making is all constant.

(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-11082(ZD-1082)-2002 is definite.)

Embodiment 140 and reference examples thereof

[component 1 formula/sheet]: Herba Reineckeae Carneae 0.300g Pericarpium Papaveris 0.200g Herba Ardisiae Japonicae 0.150g herba Saxifragae 0.150g Folium Eriobotryae 0.150g Cortex Mori 0.050g

[embodiment 140-1 method for making] preparation contains the solid dispersion (/ body) of component 1: above Six-element medical material, decoct with water secondary, each 2 hours, collecting decoction, filter, filtrate is concentrated in right amount, adds component 3 and 4 to dissolve, mix, spray drying obtains dry extract (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm); Get component 2 and cross 80 mesh sieves, add above-mentioned dry extract, mix, be loaded in suitable bubble eye or tablet mould, be cooled to room temperature after being heated to 90 ℃ of temperature and being incubated 30 minutes and get final product.

[embodiment 140-2 method for making] above Six-element medical material, decoct with water secondary, and each 2 hours, collecting decoction, filtered, and filtrate is concentrated into appropriate spray drying and obtains dry extract; Get component 3,4 use suitable quantity of water and dissolve, dry solid dispersion (/ body) (wherein the dispersate mean diameter the is not more than 10nm) powder that obtains of solution spray; Get component 2 and cross 80 mesh sieves, add above-mentioned dry extract and solid dispersion (/ body) powder, mix, be loaded in suitable bubble eye or tablet mould, be cooled to room temperature after being heated to 90 ℃ of temperature and being incubated 30 minutes and get final product.

[embodiment 140-1,2 reference examples method for makings] prepare component 1 by embodiment 140-2 same procedure; Separately get component 2～4, cross 80 mesh sieves, add component 1, mix, standby with legal system by embodiment afterwards.

Embodiment 140-3 and reference examples thereof

Except the component 3 (be that component 4 is removed, component 3 amounts increase to 30% by 20% liter) the middle component 4 of embodiment 140-1 and reference examples formula (and their method for making) thereof changed into its equivalent, other comprise that method for making is all constant.

Embodiment 140-4 and reference examples thereof

Except the component 4 (be that component 3 is removed, component 4 amounts increase to 30% by 10% liter) the middle component 3 of embodiment 140-1 and reference examples formula (and their method for making) thereof changed into its equivalent, other comprise that method for making is all constant.

Every of this product contains Pericarpium Papaveris with codeine phosphate (C ₁₈h ₂₁nO ₃h ₃pO ₄) meter, be no less than 25 μ g.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-10201(ZD-0201)-2002 is definite.)

Embodiment 141 and reference examples thereof

[component 1 formula/sheet]: zANGYINCHEN 1.120g

[embodiment 141-1 method for making] 1), preparation is containing the solid dispersion (/ body) of component 1: get 85% alcohol reflux three times for ZANGYINCHEN, each 3 hours, filter, merge extractive liquid,, filter, filtrate decompression is concentrated in right amount, adds component 3 and 4 to dissolve, mix, spray drying or vacuum drying become dry extract (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm);

2), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.1kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 141-2 method for making] 1), get 85% alcohol reflux three times for ZANGYINCHEN, each 3 hours, filter, merge extractive liquid,, filter, filtrate decompression is concentrated into appropriate spray drying or vacuum drying becomes dry extract;

2), the ethanol water of getting component 3 and 4 use appropriate 30～50% dissolves, and mixes, solution spray drying or vacuum drying become solid dispersion (/ body) powder (wherein the dispersate mean diameter is not more than 10nm);

3), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract and solid dispersion (/ body) powder, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.1kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 141-1,2 reference examples method for makings] prepare component 1 by embodiment 141-2 method for making 1 same procedure; Separately get component 2～5, cross 80 mesh sieves, add component 1, mix, standby with legal system by embodiment afterwards.

Embodiment 141-3 and reference examples thereof

Except the component 3 (be that component 4 is removed, component 3 amounts increase to 25% by 17% liter) the middle component 4 of embodiment 141-1 and reference examples formula (and their method for making) thereof changed into its equivalent, other comprise that method for making is all constant.

Embodiment 141-4 and reference examples thereof

Except the component 4 (be that component 3 is removed, component 4 amounts increase to 25% by 8% liter) component 3 in embodiment 141-1 and reference examples formula (and their method for making) thereof changed into its equivalent, reach in method for making sheet and be heated to again outside 163 ℃ of temperature, other are all constant.

Every of this product contains ZANGYINCHEN with oleanolic acid (C ₃₀h ₄₈o ₃) meter, must not be less than 3.5mg.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-11151(ZD-1151)-2002 is definite.)

Embodiment 142 and reference examples thereof

[component 1 formula/sheet]: bailey Myospalax Born 0.500g Herba Saussureae Involueratae 0.400g Flos Carthami 0.100g

[embodiment 142-1 method for making] 1), preparation contains the solid dispersion (/ body) of component 1: above three flavor medical materials, Bailey Myospalax Born is ground into coarse powder, decoct with water secondary, 8 hours for the first time, 4 hours for the second time, collecting decoction, filter, filtrate is concentrated in right amount, adds the 6-(.alpha.-D-galactosido)-D-glucose. of half amount and the Raffinose of half amount to dissolve, mix, be spray dried to extract powder (I) (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm); Herba Saussureae Involueratae is cataclasm to be mixed with Flos Carthami, decoct with water secondary, 2 hours for the first time, 1 hour for the second time, filter, filtrate is concentrated in right amount, adds the 6-(.alpha.-D-galactosido)-D-glucose. of surplus and Raffinose to dissolve, mix, be spray dried to extract powder (II) (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm); 2), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract (I) and (II), mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 105 ℃ of temperature again and is incubated 8 minutes, is cooled to room temperature and gets final product.

[embodiment 142-2 method for making] 1), above three flavor medical materials, Bailey Myospalax Born is ground into coarse powder, decocts with water secondary, 8 hours for the first time, 4 hours for the second time, collecting decoction, filtered, filtrate is concentrated into and is spray dried in right amount extract powder (I); Herba Saussureae Involueratae is cataclasm to be mixed with Flos Carthami, decocts with water secondary, and 2 hours for the first time, 1 hour for the second time, filter, filtrate is concentrated to being spray dried in right amount extract powder (II);

2), get component 3 and 4 use suitable quantity of water solution and dissolve, mix, solution spray drying or vacuum drying become solid dispersion (/ body) powder (wherein the dispersate mean diameter is not more than 10nm);

3), get component 2,5 and cross 80 mesh sieves, add above-mentioned dry extract (I), (II) and above-mentioned solid dispersion (/ body) powder, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 105 ℃ of temperature again and is incubated 8 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] prepares component 1 by EXAMPLE Example 142-2 method for making 1 same procedure; Separately get component 2～5, cross 80 mesh sieves, add component 1, mix, standby with legal system by embodiment afterwards.

Every containg sialon bone of this product, in isoleucine (C6H13NO2), must not be less than 0.20mg.(component 1 formula and method for making 1 thereof: according to China national Drug Administration standard (try): WS-10431(ZD-0431)-2002 is definite.)

Embodiment 143 and reference examples thereof

[embodiment 143-1 method for making] 1), the appropriate 90% ethanol heating for dissolving of component 1,3,4 use, mix, spraying or lyophilization become extract powder (solid dispersion (/ body) in dispersate mean diameter be not more than 100nm);

2), get component 2 and cross 80 mesh sieves, add above-mentioned dry extract, mix, add component 5, mix, be loaded in suitable bubble or tablet mould, be cooled to room temperature after being heated to 90 ℃ of temperature and being incubated 5 minutes and get final product.

[embodiment 143-2 method for making] 1), the appropriate 90% ethanol heating for dissolving of component 3,4 use, mix, the spraying or lyophilization become solid dispersion (/ body) powder (wherein the dispersate mean diameter is not more than 100nm);

2), get component 1,2 and cross 80 mesh sieves, add above-mentioned solid dispersion (/ body) powder, mix, add component 5, mix, be loaded in suitable bubble or tablet mould, be cooled to room temperature after being heated to 90 ℃ of temperature and being incubated 5 minutes and get final product.

[reference examples method for making] gets component 1～5, crosses 80 mesh sieves, mixes, standby with legal system by embodiment afterwards.

Component 1 (extract preparation) is carried out according to the preparation method of ministry of Health of China drug standard: WS3-B-1294-93 (the 7th the 27th page of Traditional Chinese medicine historical preparation) regulation.

Embodiment 144 and reference examples thereof

[component 1 formula/sheet]: Herba Taraxaci extract 0.125g Radix Scutellariae extract 0.025g radix Berberidis kunmingensis extract 0.025g Rhizoma Menispermi extract 0.025g

[method for making] component 3,4 heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder (the dispersate mean diameter is not more than 500nm) powder; Get component 1 each extract (according to the preparation method preparation of ministry of Health of China drug standard: WS3-B-2580-97 (the 13rd the 148th page of Traditional Chinese medicine historical preparation) regulation) and cross 100 mesh sieves, add the component 2 of crossing 100 mesh sieves, add above-mentioned solid dispersion (/ body) powder, mix, add component 5, mix, with the about 0.18t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 12 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, crosses 100 mesh sieves, mixes, standby with legal system by embodiment afterwards.

Embodiment 145 and reference examples thereof

[embodiment 145-1 method for making] 1), peanut hull meal is broken into coarse powder, with alcohol reflux 3 times, each 2 hours, filter, merging filtrate, being evaporated to relative density is the extractum of 1.40 (20 ℃); Get above-mentioned extractum 120mg, add the PEG2500 of 100mg and the erythritol of 30mg, heating makes it fusing, mix, solvent flashing is (solvent is less than 1%) to the material constant weight, be crushed to 100 orders (in solid dispersion (/ body), the dispersate mean diameter is not more than 100nm) after cooling, add again the appropriate silicon dioxide of crossing 100 mesh sieves to regulate material heavy to 350mg, mix, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.8kp, n=5), sheet is heated to 150 ℃ of temperature again and is incubated 2 minutes, is cooled to room temperature and gets final product.

[embodiment 145-2 method for making] 1), peanut hull meal is broken into coarse powder, with alcohol reflux 3 times, each 2 hours, filter, merging filtrate, being evaporated to relative density is the extractum of 1.40 (20 ℃); Get above-mentioned extractum 120mg, make dry extract and 100 mesh sieves; Get the PEG2500 of 100mg and the erythritol of 30mg, heating makes it fusing, mixes, and is crushed to 100 orders after cooling to obtain solid dispersion (/ body) (wherein the dispersate mean diameter is not more than 100nm); Mix above-mentioned dry extract and solid dispersion (/ body), add again the appropriate silicon dioxide of crossing 100 mesh sieves to regulate material heavy to 350mg, mix, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.8kp, n=5), sheet is heated to 150 ℃ of temperature again and is incubated 2 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] peanut hull meal is broken into coarse powder, uses alcohol reflux 3 times, and each 2 hours, filter, merging filtrate, being evaporated to relative density is the extractum of 1.40 (20 ℃); Getting above-mentioned extractum 0.12g makes dry powder and crosses 100 mesh sieves, add the PEG2500 of the 100mg that crosses 100 mesh sieves and the erythritol of 30mg, add again the appropriate silicon dioxide of crossing 100 mesh sieves to regulate material and weigh to 350mg, mix, standby with legal system by embodiment afterwards.

(component 1 Pericarppium arachidis hypogaeae extractum preparation is carried out according to the preparation method of ministry of Health of China drug standard: WS3-B-2390-97 (the 12nd the 138th page of Traditional Chinese medicine historical preparation) regulation.)

Embodiment 146 and reference examples thereof

[component 1 formula/sheet]: the dry peel of stem 2.250g of Long Ya Cortex araliae chinensis

[method for making] 1), get the dry peel of stem of Long Ya Cortex araliae chinensis, decoct with water three times, 3 hours for the first time, 2 hours for the second time, 2 hours for the third time, filter, merging filtrate, filter, filtrate concentrates and is spray dried to extract powder;

2), component 3,4 heat fused, mix, cooling, be crushed to 80～120 orders, obtain solid dispersion (/ body) powder (the dispersate mean diameter is not more than 100nm) powder, add the component 2,5 of crossing 80 mesh sieves, then add above-mentioned extract powder, mix, with the about 0.18t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] prepares the dry extract powder of component 1 by the embodiment same procedure; Separately get component 2～5, cross 80 mesh sieves, add above-mentioned dry extract powder, mix, standby with legal system by embodiment afterwards.

Component 1 extract preparation is carried out according to the preparation method of ministry of Health of China drug standard: WS3-B-2643-97 (the 13rd the 224th page of Traditional Chinese medicine historical preparation) regulation.

Embodiment 147 and reference examples thereof

[component 1 formula/sheet]: fructus Schisandrae Chinensis extractum 0.100g Radix Et Caulis Acanthopanacis Senticosi cream 0.050g

[embodiment 147-1 method for making] component 1,2,4, be dissolved in altogether or be scattered in appropriate 80% ethanol, and solution spray or lyophilization become extract powder (in solid dispersion (/ body), the dispersate mean diameter is not more than 10nm); After above-mentioned extract powder and component 3 mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.Component 1 each extract preparation is carried out according to the preparation method of ministry of Health of China drug standard: WS3-B-2529-97 (the 13rd the 90th page of Traditional Chinese medicine historical preparation) regulation.

[reference examples method for making] component 1～4, mix, standby with legal system by embodiment afterwards.

Embodiment 147-2 and reference examples thereof

Except component 4 in embodiment 147-1 and reference examples formula (and their method for making) thereof is changed into to the PEG-40 stearate, other comprise that method for making is all constant.

Embodiment 148 and reference examples thereof

※: component 1,2 meets ministry of Health of China drug standard: WS3-B-2527-97 (the 13rd the 88th page of Traditional Chinese medicine historical preparation) regulation.

[embodiment 148-1 method for making] component 4,5 heat fused, add and be micronized to the component 1 that mean diameter is not more than 5 μ m, mix, cooling, be crushed to 80～100 orders, obtain solid dispersion (/ body) powder (the dispersate mean diameter is not more than 100nm) coating powder; Get component 2,3,6 and cross 80 mesh sieves, add above-mentioned solid dispersion (/ body) powder and component 7, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 148-2 method for making] 1), get component 4,5 and be dissolved in suitable quantity of water, solution spray or lyophilization obtain solid and disperse or the coating powder; 2), get component 1,2,3,6 and cross 80 sieves, add above-mentioned solid to disperse or coating powder and component 7, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet be heated to 130～150 ℃ and be incubated 15 minutes after cooling, obtain.

[embodiment 148-3 method for making] 1), get component 4 and be dissolved in suitable quantity of water, be micronized to component 5 spray dryinges that are about 5～25 μ m and obtained solid coating powder being suspended in fluid bed with this liquid; 2), get component 1,2,3,6 and cross 80 sieves, add above-mentioned solid to disperse or coating powder and component 7, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet be heated to 120～140 ℃ and be incubated 15 minutes after cooling, obtain.

[reference examples method for making] component 1～7, mix, standby with legal system by embodiment afterwards.

Illustrate: in the following example and reference examples (formula) thereof divided by under outside the heterogeneity listed, other are all identical:

Embodiment 148-1 and reference examples component 3 thereof are maltose alcohol, and component 4 is sucrose monostearate, and component 5 is cholesterol ester stearic acid;

Embodiment 148-2 and reference examples component 3 thereof are spray drying mannitol, and component 4 is D-ribose, and component 5 is isoleucine-threonine-alanine tripeptides;

Embodiment 148-3 and reference examples component 3 thereof are the Gly-Leu dipeptides, and component 4 is 1,2,3,4,5-pentanepentol, and component 5 is maltose alcohol.

Embodiment 149 and reference examples thereof

[embodiment 149-1 method for making] component 4 heat fused, add component 3, mixes, and is crushed to 80～100 orders after cooling, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder; Get component 1,2,5,6 and cross 80 sieves, add above-mentioned solid dispersion (/ body) powder and component 7, in pack into after mixing suitable bubble or tablet mould, be heated to 80 ℃ and be incubated 15 minutes after cooling, obtain.

[embodiment 149-2 method for making] 1), get component 3,4 and be dissolved in suitable quantity of water, solution spray or lyophilization obtain solid and disperse or the coating powder; 2), get component 1,2,5,6 and cross 80 sieves, add above-mentioned solid to disperse or coating powder and component 7, in pack into after mixing suitable bubble or tablet mould, be heated to 130～160 ℃ and be incubated 15 minutes after cooling, obtain.

[embodiment 149-3 method for making] 1), get component 3 and be dissolved in suitable quantity of water, be micronized to component 4 spray dryinges that are about 1～5 μ m and obtained solid coating powder being suspended in fluid bed with this liquid; 2), get component 1,2,5,6 and cross 80 sieves, add above-mentioned solid to disperse or coating powder and component 7, in pack into after mixing suitable bubble or tablet mould, be heated to 120～140 ℃ and be incubated 15 minutes after cooling, obtain.

[reference examples method for making] gets component 1～7 mixing, crosses 80 mesh sieves, standby with legal system by embodiment after mixing.

Illustrate: in the following example and reference examples (formula) thereof divided by under outside the heterogeneity listed, other are all identical:

Embodiment 149-1 and reference examples component 1 thereof are the tea pigment dry extract, and component 2 is sweet-paddy dipeptides, and component 3 is the ethyl oleate, and component 4 is glyceryl monolaurate;

Embodiment 149-2 and reference examples component 1 thereof are the tea pigment dry extract, and component 2 is spray drying mannitol, and component 3 is 6-(.alpha.-D-galactosido)-D-glucose., and component 4 is three malt sugar group-beta-cyclodextrins;

Embodiment 149-3 and reference examples component 1 thereof are the Herba Leonuri dry extract powder, and component 2 is stachyose, and component 3 is lyxose, and component 4 is sulphur butyl-beta-schardinger dextrin-potassium salt.

★: tea pigment dry extract component 1: preparation is carried out according to the method for ministry of Health of China drug standard: WS3-B-2737-97 (the 14th the 100th page of Traditional Chinese medicine historical preparation) regulation.

◆: every of Herba Leonuri dry extract powder this product contains Herba Leonuri with stachydrine hydrochloride (C ₇h ₁₃nO ₂hCL) meter, should be 13.5mg～16.5mg.(component 1 formula and method for making 1 thereof: determine according to China national Drug Administration standard (trying): WS-11277 (ZD-1277)-2002.)

Embodiment 150 and reference examples thereof

[embodiment 150-1 method for making] 1), get Radix Fissistigmatis Glaucescentis appropriate, soak 12 hours, decoct with water three times, 2 hours for the first time, 1.5 hours for the second time, 1 hour for the third time, collecting decoction, filter component 1 that filtrate is concentrated into dry (moisture is less than 1%) (referring to the ministry of Health of China drug standard: WS3-B-3959-98 (the 20th the 277th page of Traditional Chinese medicine historical preparation)); 2), get component 2 and component 3 heat fused, add and be micronized to the component 1 that mean diameter is not more than 1 μ m, mix, cooling, be crushed to 80～100 orders, obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) coating powder 1; Get component 4,5 and cross 80 sieves, add above-mentioned solid powder 1 and component 6, in pack into after mixing suitable bubble or tablet mould, be heated to 110 ℃ and be incubated 25 minutes after cooling, obtain.

[embodiment 150-2 method for making] 1), press embodiment 150-1 with the standby component 1 of legal system; 2), get component 2,3 and be dissolved in suitable quantity of water, solution spray or lyophilization obtain solid and disperse or the coating powder; Get component 1,4,5 and cross 80 sieves, add above-mentioned solid to disperse or coating powder and component 6, in pack into after mixing suitable bubble or tablet mould, be heated to 130～160 ℃ and be incubated 15 minutes after cooling, obtain.

[embodiment 150-3 method for making] 1), press embodiment 150-1 with the standby component 1 of legal system; 2), get component 3 and be dissolved in suitable quantity of water, be micronized to component 2 spray dryinges that are about 1～5 μ m and obtained solid coating powder being suspended in fluid bed with this liquid; Get component 1,4,5 and cross 80 sieves, add above-mentioned solid coating powder and component 6, in pack into after mixing suitable bubble or tablet mould, be heated to 130～150 ℃ and be incubated 15 minutes after cooling, obtain.

[reference examples method for making] 1), press embodiment with the standby component 1 of legal system; 2), get component 1～5 and cross 80 sieves, add component 6, standby with legal system by embodiment after mixing.

Illustrate: in the following example and reference examples (formula) thereof divided by under outside the heterogeneity listed, other are all identical:

Embodiment 150-1 and reference examples component 2 thereof are PEG3500, and component 3 is xylitol, and component 4 is vicianose;

Embodiment 150-2 and reference examples component 2 thereof are anserine, and component 3 is rhamnose, and component 4 is spray-dried lactose;

Embodiment 150-3 and reference examples component 2 thereof are lysine glutamic acid dipeptides, and component 3 is sorbitol, and component 4 is calcium phosphate.

Embodiment 151 and reference examples thereof

[embodiment 151-1 method for making] 1), component 1,3,4 dissolves in appropriate 90% ethanol altogether, mixes, solution spray or lyophilization become solid dispersion (/ body) powder (wherein the dispersate mean diameter is not more than 10nm); Get component 2,5 and cross 80 mesh sieves, add above-mentioned powder and component 6, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 117 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 151-2 method for making] 1), component 3,4 dissolves in appropriate 90% ethanol altogether, mixes, solution spray or lyophilization become solid dispersion (/ body) powder (wherein the dispersate mean diameter is not more than 10nm); Get component 1,2,5 and cross 80 mesh sieves, add above-mentioned powder and component 6, mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 117 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 151-1,2 reference examples method for makings] get component 1～5, cross 80 mesh sieves, add component 6, mix, standby with legal system by embodiment afterwards.

Embodiment 151-3 and reference examples thereof

Except component 3,4 in embodiment 151-1 and reference examples formula (and their method for making) thereof is removed, change the PEG-100 octyl phenol ether of 20% amount into, other comprise that method for making is all constant.

Component 1 is pressed schisandrin B containing schizandrol and is calculated, must not be lower than 9.0%, according to the preparation method preparation of ministry of Health of China drug standard: WS3-B-3553-98 (the 19th the 33rd page of Traditional Chinese medicine historical preparation) regulation.

Embodiment 152 and reference examples thereof

[embodiment 152-1 method for making] component 1,3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 2,4 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 110 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 152-2 method for making] got component 3 and is dissolved in or is scattered in appropriate ethanol, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 90～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 152-1 with method method for making (filling a prescription constant).

[embodiment 152-3 method for making] got component 3 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 1/3rd amounts, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 152-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment afterwards.

Embodiment 153 and reference examples thereof

[embodiment 153-1 method for making] component 1,4 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 153-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 5～25 μ m obtain solid coating powder; Afterwards (other) by embodiment 153-1 with method method for making (filling a prescription constant).

[embodiment 153-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1/2nd amounts of 50～100 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 153-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 154 and reference examples thereof

[embodiment 154-1 method for making] component 1,3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Get the component 2,4～7 of crossing 100 mesh sieves (levigate in case of necessity) and mix with above-mentioned powder, after mixing, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 120 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 154-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 1～5 μ m obtain solid coating powder; Afterwards (other) by embodiment 154-1 with method method for making (filling a prescription constant).

[embodiment 154-3 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1/2nd amounts of 5～25 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,4～7 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 154-1 with method method for making (filling a prescription constant).

[reference examples method for making] got component 1～7 and crossed 100 mesh sieves (levigate in case of necessity) and mix, standby with legal system by embodiment after mixing.

Embodiment 155 and reference examples thereof

[embodiment 155-1 method for making] gets component 4 heat fused, adds the component 1 that is micronized to 500 orders (mean diameter is 5～25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated 30 minutes, is cooled to room temperature and gets final product.

[embodiment 155-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 20～40 μ m obtain solid coating powder; Afterwards (other) by embodiment 155-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 156 and reference examples thereof

[embodiment 156-1 method for making] gets component 4, and heat fused adds by appropriate alcohol-soluble component 1, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3,5～6 of crossing 100 mesh sieves (levigate in case of necessity), adds component 7, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 95 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 156-2 method for making] got component 4 and is dissolved in or is scattered in appropriate hot water, adds component 1, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 156-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 7, standby with legal system by embodiment after mixing.

Embodiment 157 and reference examples thereof

[embodiment 157-1 method for making] gets component 5, and heat fused adds by appropriate alcohol-soluble component 1, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 2～4 of crossing 100 mesh sieves, adds component 6, mixes, and with the about 1.9t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 157-2 method for making] got component 5 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to approximately 0.6～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder 1; Afterwards (other) by embodiment 157-1 with method method for making (filling a prescription constant).

[embodiment 157-3 method for making] got component 5 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,4 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, adds component 6, mix, afterwards (other) by embodiment 157-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, standby with legal system by embodiment after mixing.

Embodiment 158 and reference examples thereof

[method for making] gets component 3, and heat fused adds component 1, and heating makes it to dissolve fully, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder 1; Get component 2,4～7 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, after mixing, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 95 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 159 and reference examples thereof

[embodiment 159-1 method for making] got the appropriate hot ethanol of component 4 use and dissolved, and adds the component 1 with appropriate acetic acid ethyl dissolution, mixes, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 159-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 159-1 with method method for making (filling a prescription constant).

[embodiment 159-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 159-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 160 and reference examples thereof

[embodiment 160-1 method for making] got the appropriate hot ethanol of component 4 use and dissolved, and adds the component 1 with appropriate acetic acid ethyl dissolution, mixes, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 160-2 method for making] gets component 4 heat fused, adds component 1, makes it to be micronized to the about 100nm of mean diameter～1 μ m, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 160-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 161 and reference examples thereof

[method for making] got the appropriate hot ethanol of component 4 use and dissolved, and adds the component 1 with appropriate ether dissolution, mixes, and solution component 2 spray dryinges of crossing 100 mesh sieves (levigate in case of necessity) to 40% amount in fluid bed obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 3 of crossing 100 mesh sieves and the component 2 of surplus, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 110 ℃ of temperature again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Embodiment 162 and reference examples thereof

[embodiment 162-1 method for making] gets component 4, and heat fused adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 110 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 162-2 method for making] got component 4 and is dissolved in appropriate hot water, adds component 1, makes it to be micronized to approximately 50～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 162-1 with method method for making (filling a prescription constant).

[embodiment 162-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 162-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 163 and reference examples thereof

[embodiment 163-1 method for making] gets the appropriate dissolve with ethanol of component 3, adds the component 1 with appropriate ether dissolution, mixes, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 2,4 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 110 ℃ of temperature again and is incubated at least 5 hours under vacuum, until component 4 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 163-2 method for making] got component 3 and is dissolved in appropriate ethanol, adds component 1, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 163-1 with method method for making (filling a prescription constant).

[embodiment 163-3 method for making] got component 3 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 1/3rd amounts, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 163-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 164 and reference examples thereof

[embodiment 164-1 method for making] gets component 4, and heat fused adds the component 1 with appropriate ether dissolution, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 164-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 164-1 with method method for making (filling a prescription constant).

[embodiment 164-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 50～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 164-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 165 and reference examples thereof

[embodiment 165-1 method for making] gets the appropriate dissolve with ethanol of component 3, adds the component 1 with appropriate ether dissolution, mixes, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Get component 2,4～7 and mix, cross 100 mesh sieves (levigate in case of necessity), after mixing, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 165-2 method for making] got component 3 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 1/3rd amounts, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4～7 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 165-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 166 and reference examples thereof

[embodiment 166-1 method for making] gets the appropriate dissolve with ethanol of component 4, adds the component 1 of dissolving by proper amount of acetone, mixes, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 110 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 166-2 method for making] got component 4 and is dissolved in or is scattered in appropriate hot water, adds component 1, makes it to be micronized to the about 100nm of mean diameter～1 μ m, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 166-1 with method method for making (filling a prescription constant).

[embodiment 166-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 0.6～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 166-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 167 and reference examples thereof

[embodiment 167-1 method for making] gets component 4, and heat fused adds the component 1 with appropriate dissolve with ethanol, mixes, and flings to solvent, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 100 ℃ of temperature and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 167-2 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 40% amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 167-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 168 and reference examples thereof

The material of the common drying that Advantose FS95Fructose(is 95% fructose and 5% starch)

[method for making] gets component 4, and heat fused adds the component 1 with appropriate dissolve with ethanol, mixes, and flings to after solvent coolingly, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder reaches with component 2 component 3,5 of crossing 100 mesh sieves (levigate in case of necessity) to be mixed, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～5, crosses 100 mesh sieves (levigate in case of necessity), adds component 2, mixes, standby with legal system by embodiment after mixing.

Embodiment 169 and reference examples thereof

[method for making] component 1,3 is dissolved in altogether appropriate ethanol and obtains solution, in fluid bed, with above-mentioned solution, component 2 spray dryinges of mistake 100 mesh sieves (levigate in case of necessity) of 60% amount that suspends is obtained to solid dispersion (/ body) powder; Above-mentioned powder mixes with component 2 and the component 4 of the surplus of crossing 100 mesh sieves (levigate in case of necessity), mix afterwards with the about 0.17t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 170 and reference examples thereof

MicroceLac100, from Meggle excipients& The spray drying solid that contains 75% alpha-lactose monohydrate and 25% microcrystalline Cellulose of technology

[embodiment 170-1 method for making] gets component 3, and heat fused adds the component 1 that is micronized to 500 orders (mean diameter is 25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder and component 2 mix, and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 150 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 170-2 method for making] got component 1,3 and is dissolved in appropriate ethanol, and solution spray obtains solid coating powder; Afterwards (other) by embodiment 170-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1,3, crosses 100 mesh sieves (levigate in case of necessity), adds component 2, mixes, standby with legal system by embodiment after mixing.

Embodiment 171 and reference examples thereof

[method for making] gets component 4, and heat fused adds the component 1 that is micronized to 150～160 orders (mean diameter is 100 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Embodiment 172 and reference examples thereof

t, the maltodextrin of Roquette American Inc. and spray-dired glucose

[embodiment 171-1 method for making] gets component 3, and heat fused adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 1～5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with component 2, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 100 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 172-2 method for making] got component 3 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to the about 100nm of mean diameter～1 μ m, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 171-1 with method method for making (filling a prescription constant).

[reference examples method for making] got component 1,3 and crossed 100 mesh sieves (levigate in case of necessity), adds component 2, mixes, standby with legal system by embodiment after mixing.

Embodiment 173 and reference examples thereof

[embodiment 173-1 method for making] gets component 3, and heat fused adds the component 1 that is micronized to 6000～10000 orders (1～2 μ m), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Get component 2,4～7 and mix, cross 100 mesh sieves (levigate in case of necessity), after mixing, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 173-2 method for making] got component 3 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to the about 100nm of mean diameter～1 μ m, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 173-1 with method method for making (filling a prescription constant).

[embodiment 173-3 method for making] got component 3 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4～7 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 173-1 with method method for making (filling a prescription constant).

[reference examples method for making] got component 1～7 and crossed 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Embodiment 174 and reference examples thereof

[embodiment 174-1 method for making] component 1 and component 4 are dissolved in appropriate ethanol-acetone (1:1) solution altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with component 2 and the component 3,5 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.8kp, n=5), sheet is heated to temperature 50 C again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 174-2 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 30% amount, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 174-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Embodiment 175 and reference examples thereof

[method for making] component 1 and component 4 are dissolved in appropriate hot ethanol altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder mixes with the component 2～3,5～7 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 110 ℃ of temperature again and is incubated at least 1 hour under vacuum, until component 7 volatilizations are complete, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 176 and reference examples thereof

Cellactose80, from Meggle excipients& The spray-dired compound formed by 75% alpha-lactose monohydrate and 25% cellulose powder of technology

[embodiment 176-1 method for making] gets component 3, and heat fused adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with component 2,4,5 and component 6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 176-2 method for making] got component 3 and is dissolved in appropriate hot water, adds component 1, makes it to be micronized to the about 100nm of mean diameter～1 μ m, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 176-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, standby with legal system by embodiment after mixing.

Embodiment 177 and reference examples thereof

[method for making] component 1,3 is dissolved in appropriate hot ethanol altogether, and solution component 2 spray dryinges to mistake 100 mesh sieves (levigate in case of necessity) of 50% amount in fluid bed obtain solid powder 1; Above-mentioned powder 1 mixes with component 2 and the component 4,5 of the surplus of crossing 100 mesh sieves (levigate in case of necessity), mix, with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 25 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] got the component 1～5 of 100 mesh sieves (levigate in case of necessity), mixed, and mixed, standby with legal system by embodiment afterwards.

Embodiment 178 and reference examples thereof

[embodiment 178-1 method for making] gets component 4, and heat fused adds the component 1 that is micronized to 500 orders (mean diameter is 25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 115 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 178-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 1～5 μ m obtain solid coating powder; Afterwards (other) by embodiment 178-1 with method method for making (filling a prescription constant).

[embodiment 178-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 40% amount of 60～100 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 178-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 179 and reference examples thereof

[embodiment 179-1 method for making] gets component 3, and heat fused adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,4～6 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 95 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 179-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 60～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 179-1 with method method for making (filling a prescription constant).

[embodiment 179-3 method for making] got component 3 and is dissolved in suitable quantity of water, adds the component 2 of half amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4～6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 179-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment afterwards.

Embodiment 180 and reference examples thereof

[embodiment 180-1 method for making] got component 1,3 and used appropriate ether dissolution, and solution spray or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2,4～6 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to temperature 60 C again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 180-2 method for making] got component 3 and is dissolved in or is scattered in appropriate hot water, adds and is micronized to the approximately component 1 of 90～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 180-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 181 and reference examples thereof

[embodiment 181-1 method for making] got the appropriate distilled water of component 3 use and dissolved, and adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mixes, and this liquid spraying or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2,4～5 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 181-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1/2nd amounts of 5～25 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,4～5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 181-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 182 and reference examples thereof

[embodiment 182-1 method for making] got the appropriate distilled water of component 1,4 use and dissolved, and mixes, and this liquid spraying or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2,3,5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 150 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 182-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1/2nd amounts of 5～25 μ m obtain solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 182-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 183 and reference examples thereof

[embodiment 183-1 method for making] component 1,4 is dissolved in appropriate hot ethanol altogether, and solution spray or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 95 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 183-2 method for making] got component 4 and is dissolved in or is scattered in appropriate hot water, adds and is micronized to the approximately component 1 of 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 183-1 with method method for making (filling a prescription constant).

[embodiment 183-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 183-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 184 and reference examples thereof

[embodiment 184-1 method for making] component 1,4 is dissolved in appropriate ethanol altogether, and solution spray or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 100 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 184-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds and is micronized to the approximately component 1 of 90～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 184-1 with method method for making (filling a prescription constant).

[embodiment 184-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 30% amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 184-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 185 and reference examples thereof

[embodiment 185-1 method for making] component 1 is approximately used the dissolve with ethanol of 10 times of its volumes, and component 4 is approximately dissolved with the distilled water of 2 times of its volumes, and two liquid mix, and mix rear spray drying and obtain solid powder 1; Above-mentioned powder mixes with the component 2,3,5,6 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 130 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 185-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds and is micronized to the approximately component 1 of 90～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 185-1 with method method for making (filling a prescription constant).

[embodiment 185-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 25% amount, makes it to be micronized to approximately 0.6～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5,6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 185-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 186 and reference examples thereof

[embodiment 186-1 method for making] component 1,4 is dissolved in appropriate ethanol altogether, and solution spray or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 100 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 186-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 186-1 with method method for making (filling a prescription constant).

[embodiment 186-3 method for making] got component 4 and is dissolved in or is scattered in appropriate ethanol, adds the component 2 of 25% amount, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 186-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 187 and reference examples thereof

[embodiment 187-1 method for making] component 1,4 is dissolved in appropriate water, the spray-dried powder 1 that obtains of solution; Above-mentioned powder 1 mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 160 ℃ of temperature and is incubated 3 minutes, is cooled to room temperature and gets final product.

[embodiment 187-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 187-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 188 and reference examples thereof

[method for making] component 1,3 is dissolved in appropriate water, the spray-dried powder 1 that obtains of solution; Above-mentioned powder mixes with component 2,4, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 145 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, standby with legal system by embodiment after mixing.

Embodiment 189 and reference examples thereof

[embodiment 189-1 method for making] component 1,4 is dissolved in appropriate water, the spray-dried powder 1 that obtains of solution; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 150 ℃ of temperature again and is incubated at least 0.5 hour under vacuum, until component 5 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 189-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 90～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 189-1 with method method for making (filling a prescription constant).

[embodiment 189-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 189-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 190 and reference examples thereof

[embodiment 190-1 method for making] component 1,4,5 is dissolved in appropriate water, the spray-dried powder 1 that obtains of solution; Above-mentioned powder mixes with the component 2～3,6 of crossing 100 mesh sieves (levigate in case of necessity), with the about 0.8t/ pestle of tabletting pressure tabletting (sheet hardness 5kp, n=5), sheet is heated to 120 ℃ of temperature again and is incubated at least 1 hour under vacuum, until component 6 volatilizations are complete, are cooled to room temperature and get final product.

[embodiment 190-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3,5,6 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 190-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 191 and reference examples thereof

[embodiment 191-1 method for making] component 1,4,5 is dissolved in appropriate water, the spray-dried powder 1 that obtains of solution; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 150 ℃ of temperature again and is incubated 30 minutes, is cooled to room temperature and gets final product.

[embodiment 191-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 191-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 192 and reference examples thereof

[embodiment 192-1 method for making] gets component 3, and heat fused adds the component 1 that is micronized to 6000～10000 orders (1～2 μ m), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,4,5,6 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.25t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 20 minutes, is cooled to room temperature and gets final product.

[embodiment 192-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 5～25 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,4,5,6 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 192-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment afterwards.

Embodiment 193 and reference examples thereof

[embodiment 193-1 method for making] gets component 4, and heat fused adds the component 1 that is micronized to 500 orders (mean diameter is 25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder 1 mixes with component 2,3,5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 193-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 25 μ m obtain solid coating powder; Afterwards (other) by embodiment 193-1 with method method for making (filling a prescription constant).

[embodiment 193-3 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1～5 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 193-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 194 and reference examples thereof

[embodiment 194-1 method for making] gets component 3, and heat fused adds and is micronized to the approximately component 1 of 1～5 μ m of about mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,4,5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 140 ℃ of temperature and is incubated 35 minutes, is cooled to room temperature and gets final product.

[embodiment 194-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1～5 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,4,5 of crossing 100 mesh sieves (levigate in case of necessity), afterwards (other) by embodiment 194-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 195 and reference examples thereof

[embodiment 195-1 method for making] gets component 4 heat fused, then adds and be micronized to the approximately component 1 of 1～5 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains the solid powder; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5, mixes, and with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 195-2 method for making] got component 4 and is dissolved in suitable quantity of water, with this liquid to being suspended in fluid bed of 1/3rd amounts be micronized to mean diameter approximately component 2 spray dryinges of 1～5 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 5, mix, afterwards (other) by embodiment 195-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 196 and reference examples thereof

[embodiment 196-1 method for making] gets component 3 heat fused, then adds and be micronized to the approximately component 1 of 6000～10000 orders (1～2 μ m), mixes, cooling, is crushed to 100～120 orders, obtains the solid powder; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), adds component 4, mixes, and with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 196-2 method for making] got component 3 and is dissolved in appropriate ethanol, adds the component 2 of 1/4th amounts, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 4, mix, afterwards (other) by embodiment 196-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 197 and reference examples thereof

[embodiment 197-1 method for making] gets component 3, and heat fused adds and is micronized to the approximately component 1 of 2000～4000 orders (mean diameter is 5 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,4,5,6 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 197-2 method for making] got component 3 and is dissolved in appropriate ethanol, adds the component 2 of 1/2nd amounts, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4～6 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 197-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 198 and reference examples thereof

[embodiment 198-1 method for making] got component 4 use suitable quantity of water and dissolved, add the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), after mixing in fluid bed 100 mesh sieves (levigate in case of necessity) of mistake component, 2 spray dryinges to 50% amount that suspends obtain solid powder 1; Above-mentioned powder mixes with component 2 and the component 3 of crossing the surplus of 100 mesh sieves (levigate in case of necessity), adds component 5, mixes, with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 100～150 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 198-2 method for making] got component 4 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5, mix, afterwards (other) by embodiment 198-1 with method method for making (filling a prescription constant).

[embodiment 198-3 method for making] got component 4 and is dissolved in appropriate ethanol, adds the component 2 of 1/4th amounts, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 5, mix, afterwards (other) by embodiment 198-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 199 and reference examples thereof

[embodiment 199-1 method for making] got component 1,3,4 and is dissolved in altogether suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder mixes with the component 2 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 199-2 method for making] got component 3,4 and is dissolved in altogether suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder mixes with the component 1,2 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2,5, standby with legal system by embodiment after mixing.

Embodiment 200 and reference examples thereof

The appropriate hot ethanol of [embodiment 200-1 method for making] component 1,3 use dissolves, and solution spray or lyophilization obtain solid powder 1; Above-mentioned powder mixes with the component 2,4～7 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.3t/ pestle of tabletting pressure tabletting (sheet hardness 2.3kp, n=5), sheet is heated to 110 ℃ of temperature and is incubated 7 minutes, is cooled to room temperature and gets final product.

[embodiment 200-2 method for making] got component 3 and is dissolved in suitable quantity of water, adds component 1, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 200-1 with method method for making (filling a prescription constant).

[embodiment 200-3 method for making] got component 3 and is dissolved in suitable quantity of water, adds the component 2 of 1/4th amounts, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; The component 2 of above-mentioned powder and the component 1,4～7 of crossing 100 mesh sieves (levigate in case of necessity) and surplus is mixed to even, afterwards (other) by embodiment 200-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 201 and reference examples thereof

[embodiment 201-1 method for making] component 1,4 is dissolved in appropriate hot ethanol, the spray-dried powder 1 that obtains of solution; Above-mentioned powder 1 mixes with the component 2,3,5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 150 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 201-2 method for making] got component 4 and is dissolved in or is scattered in appropriate hot water, adds component 1, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Afterwards (other) by embodiment 201-1 with method method for making (filling a prescription constant).

[embodiment 201-3 method for making] got component 4 and is dissolved in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 5～25 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, afterwards (other) by embodiment 201-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 202 and reference examples thereof

[embodiment 202-1 method for making] component 1,4 is dissolved in appropriate ethanol, and spray drying after solution, obtain powder 1; Above-mentioned powder 1 mixes with component 2,3,5, after mixing with the about 0.3t/ pestle of tabletting pressure tabletting (sheet hardness 2.3kp, n=5),, then be heated to 150 ℃ of temperature and be incubated 30 minutes, be cooled to room temperature and get final product.

[embodiment 202-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds the component 2 of half amount, makes it to be micronized to approximately 70～100 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, afterwards (other) by embodiment 202-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 203 and reference examples thereof

[embodiment 203-1 method for making] component 1,4 is dissolved in appropriate ethanol, the spray-dried powder 1 that obtains of solution; Above-mentioned powder 1 mixes with the component 2,3,5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 110 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 203-2 method for making] got component 4 and is dissolved in or is scattered in appropriate hot water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 90～100 μ m obtain solid coating powder; Afterwards (other) by embodiment 203-1 with method method for making (filling a prescription constant).

[embodiment 203-3 method for making] got component 4 and is dissolved in appropriate ethanol, adds the component 2 of 1/3rd amounts, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, afterwards (other) by embodiment 203-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 204 and reference examples thereof

Appropriate 70% ethanol (aqueous solution) of [embodiment 204-1 method for making] component 5 use dissolves, in fluid bed to suspend be micronized to mean diameter approximately component 1 spray drying of 80～100 μ m obtain solid powder 1; Above-mentioned powder mixes with the component 2～4 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.6kp, n=5), sheet is heated to 120 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 204-2 method for making] got component 1,5 and is dissolved in altogether or is scattered in appropriate 70% ethanol (aqueous solution), and this liquid of spray drying obtains solid coating powder; Afterwards (other) by embodiment 204-1 with method method for making (filling a prescription constant).

[embodiment 204-3 method for making] got component 5 and is dissolved in appropriate ethanol, adds the component 2 of 1/5th amounts, makes it to be micronized to approximately 1～5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,4 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 6, mix, afterwards (other) by embodiment 204-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 205 and reference examples thereof

[embodiment 205-1 method for making] component 1,4 shares appropriate ethanol and dissolves, and mixes rear spray drying and obtains solid powder 1; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to temperature 70 C again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 205-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds the component 2 of 1/2nd amounts, makes it to be micronized to mean diameter and is about 5～25 μ m, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3,5 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, afterwards (other) by embodiment 205-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 206 and reference examples thereof

[embodiment 206-1 method for making] component 4 use are the water dissolution of 10 to 20 times of its volumes approximately, adds the component 1 that is micronized to 2000～4000 orders (mean diameter is 5 μ m approximately), mixes rear spray drying and obtains solid powder 1; Above-mentioned powder mixes with the component 2～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 5, mixes, and with the about 0.26t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 100 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 206-2 method for making] got component 4 and is dissolved in appropriate ethanol, adds the component 2 of 1/3rd amounts, makes it to be micronized to mean diameter and is about 5～25 μ m, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,3 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 5, mix, afterwards (other) by embodiment 206-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 207 and reference examples thereof

[embodiment 207-1 method for making] component 3 use are the water dissolution of 10 to 50 times of its volumes approximately, adds and is micronized to the approximately component 1 of 6000～10000 orders (1～2 μ m), mixes rear spray drying and obtains solid powder 1; Above-mentioned powder mixes with the component 2,4～5 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 120 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 207-2 method for making] got component 3 and is dissolved in suitable quantity of water, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 2 spray dryinges of 1/3rd amounts of 90～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1,4,5 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, afterwards (other) by embodiment 207-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 208 and reference examples thereof

[embodiment 208-1 method for making] component 1,4 is dissolved in appropriate hot ethanol, and spray drying after solution obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 0.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.7kp, n=5), sheet is heated to 120～160 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 208-2 method for making] got component 4 and is dissolved in appropriate hot alcohol, gets component 5 and is dissolved in appropriate hot water, and two liquid sprays mix the dry solid coating powder that obtains of rear mist; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, and (other) press embodiment 208-1 with the method method for making afterwards.

[embodiment 208-3 method for making] gets component 4 heat fused, adds the component 5 that is micronized to 500 orders (mean diameter is 25 μ m approximately), mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mix, afterwards (other) by embodiment 208-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, standby with legal system by embodiment afterwards.

Illustrate: in embodiment 208-1 and reference examples, embodiment 208-2 and reference examples thereof, embodiment 208-3 and reference examples thereof, except component 4 is followed successively by xylitan monostearate, xylitan monostearate, cera alba, other are all identical.

Embodiment 209 and reference examples thereof

[embodiment 209-1 method for making] got component 1,3 and is dissolved in appropriate hot ethanol, the spray-dried powder that obtains of solution; Above-mentioned powder mixes with the component 2,4,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 110 ℃ of temperature and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 209-2 method for making] got component 3 and is dissolved in or is scattered in appropriate hot alcohol, adds the component 2 of 1/2nd amounts, makes it to be micronized to mean diameter and is about 5～25 μ m, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with the component 1,4,5 of crossing 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus, adds component 6, mix, afterwards (other) by embodiment 209-1 with method method for making (filling a prescription constant).

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, standby with legal system by embodiment afterwards.

Embodiment 210 and reference examples thereof

[method for making] component 1～3 is total to molten or is scattered in suitable quantity of water, and solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 4,5, heat fused, mix, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 2; Pack into after above-mentioned powder 1,2 mixes in suitable bubble eye or tablet mould, then be heated to 75 ℃ of temperature and be incubated 5 minutes, be cooled to room temperature and get final product.

[reference examples method for making] component 1～3 is total to molten or is scattered in suitable quantity of water, and solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 4～5 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, after mixing, (other) are standby with legal system by embodiment.

Embodiment 211 and reference examples thereof

[embodiment 211-1,2 method for makings] get component 4, and heat fused adds and is micronized to the approximately component 5 of 5～25 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 211-3 method for making] gets component 4, and heat fused adds and is micronized to the approximately component 1 of 1～5 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder and component 2～3, the 5(sodium glycine carbonate of crossing 100 mesh sieves (levigate in case of necessity)) mix, mix, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

In embodiment 211-1, component 5 is aluminium oxide, and in embodiment 211-2,3, component 5 is sodium glycine carbonate, and other are identical.

Embodiment 212 and reference examples thereof

[method for making] gets component 3～5, and heat fused mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 1～2,6～9 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, mix afterwards with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～9, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 213 and reference examples thereof

[embodiment 213-1 method for making] gets component 4,5, and heat fused adds and is micronized to the approximately component 3 of 70～100 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～2,6,7 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to temperature 70 C again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[embodiment 213-2 method for making] gets component 4,5, and heat fused adds and is micronized to the approximately component 1 of 5～25 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2,3,6,7 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to temperature 70 C again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 214 and reference examples thereof

[embodiment 214-1 method for making] gets component 4, and heat fused adds and is micronized to the approximately component 5 of 5～25 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 75 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 214-2 method for making] gets component 4, and heat fused adds and is micronized to the approximately component 1 of 1～5 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 85 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 215 and reference examples thereof

[embodiment 215-1 method for making] gets component 4, and heat fused adds and is micronized to the approximately component 5 of 1～5 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 215-2 method for making] gets component 4, and heat fused adds appropriate alcohol-soluble component 1, mixes, and flings to after solvent coolingly, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), adds component 6, mixes, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 6, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 216 and reference examples thereof

[method for making] gets component 3, and heat fused adds and is micronized to the approximately component 4 of 1～5 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion (/ body) powder; Above-mentioned powder mixes (levigate in case of necessity) with component 1,2, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to temperature 70 C again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 217 and reference examples thereof

(from RoquetteAmerican, the spray drying solid that contains 15% corn starch and 85% alpha-lactose monohydrate of Inc.)

[method for making] component 4 and component 5 are dissolved in altogether or are scattered in appropriate hot water, and solution or dispersion liquid spray drying obtain that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 100nm) powder 1; Above-mentioned powder 1 mixes (levigate in case of necessity) with component 1 and 2, adds component 3 to mix, and adds component 6 to mix, with the about 1.1t/ pestle of tabletting pressure tabletting (sheet hardness 0.8kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), add component 6 mix after (other) standby with legal system by embodiment.

Embodiment 218 and reference examples thereof

[embodiment 218-1 method for making] component 3 and component 4 are dissolved in altogether or are scattered in appropriate hot water, and solution or dispersion liquid spray drying or lyophilization obtain that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 100nm) powder 1; Above-mentioned powder with cross 100 mesh sieves) component 1 and component 2 mix (levigate in case of necessity, mix, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 25 minutes, is cooled to room temperature and gets final product.

[embodiment 218-2 method for making] component 1 and component 3 are dissolved in altogether or are scattered in appropriate hot water, and solution or dispersion liquid spray drying or lyophilization obtain that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 500nm) powder 1; Above-mentioned powder with cross 100 mesh sieves) component 2 and component 4 mix (levigate in case of necessity, mix, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 25 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 219 and reference examples thereof

100 (from Meggle excipients& The spray drying solid that contains 75% alpha-lactose monohydrate and 25% microcrystalline Cellulose of technology)

[method for making] component 1,3～4 is dissolved in altogether or is scattered in appropriate hot water and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder and component 2 mix, and in pack into after mixing suitable bubble eye or tablet mould, then are heated to 90 ℃ of temperature and are incubated 25 minutes, are cooled to room temperature and get final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 220 and reference examples thereof

The material of the common drying that Advantose FS95Fructose(is 95% fructose and 5% starch).

[method for making] component 4～5 is dissolved in altogether or is scattered in appropriate hot water and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with component 1,2 and the component 3 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 75 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,2,4,5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 3, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 221 and reference examples thereof

[embodiment 221-1 method for making] component 4～5 is dissolved in altogether or is scattered in appropriate hot water and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,3 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90～100 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[embodiment 221-2 method for making] component 1,4 is dissolved in altogether or is scattered in appropriate hot water and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 2,3,5 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90～100 ℃ of temperature again and is incubated 16 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 222 and reference examples thereof

[embodiment 222-1 method for making] got component 3 and is dissolved in appropriate ethanol, with gained liquid to be suspended in fluid bed be micronized to mean diameter approximately component 4 spray dryinges of 25～100 μ m obtain solid coating powder; Above-mentioned powder mixes with component 1,2, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 222-2 method for making] got component 3 and is dissolved in appropriate ethanol, adds component 1, makes it to be micronized to approximately 0.5～1 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder; Above-mentioned powder mixes with component 2,4, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3,4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, and after mixing, (other) are standby with legal system by embodiment.

Embodiment 223 and reference examples thereof

[method for making] got component 4 and is dissolved in appropriate ethanol, with gained liquid to be suspended in fluid bed be micronized to mean diameter approximately component 5 spray dryinges of 5～25 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 1～3,6～8 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～8, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 224 and reference examples thereof

[embodiment 224-1 method for making] got component 3,4 and is dissolved in suitable quantity of water obtaining solution, this solution spray dry solid coating or dispersion (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder; Above-mentioned powder mixes with the component 1～2 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 1.8t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 224-2 method for making] got component 3 and is dissolved in appropriate ethanol obtaining solution, with this liquid to be suspended in fluid bed be micronized to mean diameter approximately component 1 spray drying of 40～100 μ m obtain solid coating powder; Above-mentioned powder mixes with the component 2,4 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 1.8t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 225 and reference examples thereof

[embodiment 225-1 method for making] got component 4,5 and is dissolved in or is scattered in appropriate hot water, and gained solution or dispersion liquid spray drying obtain solid coating (dispersate or be wrapped by the thing mean diameter be not more than 100nm) powder; Above-mentioned powder mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90～100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 225-2 method for making] got component 1,4 and is dissolved in or is scattered in right amount in (acetic acid or hcl acidifying) water, and gained solution or dispersion liquid spray drying obtain solid coating (dispersate or be wrapped by the thing mean diameter be not more than 100nm) powder; Above-mentioned powder mixes with the component 2～3,5 of crossing 100 mesh sieves (levigate in case of necessity), after mixing with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90～100 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 226 and reference examples thereof

[method for making] component 3～4 is dissolved in altogether in suitable or the amount of being scattered in ethanol and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder; Above-mentioned powder mixes with the component 1,2,5,6 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 70～90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 227 and reference examples thereof

[method for making] component 3～4 is dissolved in altogether fitting or being scattered in calorimetric water and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 10nm) powder 1; Get component 1,2,5～7 and mix, cross 100 mesh sieves (levigate in case of necessity), add above-mentioned powder 1, mix afterwards with the about 0.2t/ pestle of tabletting pressure tabletting (sheet hardness 1.5kp, n=5), sheet is heated to 95 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～7 mixing, crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 228 and reference examples thereof

[embodiment 228-1 method for making] got the appropriate hot ethanol of component 4 use and dissolved, and adds the component 1 with appropriate ether dissolution, mixes the dry solid dispersion (/ body) powder 1 that obtains of solution spray; Above-mentioned powder 1 mixes with the component 2,3 of crossing 100 mesh sieves (levigate in case of necessity), mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90～110 ℃ of temperature again and is incubated 6 minutes, is cooled to room temperature and gets final product.

[embodiment 228-2 method for making] got the appropriate hot ethanol of component 4 use and dissolved, and adds the component 2 of half amount, makes it to be micronized to approximately 5 μ m of mean diameter, and the dispersion liquid spray drying obtains solid coating powder 1; Above-mentioned powder 1 is with the component 1,3 of 100 mesh sieves (levigate in case of necessity) and the component 2 of surplus are mixed excessively, mix, with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 80 ℃ of temperature again and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets the component 1～4 of crossing 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Embodiment 229 and reference examples thereof

The material of the common drying that Advantose FS95Fructose(is 95% fructose and 5% starch)

[method for making] gets component 3, adds the aqueous dispersion (mean diameter is 0.5～5 μ m approximately) of component 4, mixes, and above-mentioned dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 reaches with component 2 component 1,5 of crossing 100 mesh sieves (levigate in case of necessity) to be mixed, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to 90 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～5, crosses 100 mesh sieves (levigate in case of necessity), adds component 2, mixes, standby with legal system by embodiment after mixing.

Embodiment 230 and reference examples thereof

[method for making] component 1,3 is dissolved in altogether appropriate ethanol and obtains solution, in fluid bed, with above-mentioned solution, component 2 spray dryinges of mistake 100 mesh sieves (levigate in case of necessity) of 60% amount that suspends is obtained to solid dispersion (/ body) powder; Above-mentioned powder mixes with component 2 and the component 4 of the surplus of crossing 100 mesh sieves (levigate in case of necessity), mix afterwards with the about 0.17t/ pestle of tabletting pressure tabletting (sheet hardness 1.3kp, n=5), sheet is heated to temperature 70 C again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 231 and reference examples thereof

[embodiment 231-1 method for making] component 3～4 is dissolved in altogether fitting or being scattered in calorimetric ethanol and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; Above-mentioned powder mixes with the component 1,2,5 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[embodiment 231-2 method for making] component 1,4 is dissolved in altogether fitting or being scattered in calorimetric ethanol and obtains solution or dispersion liquid, and above-mentioned solution or dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) (the dispersate mean diameter is not more than 100nm) powder 1; Above-mentioned powder mixes with the component 2,3,5 of crossing 100 mesh sieves, mixes, and with the about 1.5t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 10 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, crosses 100 mesh sieves (levigate in case of necessity), mixes, standby with legal system by embodiment after mixing.

Embodiment 232 and reference examples thereof

[method for making] component 1,3 is dissolved in appropriate hot ethanol, adds component 4, makes it to be micronized to approximately 1～5 μ m of mean diameter, and gained dispersion liquid spray drying obtains solid coating powder 1; Above-mentioned powder 1 with and component 2,5 mix, mix, with the about 2.5t/ pestle of tabletting pressure tabletting (sheet hardness 2kp, n=5), sheet is heated to 90 ℃ of temperature again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and mixes, standby with legal system by embodiment afterwards.

Embodiment 233 and reference examples thereof

[method for making] component 1,3 is dissolved in appropriate hot ethanol, and gained dispersion liquid spray drying obtains that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder 1; Above-mentioned powder 1 mixes with component 2,4,5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 65 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2, standby with legal system by embodiment after mixing.

Embodiment 234 and reference examples thereof

[method for making] component 3 is dissolved in appropriate hot ethanol, adds component 1, makes it to be micronized to approximately 0.5～5 μ m of mean diameter, and gained dispersion liquid spray drying obtains solid coating powder 1; Above-mentioned powder 1 mixes with component 2,4,5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), standby with legal system by embodiment after mixing.

Embodiment 235 and reference examples thereof

[method for making] gets component 3, adds the aqueous dispersion (mean diameter is 0.1～1 μ m approximately) of component 4, mixes, and above-mentioned dispersion liquid spraying or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with component 1,2, adds component 5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 80 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1,3～4, mixes, and crosses 100 mesh sieves (levigate in case of necessity), adds component 2,5, standby with legal system by embodiment after mixing.

Embodiment 236 and reference examples thereof

[method for making] component 4,5 is dissolved in suitable quantity of water, and the gained solution spray is dry that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder 1; Above-mentioned powder 1 mixes with component 1,2,3,6, in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85～95 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6 mixing, crosses 100 mesh sieves (levigate in case of necessity), mixes, and (other) are standby with legal system by embodiment afterwards.

Embodiment 237 and reference examples thereof

[method for making] component 3,4,5 is dissolved in or is scattered in appropriate hot water, and gained solution or dispersion liquid spray drying obtain that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 100nm) powder 1; Above-mentioned powder mixes with the component 1～2,6 of crossing 100 mesh sieves (levigate in case of necessity), and with the about 0.28t/ pestle of tabletting pressure tabletting (sheet hardness 2.4kp, n=5), sheet is heated to 80～90 ℃ of temperature and is incubated 8 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～6, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 238 and reference examples thereof

[method for making] component 1～3 is dissolved in altogether or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Component 4,5 is dissolved in appropriate hot water, and the gained solution spray is dry that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder 2; Above-mentioned powder 1,2 mixes with the component 6～7 of crossing 100 mesh sieves (levigate in case of necessity), in pack into after mixing suitable bubble eye or tablet mould, then is heated to 85 ℃ of temperature and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] component 1～3 is total to molten or is scattered in suitable quantity of water, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 4～7 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Embodiment 239 and reference examples thereof

[embodiment 239-1,2 method for makings] component 4,5 is dissolved in appropriate hot water, and the gained solution spray is dry that solid disperses or coating (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder 1; Above-mentioned powder 1 mixes with the component 1～3 of crossing 100 mesh sieves (levigate in case of necessity), mix, with the about 0.15t/ pestle of tabletting pressure tabletting (sheet hardness 1.2kp, n=5), sheet is heated to 90～100 ℃ of temperature (embodiment 239-1) or 130～160 ℃ (embodiment 239-2) again and is incubated 5 minutes, is cooled to room temperature and gets final product.

[reference examples method for making] gets component 1～5, mixes, and crosses 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

The # explanation: in embodiment 239-1, component 4 is PEG10000, and in embodiment 239-2, component 5 is glucose, and other are identical.

Embodiment 240 and reference examples thereof

[embodiment 240-1 method for making] component 1,2,3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder 1; Component 4 heat fused, add and be micronized to the approximately component 5 of 1 μ m of mean diameter, mixes, cooling, is crushed to 100～120 orders, obtains solid dispersion powder 2; Above-mentioned powder 1,2 mixes, and in pack into after mixing suitable bubble eye or tablet mould, then is heated to temperature 70 C and is incubated 15 minutes, is cooled to room temperature and gets final product.

[embodiment 240-2 method for making] component 2,3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (dispersate or be wrapped by the thing mean diameter be not more than 10nm) powder 1; Component 1,4 is dissolved in or is scattered in appropriate hot water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) (dispersate or be wrapped by the thing mean diameter be not more than 100nm) powder 2; Above-mentioned powder 1,2 mixes, and adds component 5, in pack into after mixing suitable bubble eye or tablet mould, then is heated to temperature 70 C and is incubated 15 minutes, is cooled to room temperature and gets final product.

[reference examples 240-1 method for making] component 1,2,3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 4～5 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

[reference examples 240-2 method for making] component 2,3 is dissolved in suitable quantity of water altogether, and solution spray or lyophilization obtain solid dispersion (/ body) powder 1; Above-mentioned powder 1 mixes with the component 1,4～5 of crossing 100 mesh sieves (levigate in case of necessity), and after mixing, (other) are standby with legal system by embodiment.

Test example

Measure embodiment (annotate: embodiment for simplicity in table 2 with case representation) and the broken degree of hardness, Wei, intraoral disintegration time and the drug-eluting amount (speed) of reference substance sample; Embodiment and reference substance sample thereof are slowly heated, observe and count the record tablet and start temperature when softening; Calculate porosity (above all mensuration 9 times, average).

Wherein, the intraoral disintegration time is by following test determination:

Mouthful do not contain in health becomes man's oral cavity in the oral cavity of moisture and make it contain tablet of the present invention, measure tablet only with the complete disintegrate of saliva until the time of dissolving.

Wherein, drug-eluting amount (speed) is by following test determination:

Getting respectively 1, embodiment and reference substance sample thereof inserts and the about 23ml of same amount is housed measures with liquid (dissolution medium, general pH value approximately 7 ± 0.2 double distilled water or the mensuration liquid of national medicine prison department's Open Standard as listed in pharmacopeia of adopting, other need to indicate especially separately or to specify) but cylindrical or other appropriate vessel of accurate quantification, jolt container 1 minute with method, add and measure with liquid to 25.00ml(25 ℃), shake up (above-mentioned whole process needs to complete in 5 minutes) with method, (dissolution fluid filters with suitable microporous filter membrane immediately to get immediately appropriate dissolution fluid after 5 minutes, from being sampled to filtration, should within 30 seconds, complete) do further to measure.The percentage ratio that accounts for labelled amount with the stripping quantity recorded means (above all mensuration 9 times, average).Special instruction, the stripping quantity of measuring the Chinese medicine extract that contains effective (activity) composition only is determined at the stripping quantity that the China national drug standard regulation of pointing out in description will be measured the Chinese medicine extract composition of content (the maximum composition of the bioassay standard regulation the highest content in other words of content (limit) during multicomponent), its labelled amount is the meansigma methods (when the bound regulation is arranged) of bound for the median of the content limit of this ingredient standard regulation, be perhaps the bottom line (while only stipulating bottom line) of the content of this ingredient standard regulation, dissolution be take this labelled amount as benchmark.

Wherein, the porosity of tablet (Porosity) calculates by following calculating formula (I), puts down in writing the meansigma methods of 9.

Calculating formula (I):

$\mathrm{Porosity}=\frac{v-\mathrm{\Σw}/\mathrm{\ρ}}{v}$

In formula, v: the volume w of tablet: the weight of tablet ingredients, ρ: the proportion that forms tablet ingredients.

The results are shown in Table 2, result shows, the embodiment sample has performance preferably: as mechanical performance is further strengthened, and/or there is higher porosity, and/or there is weatherability (higher fusing point) preferably, and/or there is hydrophilic or intraoral disintegration performance preferably, and/or there is preferably in drug-eluting performance etc. one or several performance and be enhanced.

The broken degree of hardness, Wei of table 2 embodiment and its reference substance, intraoral disintegration time, drug-eluting amount, start softening temperature and the measurement result of porosity

The measurement result of the broken degree of hardness, Wei, (in oral cavity) disintegration time, (medicine) stripping quantity, (beginning) softening temperature and the porosity of table 2 real (executing) example and its reference examples sample

Table 2-1

Table 2-2

Table 2-3

Table 2-4

Table 2-5

Table 2-6

Table 2-7

Table 2-8

Table 2-9

Table 2-10

Table 2-11

Table 2-12

Table 2-13

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 73-1	4.9	0.62	35s	-	68℃	36
Its reference examples	2.2	1.27	66s	-	62℃	38
							Example 73-2	5.7	0.47	15s	-	116℃	37
Its reference examples	2.9	1.16	50s	-	92℃	35
							Example 74-1	7.9	0.19	17s	60	55℃	37
Its reference examples	4.8	0.61	45s	34	40℃	35
							Example 74-2	7.7	0.21	11s	72	58℃	36
Its reference examples	4.3	0.69	40s	38	40℃	37
							Example 75-1	5.9	0.43	5s	99	137℃	42
Example 75-2	4.8	0.60	11s	79	103℃	40
							Its reference examples	2.8	1.17	46s	61	95℃	41
Example 75-3	5.5	0.47	17s	73	106℃	40
							Example 75-4	4.3	0.67	28s	67	101℃	39
Its reference examples	2.6	1.19	49s	58	94℃	41
							Example 76-1	4.7	0.56	22s	68	57℃	22
Example 76-2	5.8	0.42	13s	86	63℃	23
							Its reference examples	3.2	0.89	46s	42	41℃	23
Example 77-1	5.2	0.53	18s	-	58℃	22
							Example 77-2	5.8	0.47	12s	-	63℃	20
Its reference examples	3.5	0.82	36s	-	50℃	21
							Example 78-1	5.9	0.31	6s	96	98℃	31
Example 78-2	5.2	0.43	11s	81	76℃	32
							Example 78-3	4.3	0.61	15s	70	67℃	34
Example 78-4	4.0	0.65	24s	69	66℃	35
							Its reference examples	2.6	1.12	48s	58	59℃	33
Example 78-5	5.5	0.38	5s	78	83℃	34
							Its reference examples	2.9	1.03	28s	60	60℃	36
Example 78-6	5.3	0.40	8s	75	88℃	35
							Its reference examples	2.8	1.07	32s	61	62℃	34

Table 2-14

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 79-1	5.7	0.43	11s	76	76℃	36
Example 79-2	4.8	0.52	18s	68	62℃	37
							Its reference examples	2.8	1.16	36s	55	52℃	38
Example 80-1	6.8	0.32	23s	78	53℃	63

Example 80-2	7.8	0.19	17s	89	57℃	65
							Its reference examples	5.7	0.51	48s	57	46℃	64
Example 81-1	6.3	0.34	7s	95	106℃	40
							Example 81-2	3.7	0.67	22s	60	49℃	41
Example 81-3	5.0	0.52	15s	79	57℃	40
							Its reference examples	2.3	1.22	32s	47	46℃	39
Example 81-4	5.3	0.47	12s	67	59℃	43
							Its reference examples	2.5	1.18	37s	53	47℃	41
Example 81-5	5.6	0.45	16s	64	60℃	41
							Its reference examples	2.7	1.13	38s	50	48℃	40
Example 82-1	4.4	0.63	36s	58	67℃	32
							Its reference examples	2.4	1.09	67s	34	56℃	31
Example 82-2	4.2	0.66	30s	53	69℃	32
							Example 82-3	5.3	0.48	20s	68	73℃	34
Its reference examples	2.8	1.04	49s	38	58℃	33
							Example 83-1	5.5	0.51	5s	101	149℃	46
Example 83-2	4.5	0.67	12s	75	121℃	43
							Example 83-3	3.8	0.81	20s	68	115℃	47
Its reference examples	2.7	1.17	43s	57	106℃	44
							Example 83-4	5.1	0.61	10s	81	128℃	46
Its reference examples	2.4	1.19	40s	60	107℃	45
							Example 84-1	5.8	0.47	11s	100	77℃	43
Example 84-2	4.2	0.68	23s	78	58℃	45
							Its reference examples	2.8	1.15	38s	36	53℃	43

Table 2-15

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 85-1	4.6	0.61	15s	65	69℃	31
Example 85-2	5.5	0.48	11s	76	63℃	30
							Its reference examples	2.6	1.19	32s	53	48℃	29
Example 86	5.8	0.45	18s	87	53℃	33
							Its reference examples	3.2	0.96	47s	42	42℃	34
Example 87-1	4.6	0.63	33s	76	53℃	38
							Example 87-2	5.7	0.47	23s	89	55℃	36
Its reference examples	2.5	1.20	65s	45	40℃	37
							Example 88-1	4.6	0.58	11s	101	43℃	46
Example 88-2	5.0	0.50	22s	78	42℃	43
							Its reference examples	2.3	1.23	56s	56	38℃	41
Example 89-1	5.8	0.46	19s	76	65℃	33
							Example 89-2	4.6	0.58	24s	68	55℃	32
Example 89-3	3.9	0.65	33s	59	51℃	31
							Its reference examples	2.3	1.17	58s	43	47℃	30
Example 90-1	5.9	0.42	16s	-	110℃	33
							Example 90-2	4.4	0.57	27s	-	84℃	32

Its reference examples	2.8	1.05	49s	-	80℃	33
							Example 90-3	4.6	0.53	25s	-	86℃	36
Its reference examples	2.7	1.06	46s	-	81℃	34

Table 2-16

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 91-1	4.4	0.54	15s	67	63℃	31
Example 91-2	5.2	0.46	12s	72	63℃	31
							Its reference examples	2.6	1.12	52s	46	49℃	29
Example 91-3	5.6	0.43	11s	61	67℃	31
							Its reference examples	2.4	1.17	50s	43	50℃	33
Example 92-1	6.4	0.37	17s	-	76℃	34
							Example 92-2	4.5	0.62	35s	-	72℃	32
Its reference examples	2.3	1.20	63s	-	67℃	33
							Example 93-1	5.3	0.44	15s	-	75℃	34
Example 93-2	4.1	0.63	33s	-	65℃	31
							Its reference examples	2.6	1.12	67s	-	38℃	32
Example 94-1	5.6	0.41	14s	-	57℃	37
							Example 94-2	4.1	0.59	27s	-	45℃	35
Its reference examples	2.3	1.12	61s	-	36℃	34
							Example 95-1	4.3	0.62	49s	-	59℃	31
Example 95-2	5.7	0.47	35s	-	50℃	33
							Its reference examples	2.4	1.18	75s	-	35℃	32
Example 96-1	4.4	0.58	20s	-	53℃	87
							Example 96-2	4.9	0.51	13s	-	47℃	56
Its reference examples	2.6	1.13	58s	-	43℃	45

Table 2-17

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 97-1	5.5	0.41	23s	-	73℃	45
Example 97-2	4.9	0.55	15s	-	67℃	46
							Example 97-3	5.1	0.49	6s	-	63℃	47
Its reference examples	2.1	1.23	56s	-	56℃	45
							Example 98-1	6.2	0.33	15s	-	110℃	25
Example 98-2	5.4	0.47	19s	-	117℃	26
							Example 98-3	5.8	0.40	21s	-	120℃	25
Its reference examples	3.2	0.89	50s	-	105℃	24
							Example 98-4	6.0	0.36	19s	-	128℃	25
Its reference examples	2.7	0.97	54s	-	105℃	27
							Example 99-1	6.4	0.33	8s	99	114℃	43
Example 99-2	5.3	0.47	15s	78	102℃	44
							Its reference examples	2.7	1.18	52s	57	94℃	41
Example 99-3	4.8	0.55	26s	75	98℃	45
							Its reference examples	2.4	1.23	57s	53	93℃	42
Example 100-1	4.5	0.65	8s	88	56℃	46

Example 100-2	5.6	0.51	3s	73	52℃	49
							Example 100-3	3.8	0.88	22s	61	44℃	48
Its reference examples	2.2	1.25	40s	52	38℃	47
							Example 101-1	5.9	0.48	13s	73	86℃	44
Example 101-2	4.3	0.67	20s	86	42℃	42
							Its reference examples	2.1	1.28	47s	42	33℃	43
Example 102-1	5.7	0.40	5s	76	65℃	46
							Example 102-2	4.8	0.60	13s	51	58℃	47
Example 102-3	3.8	0.71	23s	42	45℃	47
							Its reference examples	2.6	1.22	40s	33	40℃	48

Table 2-18

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 103-1	5.3	0.51	17s	-	62℃	40
Example 103-2	4.9	0.63	28s	-	54℃	42
							Its reference examples	2.6	1.25	63s	-	43℃	43
Example 104-1	5.8	0.45	15s	78	58℃	27
							Example 104-2	5.2	0.52	25s	65	49℃	26
Example 104-3	4.0	0.63	36s	58	44℃	25
							Its reference examples	2.8	0.99	68s	39	33℃	24
Example 105-1	4.3	0.68	22s	-	41℃	22
							Example 105-2	5.4	0.47	15s	-	47℃	21
Its reference examples	3.1	0.95	47s	-	30℃	21
							Example 106-1	4.5	0.67	25s	-	56℃	34
Example 106-2	5.4	0.50	17s	-	64℃	32
							Its reference examples	2.3	1.21	65s	-	42℃	33
Example 107-1	4.8	0.57	28s	53	63℃	34
							Its reference examples	2.3	1.17	65s	35	46℃	32
Example 107-2	5.2	0.49	10s	92	125℃	45
							Its reference examples	3.0	1.0	40s	55	104℃	46
Example 108-1	6.4	0.36	15s	-	70℃	33
							Example 108-2	4.1	0.68	26s	-	56℃	35
Example 108-3	5.2	0.51	19s	-	61℃	33
							Its reference examples	2.4	1.20	58s	-	51℃	34
Example 109-1	4.1	0.65	4s	-	47℃	76
							Its reference examples	2.4	1.15	10s	-	38℃	78
Example 109-2	5.3	0.50	2s	-	57℃	87
							Its reference examples	3.0	0.90	7s	-	41℃	85

Table 2-19

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 110-1	5.1	0.47	12s	-	54℃	50
Example 110-2	5.7	0.42	8s	-	55℃	49
							Its reference examples	3.6	0.86	36s	-	45℃	51
Example 110-3	6.3	0.36	4s	-	73℃	50

Its reference examples	3.5	0.89	24s	-	46℃	52
							Example 110-4	4.6	0.58	20s	-	57℃	55
Its reference examples	3.3	0.93	35s	-	48℃	53
							Example 111-1	6.2	0.40	15s	-	68℃	23
Example 111-2	4.8	0.54	22s	-	49℃	24
							Its reference examples	3.7	0.81	46s	-	41℃	23
Example 111-3	5.9	0.45	12s	-	52℃	27
							Example 111-4	6.0	0.42	6s	-	75℃	25
Its reference examples	3.5	0.83	35s	-	42℃	26
							Example 111-5	6.6	0.37	8s	-	79℃	24
Its reference examples	3.9	0.76	40s	-	41℃	27
							Example 112-1	4.7	0.56	4s	101	56℃	76
Example 112-2	4.3	0.61	6s	78	51℃	75
							Its reference examples	3.2	0.91	13s	65	37℃	78
Example 113-1	5.0	0.47	23s	-	61℃	29
							Example 113-2	6.7	0.32	12s	-	67℃	28
Its reference examples	3.3	0.81	49s	-	53℃	27
							Example 114-1	4.9	0.52	20s	-	57℃	38
Its reference examples	2.4	1.18	60s	-	32℃	40
							Example 114-2	4.2	0.61	26s	-	61℃	44
Its reference examples	2.6	1.12	65s	-	44℃	42
							Example 114-3	5.6	0.48	12s	-	69℃	41
Its reference examples	2.8	1.02	40s	-	42℃	43
							Example 115-1	6.3	0.35	11s	92	69℃	31
Example 115-2	5.4	0.48	16s	68	66℃	33
							Example 115-3	4.1	0.63	28s	52	60℃	33
Its reference examples	2.8	0.97	57s	38	48℃	32

Table 2-20

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 116-1	4.3	0.62	18s	-	67℃	43
Example 116-2	3.8	0.78	13s	-	53℃	45
							Its reference examples	2.2	1.25	52s	-	45℃	43
Example 116-3	4.8	0.53	5s	-	73℃	45
							Its reference examples	2.4	1.20	34s	-	45℃	47
Example 117-1	5.8	0.42	8s	-	112℃	37
							Example 117-2	4.2	0.65	17s	-	101℃	38
Its reference examples	2.5	1.18	40s	-	96℃	36
							Example 117-3	5.0	0.53	11s	-	106℃	38
Its reference examples	2.3	1.22	45s	-	98℃	37
							Example 117-4	4.8	0.57	13s	-	109℃	36
Its reference examples	2.2	1.24	49s	-	97℃	38
							Example 118-1	4.4	0.65	4s	-	65℃	41
Example 118-2	3.6	0.87	7s	-	43℃	42

Its reference examples	2.1	1.26	23s	-	35℃	43
							Example 118-3	4.8	0.60	2s	-	75℃	44
Its reference examples	2.3	1.20	21s	-	35℃	46
							Example 119-1	5.9	0.41	15s	101	115℃	35
Example 119-2	5.1	0.52	22s	83	112℃	34
							Its reference examples	2.8	1.16	35s	65	100℃	33
Example 119-3	4.8	0.55	12s	80	108℃	34
							Its reference examples	2.5	1.19	33s	63	101℃	35
Example 120-1	5.9	0.48	8s	-	78℃	46
							Example 120-2	4.7	0.59	15s	-	60℃	47
Its reference examples	2.4	1.18	28s	-	54℃	45
							Example 121-1	5.9	0.40	4s	101	136℃	44
Example 121-2	5.1	0.52	10s	82	125℃	42
							Its reference examples	2.6	1.15	37s	70	113℃	43
Example 121-3	4.8	0.55	15s	93	137℃	45
							Its reference examples	2.3	1.19	39s	68	115℃	44
Example 121-4	5.7	0.45	7s	101	143℃	44
							Its reference examples	2.8	1.10	33s	72	114℃	42
Example 122-1	5.8	0.42	11s	92	93℃	43
							Example 122-2	5.3	0.50	18s	68	81℃	43
Its reference examples	2.7	1.13	43s	53	55℃	41
							Example 122-3	4.2	0.61	27s	76	60℃	42
Its reference examples	2.4	1.13	45s	55	56℃	43
							Example 123-1	5.5	0.51	15s	98	65℃	39
Example 123-2	4.9	0.58	13s	85	61℃	39
							Its reference examples	3.0	0.89	31s	68	57℃	40
Example 123-3	6.6	0.32	7s	86	73℃	43
							Its reference examples	3.2	0.85	30s	69	57℃	41
Example 124-1	5.8	0.38	9s	92	77℃	36
							Example 124-2	4.6	0.61	15s	76	71℃	38
Its reference examples	2.1	1.25	40s	62	42℃	37
							Example 124-3	4.9	0.57	16s	74	74℃	38
Its reference examples	2.3	1.21	43s	60	41℃	36
							Example 125-1	6.4	0.34	6s	101	76℃	45
Example 125-2	5.5	0.52	12s	99	72℃	45
							Example 125-3	5.3	0.54	13s	87	70℃	45
Its reference examples	2.0	1.26	37s	76	54℃	47
							Example 125-4	4.8	0.60	12s	86	74℃	44
Its reference examples	1.8	1.30	34s	75	53℃	46

Table 2-21

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 126-1	5.7	0.47	7s	95	85℃	40
Example 126-2	4.9	0.61	12s	79	76℃	42

Its reference examples	2.4	1.20	37s	55	52℃	41
							Example 126-3	4.9	0.61	12s	75	76℃	42
Its reference examples	2.2	1.23	38s	56	51℃	43
							Example 126-4	3.8	0.81	17s	68	55℃	42
Its reference examples	2.0	1.27	48s	53	50℃	44
							Example 127-1	5.0	0.54	7s	93	76℃	46
Its reference examples	2.5	1.12	35s	47	51℃	43
							Example 127-2	5.8	0.43	9s	87	72℃	44
Its reference examples	3.3	0.97	40s	47	50℃	46
							Example 128-1	4.3	0.63	7s	78	48℃	59
Its reference examples	2.4	1.18	18s	58	36℃	57
							Example 128-2	4.8	0.57	3s	92	63℃	58
Its reference examples	2.2	1.23	13s	75	36℃	56
							Example 129	5.0	0.52	12s	102	48℃	31
Its reference examples	2.6	1.11	31s	67	32℃	30
							Example 130-1	5.8	0.43	10s	90	117℃	28
Its reference examples	2.9	1.06	27s	69	95℃	26
							Example 130-2	5.2	0.48	14s	83	121℃	27
Its reference examples	2.7	1.12	32s	65	97℃	29
							Example 131-1	5.8	0.42	14s	87	68℃	45
Example 131-2	4.5	0.58	24s	67	56℃	43
							Its reference examples	3.0	0.90	48s	45	48℃	44
Example 131-3	4.6	0.60	9s	101	56℃	45
							Its reference examples	2.8	0.92	40s	53	46℃	46
Example 132-1	5.6	0.43	17s	85	58℃	26
							Its reference examples	3.5	0.81	62s	52	40℃	28
Example 132-2	4.8	0.57	8s	97	51℃	27
							Its reference examples	3.1	0.89	47s	58	37℃	29
Example 133-1	5.9	0.43	15s	84	76℃	34
							Example 133-2	4.3	0.65	25s	63	69℃	34
Its reference examples	2.8	1.13	61s	52	56℃	35
							Example 134-1	5.9	0.37	14s	106	51℃	38
Example 134-2	5.4	0.46	18s	89	48℃	39
							Its reference examples	4.3	0.67	33s	60	44℃	38

Table 2-22

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 135	4.9	0.65	36s	-	47℃	18
Its reference examples	3.7	0.81	53s	-	38℃	17
							Example 136	4.7	0.61	5s	-	58℃	91
Its reference examples	2.8	0.92	35s	-	45℃	90
							Example 137-1	5.2	0.48	9s	150	58℃	38
Example 137-2	4.7	0.57	19s	89	56℃	38

Its reference examples	2.6	1.12	57s	73	47℃	37
							Example 138-1	5.7	0.43	15s	91	73℃	37
Example 138-2	4.5	0.55	21s	76	61℃	34
							Its reference examples	2.3	1.18	48s	47	37℃	36
Example 138-3	4.4	0.65	12s	118	45℃	35
							Its reference examples	2.1	1.23	40s	56	34℃	37
Example 139-1	5.6	0.47	8s	-	92℃	31
							Example 139-2	4.3	0.61	17s	-	67℃	31
Its reference examples	2.4	1.23	35s	-	56℃	28
							Example 139-3	4.4	0.67	18s	-	81℃	29
Its reference examples	2.0	1.29	41s	-	53℃	30
							Example 139-4	6.8	0.32	9s	-	96℃	32
Its reference examples	3.6	0.85	37s	-	80℃	30
							Example 140-1	5.9	0.37	6s	112	87℃	53
Example 140-2	4.3	0.65	16s	79	75℃	53
							Its reference examples	2.4	1.19	32s	68	56℃	55
Example 140-3	4.5	0.63	9s	101	79℃	52
							Its reference examples	2.1	1.22	39s	52	53℃	53
Example 140-4	6.7	0.35	4s	125	98℃	51
							Its reference examples	3.3	0.98	25s	78	82℃	53
Example 141-1	5.6	0.41	6s	157	79℃	37
							Example 141-2	4.2	0.57	16s	89	62℃	37
Its reference examples	2.7	1.18	36s	72	38℃	39
							Example 141-3	3.8	0.80	10s	135	69℃	36
Its reference examples	1.9	1.32	43s	65	35℃	38
							Example 141-4	6.5	0.35	4s	116	159℃	35
Its reference examples	3.3	0.87	28s	53	150℃	37
							Example 142-1	5.9	0.30	7s	118	97℃	31
Example 142-2	4.5	0.52	16s	81	84℃	28
							Its reference examples	2.9	1.07	36s	62	81℃	30

Table 2-23

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 143-1	5.6	0.40	9s	89	79℃	45
Example 143-2	4.2	0.58	17s	61	57℃	45
							Its reference examples	2.7	1.15	46s	45	41℃	47
Example 144	5.8	0.46	23s	-	76℃	33
							Its reference examples	2.9	1.03	64s	-	52℃	34
Example 145-1	6.5	0.38	9s	-	89℃	29
							Example 145-2	4.8	0.52	17s	-	76℃	26
Its reference examples	3.0	0.93	42s	-	55℃	28
							Example 146	6.5	0.37	20s	-	73℃	30
Its reference examples	3.2	0.89	42s	-	37℃	32
							Example 147-1	5.4	0.57	14s	98	89℃	38

Its reference examples	2.5	1.12	57s	52	56℃	39
							Example 147-2	4.2	0.68	9s	102	77℃	36
Its reference examples	2.0	1.24	40s	63	44℃	37
							Example 148-1	6.0	0.38	15s	92	67℃	34
Its reference examples	2.8	1.08	54s	46	52℃	36
							Example 148-2	5.7	0.43	4s	87	121℃	41
Its reference examples	3.1	0.93	37s	56	88℃	40
							Example 148-3	4.5	0.62	12s	78	112℃	34
Its reference examples	2.6	1.12	40s	51	104℃	35
							Example 149-1	4.8	0.59	32s	76	65℃	40
Its reference examples	2.6	1.12	61s	32	36℃	42
							Example 149-2	5.3	0.51	3s	93	123℃	66
Its reference examples	2.8	1.06	18s	47	86℃	65
							Example 149-3	5.7	0.45	11s	85	117℃	44
Its reference examples	3.0	0.98	29s	42	108℃	45
							Example 150-1	5.1	0.55	5s	-	82℃	47
Its reference examples	2.8	1.08	26s	-	53℃	45
							Example 150-2	4.5	0.63	3s	-	132℃	63
Its reference examples	2.3	1.19	16s	-	89℃	65
							Example 150-3	5.5	0.47	14s	-	124℃	41
Its reference examples	3.1	0.94	39s	-	113℃	40
							Example 151-1	5.9	0.39	13s	92	85℃	31
Example 151-2	4.3	0.57	19s	62	68℃	31
							Its reference examples	2.4	1.12	58s	42	52℃	33
Example 151-3	4.0	0.65	12s	99	78℃	34
							Its reference examples	2.1	1.22	50s	48	56℃	32

(illustrate: the stripping quantity of measuring tanshinone IIA in embodiment 143 and reference examples thereof; Measure the stripping quantity of oleanolic acid in embodiment 148 and reference examples thereof; Using the total amount of mentioned component in the sheet recorded as the basis of reference of its stripping quantity)

Table 2-24

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 152-1	4.9	0.67	4s	101	82℃	42
Example 152-2	3.3	0.89	13s	92	46℃	44
							Example 152-3	4.0	0.78	6s	82	48℃	45
Its reference examples	2.2	1.26	28s	65	42℃	43
							Example 153-1	5.8	0.52	9s	100	98℃	32
Example 153-2	4.9	0.69	18s	88	92℃	31
							Example 153-3	3.6	0.83	26s	73	90℃	32
Its reference examples	2.7	1.14	46s	56	87℃	33
							Example 154-1	4.8	0.64	7s	100	102℃	30
Example 154-2	4.6	0.68	9s	95	98℃	33
							Example 154-3	5.3	0.57	13s	90	99℃	32
Its reference examples	3.1	0.99	49s	60	95℃	31
							Example 155-1	5.3	0.55	15s	90	101℃	36

Example 155-2	4.8	0.61	16s	93	99℃	37
							Its reference examples	3.2	0.94	52s	57	96℃	38
Example 156-1	4.5	0.73	18s	92	78℃	42
							Example 156-2	3.6	0.88	20s	85	61℃	44
Its reference examples	2.1	1.26	46s	42	57℃	43
							Example 157-1	4.8	0.61	8s	99	65℃	31
Example 157-2	4.2	0.69	10s	92	59℃	34
							Example 157-3	5.8	0.52	7s	80	57℃	33
Its reference examples	2.7	1.18	43s	47	53℃	32
							Example 158	4.9	0.64	20s	99	62℃	31
Its reference examples	3.2	0.95	26s	53	57℃	33
							Example 159-1	5.4	0.55	15s	88	88℃	23
Example 159-2	4.3	0.67	19s	71	62℃	25
							Example 159-3	6.4	0.43	11s	60	67℃	24
Its reference examples	3.2	0.97	56s	37	57℃	26

Table 2-25

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 160-1	4.9	0.60	21s	82	62℃	32
Example 160-2	4.4	0.68	26s	76	60℃	34
							Its reference examples	2.8	1.08	68s	38	57℃	33
Example 161	4.7	0.66	13s	91	72℃	33
							Its reference examples	2.1	1.21	45s	38	36℃	35
Example 162-1	5.3	0.60	23s	76	65℃	32
							Example 162-2	4.2	0.72	29s	52	61℃	35
Example 162-3	5.8	0.52	17s	44	63℃	33
							Its reference examples	2.8	1.12	62s	33	58℃	34
Example 163-1	5.3	0.55	9s	69	89℃	62
							Example 163-2	4.8	0.61	6s	55	64℃	58
Example 163-3	5.9	0.50	4s	49	66℃	60
							Its reference examples	3.8	0.86	28s	38	56℃	61
Example 164-1	4.6	0.63	16s	88	-	57
							Example 164-2	4.0	0.72	20s	76	-	55
Example 164-3	4.8	0.60	22s	51	-	56
							Its reference examples	2.4	1.16	41s	38	-	57
Example 165-1	3.9	0.78	19s	99	67℃	32
							Example 165-2	5.3	0.58	11s	78	65℃	33
Its reference examples	3.1	0.89	24s	56	58℃	34
							Example 166-1	4.0	0.72	12s	93	83℃	50
Example 166-2	4.4	0.68	8s	91	75℃	51
							Example 166-3	5.2	0.57	4s	58	72℃	52
Its reference examples	2.7	1.11	26s	41	40℃	53
							Example 167-1	3.0	0.98	22s	101	45℃	46
Example 167-2	5.8	0.51	11s	86	51℃	47

Its reference examples

2.2

1.18

24s

70

43℃

48

Table 2-26

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 168	3.3	0.78	6s	98	58℃	76
Its reference examples	2.6	1.09	8s	56	53℃	73
							Example 169	5.2	0.53	12s	99	40℃	41
Its reference examples	2.5	1.12	43s	32	35℃	38
							Example 170-1	4.0	0.65	27s	43	61℃	41
Example 170-2	4.9	0.58	18s	67	97℃	45
							Its reference examples	2.3	1.18	67s	21	55℃	43
Example 171	4.8	0.60	32s	79	47℃	36
							Its reference examples	2.6	1.18	56s	41	33℃	38
Example 172-1	3.8	0.82	8s	67	55℃	52
							Example 172-2	4.6	0.68	4s	89	62℃	57
Its reference examples	2.0	1.23	20s	34	48℃	54
							Example 173-1	4.2	0.72	10s	92	59℃	30
Example 173-2	4.8	0.68	7s	101	62℃	32
							Example 173-3	6.8	0.39	6s	75	56℃	29
Its reference examples	3.2	0.91	40s	47	53℃	31
							Example 174-1	3.6	0.88	19s	101	45℃	36
Example 174-2	4.8	0.71	12s	83	44℃	34
							Its reference examples	2.1	1.22	52s	56	40℃	37
Example 175	4.5	0.63	15s	52	85℃	65
							Its reference examples	2.6	1.21	39s	24	36℃	68

Table 2-27

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 176-1	4.4	0.69	6s	91	57℃	53
Example 176-2	5.2	0.53	4s	102	61℃	51
							Its reference examples	2.6	1.16	26s	57	51℃	56
Example 177	6.8	0.35	8s	101	62℃	23
							Its reference examples	2.7	1.18	67s	68	53℃	25
Example 178-1	4.5	0.64	6s	75	107℃	33
							Example 178-2	5.3	0.55	4s	89	108℃	31
Example 178-3	6.3	0.41	9s	58	109℃	33
							Its reference examples	3.2	0.89	43s	37	105℃	35
Example 179-1	5.7	0.45	10s	101	85℃	32
							Example 179-2	5.1	0.52	18s	88	83℃	33
Example 179-3	6.8	0.34	8s	81	86℃	31
							Its reference examples	3.3	0.86	37s	62	81℃	35
Example 180-1	5.3	0.52	14s	95	48℃	28
							Example 180-2	4.8	0.63	18s	57	45℃	30
Its reference examples	3.0	0.89	65s	29	44℃	31
							Example 181-1	4.9	0.61	11s	93	108℃	32

Example 181-2	5.6	0.52	8s	78	109℃	33
							Its reference examples	3.3	0.89	37s	51	104℃	35
Example 182-1	5.2	0.54	3s	102	127℃	83
							Example 182-2	4.5	0.68	8s	83	92℃	85
Its reference examples	2.6	1.07	26s	65	86℃	88

Table 2-28

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 183-1	4.7	0.65	18s	91	68℃	50
Example 183-2	4.9	0.61	15s	83	49℃	49
							Example 183-3	5.6	0.53	12s	57	51℃	47
Its reference examples	2.4	1.12	47s	43	43℃	52
							Example 184-1	5.0	0.57	9s	96	86℃	29
Example 184-2	4.2	0.71	12s	83	38℃	31
							Example 184-3	4.8	0.63	6s	71	41℃	30
Its reference examples	2.3	1.16	43s	38	33℃	33
							Example 185-1	6.7	0.39	11s	91	89℃	33
Example 185-2	4.5	0.65	15s	76	42℃	31
							Example 185-3	5.8	0.47	6s	63	64℃	32
Its reference examples	2.6	1.08	42s	35	37℃	30
							Example 186-1	6.8	0.35	9s	102	81℃	26
Example 186-2	5.2	0.48	16s	88	59℃	28
							Example 186-3	5.9	0.42	12s	80	61℃	27
Its reference examples	3.3	0.86	47s	68	53℃	30
							Example 187-1	6.3	0.39	6s	102	-	51
Example 187-2	5.5	0.48	12s	89	-	54
							Its reference examples	3.2	0.87	33s	68	-	56
Example 188	4.8	0.56	2s	101	-	80
							Its reference examples	2.6	1.12	38s	70	-	83
Example 189-1	6.3	0.41	4s	101	89℃	35
							Example 189-2	5.0	0.56	8s	87	39℃	37
Example 189-3	5.4	0.50	13s	75	41℃	36
							Its reference examples	3.6	0.85	32s	63	35℃	38
Example 190-1	5.5	0.54	5s	99	88℃	55
							Example 190-2	5.3	0.50	8s	73	53℃	56
Its reference examples	3.4	0.89	31s	46	48℃	58

Table 2-29

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 191-1	5.8	0.48	12s	101	-	32
Example 191-2	6.0	0.43	15s	86	-	33
							Its reference examples	3.0	0.91	38s	48	-	36
Example 192-1	4.3	0.64	9s	87	56℃	27
							Example 192-2	5.4	0.51	6s	50	57℃	25
Its reference examples	3.2	0.92	42s	38	52℃	28

Example 193-1	4.2	0.65	11s	78	65℃	43
							Example 193-2	4.8	0.58	8s	86	66℃	42
Example 193-3	5.5	0.49	5s	60	70℃	41
							Its reference examples	2.8	1.06	27s	38	62℃	45
Example 194-1	3.7	0.85	11s	97	126℃	46
							Example 194-2	6.4	0.41	7s	76	131℃	43
Its reference examples	3.3	0.93	23s	58	123℃	47
							Example 195-1	4.2	0.67	17s	101	42℃	32
Example 195-2	5.8	0.47	9s	87	44℃	31
							Its reference examples	3.1	0.92	40s	68	39℃	33
Example 196-1	5.2	0.50	20s	99	55℃	29
							Example 196-2	6.9	0.38	15s	78	60℃	28
Its reference examples	3.3	0.88	45s	52	47℃	31
							Example 197-1	5.3	9.53	18s	92	52℃	28
Example 197-2	6.6	0.41	13s	72	60℃	27
							Its reference examples	3.0	0.92	41s	50	48℃	30
Example 198-1	4.9	0.60	9s	85	66℃	29
							Example 198-2	5.6	0.51	8s	96	73℃	28
Example 198-3	6.5	0.42	6s	72	97℃	27
							Its reference examples	3.0	0.93	43s	51	58℃	31

Table 2-30

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 199-1	4.9	0.54	2s	101	87℃	87
Example 199-2	4.3	0.62	7s	80	72℃	86
							Its reference examples	2.6	1.19	20s	68	39℃	84
Example 200-1	6.1	0.41	14s	99	88℃	26
							Example 200-2	5.8	0.46	17s	93	78℃	25
Example 200-3	5.2	0.53	23s	73	65℃	27
							Its reference examples	3.3	0.93	52s	58	57℃	28
Example 201-1	4.8	0.61	7s	94	103℃	55
							Example 201-2	4.5	0.67	9s	88	71℃	54
Example 201-3	5.3	0.51	5s	67	62℃	53
							Its reference examples	2.4	1.16	27s	56	57℃	57
Example 202-1	5.5	0.53	26s	86	94℃	26
							Example 202-2	6.2	0.40	17s	65	68℃	28
Its reference examples	3.3	0.95	68s	42	65℃	29
							Example 203-1	4.8	0.63	7s	102	83℃	51
Example 203-2	4.2	0.71	9s	88	51℃	53
							Example 203-3	5.6	0.52	5s	78	61℃	50
Its reference examples	2.4	1.17	27s	66	47℃	55
							Example 204-1	4.8	0.62	12s	94	59℃	28
Example 204-2	5.9	0.48	6s	102	82℃	27
							Example 204-3	5.1	0.56	8s	85	64℃	29

Its reference examples	2.9	1.04	49s	74	55℃	31
							Example 205-1	4.0	0.67	8s	92	51℃	31
Example 205-2	5.8	0.48	17s	73	46℃	29
							Its reference examples	2.2	1.21	62s	61	41℃	33

Table 2-31

	Hardness (kg)	The broken degree of Wei (%)	Disintegration time	Stripping quantity (%)	Softening temperature	Porosity (%)
							Example 206-1	4.6	0.62	23s	85	60℃	28
Example 206-2	5.1	0.54	15s	62	62℃	26
							Its reference examples	2.8	1.03	68s	47	57℃	30
Example 207-1	4.5	0.64	9s	91	108℃	52
							Example 207-2	6.1	0.45	6s	65	107℃	51
Its reference examples	2.7	1.06	25s	48	104℃	53
							Example 208-1	5.9	0.48	9s	78	93℃	38
Example 208-2	4.3	0.67	11s	43	76℃	36
							Its reference examples	1.8	1.32	37s	29	53℃	37
Example 208-3	3.3	0.89	25s	36	70℃	38
							Its reference examples	1.9	1.30	48s	27	65℃	36
Example 209-1	5.3	0.53	6s	85	87℃	51
							Example 209-2	4.9	0.61	9s	63	67℃	52
Its reference examples	2.3	1.18	38s	41	58℃	55
							Example 210	4.3	0.63	3s	-	52℃	63
Its reference examples	2.9	0.96	11s	-	39℃	67
							Example 211-1	5.0	0.43	15s	-	55℃	34
Its reference examples	2.8	0.92	32s	-	47℃	36
							Example 211-2	5.6	0.37	11s	-	53℃	35
Example 211-3	5.4	0.39	9s	-	58℃	38
							Its reference examples	3.2	0.86	24s	-	45℃	37
Example 212	5.1	0.45	10s	-	55℃	36
							Its reference examples	3.0	0.88	31s	-	33℃	34
Example 213-1	5.5	0.40	23s	92	55℃	23
							Example 213-2	4.8	0.58	45s	59	47℃	25
Its reference examples	3.0	0.90	56s	47	42℃	23
							Example 214-1	5.0	0.49	19s	82	69℃	32
Example 214-2	5.4	0.40	15s	95	62℃	31
							Its reference examples	2.9	1.05	43s	69	56℃	33

Table 2-32

Table 2-33

Table 2-34

Table 2-35

Attached: list of references

1, Xu Cuiyun, nanosecond science and technology research application present situation and trend analysis both at home and abroad, Chinese powder technology, 2002 (8) 3:32-36.

2, Zhang Lide, the progress of nano materials research and the countermeasure of China, scientific and technological Leader, 2000,10:33-34.

3, Bai Chunli, nanosecond science and technology and development progress thereof, Chinese engineering consulting, 2000,4:38-41

4, Zhang Lide, Mu Jimei work, nano material and nanostructured, Beijing: Science Press, 2001,99-102.

5, Xu Guocai, Zhang Lide work, nano composite material, Beijing: Materials Science and Engineering publishing centre, 2001,101-105.

6, permitted clod of earth and respected etc., the peptizaiton of high molecular surfactant to the oxide ceramics ultramicro powder, Chinese pottery, 1999 (35): 515-518.

7, Wu Renjie, the status and prospectives of metal-base composites, Acta Metallurgica Sinica, 1991,33(1): 78-84.

8, Gui Manchang etc., the preparation of particles reiforced metal-base composition and application, material Leader 1996, (3): 65-71.

9, Hao Yuankai, discontinuous reinforcement light metal composite research status and prospect, material Leader, 1991, (5): 67-71.

10, Huang Zewen, the large-scale production of metal-base composites and commercialization development, material Leader, 1996, (supplementary issue): 18-25.

11、V.K.Lindroos,M.J.Talvitie,Recent Advances in Mental Matrix Composites.J.Mater.Process.Tech.，1995,(53):273-284.

Claims (50)

1. the tablet of a performance improvement, this tablet comprises:

1), at least one active components A 1;

2), at least one pharmaceutically acceptable hydrophilic diluent B 1; And

3), at least one is selected from following fusible adhesion agent C1:

C1-1: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion I of 25 ℃ of temperature, above-mentioned solid dispersion I contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, perhaps

C1-2: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion II of 25 ℃ of temperature, above-mentioned solid dispersion II contain at least one fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the surfactant E2 of above-mentioned medicinal lipid additive D2, perhaps

C1-3: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion III of 25 ℃ of temperature, above-mentioned solid dispersion III contain at least one fusing point (more above-mentioned diluent B 1 low but) hydrophilic surfactant E21 higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, perhaps

C1-4: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion IV of 25 ℃ of temperature, above-mentioned solid dispersion IV contain at least one fusing point (more above-mentioned diluent B 1 low but) hydrophilic surfactant E21 higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, perhaps

C1-5: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid dispersion V of 25 ℃ of temperature, above-mentioned solid dispersion V contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than the hydrophilic medical additive E2 of 25 ℃ of temperature, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, perhaps,

C1-6: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating I of 25 ℃ of temperature, above-mentioned solid coating I comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D1 and by the above-mentioned fusible outer core core 1 that fusing point that thing D1 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned fusible outer cover thing D1 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, above-mentioned core core 1 comprises the medical additive E3 that at least one pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, perhaps,

C1-7: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating II of 25 ℃ of temperature, above-mentioned solid coating II comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D2 and by the above-mentioned fusible outer core core 2 that fusing point that thing D2 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned fusible outer cover thing D2 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, above-mentioned core core 2 comprises the hydrophilic medical additive E4 that at least one pharmaceutically acceptable fusing point is not less than 25 ℃ of temperature, perhaps,

C1-8: the solid dispersion VI of the further combination in any of solid dispersion in above-mentioned fusible adhesion agent C1-1～C1-5, or,

C1-9: the mixture of two or more in above-mentioned fusible adhesion agent C1-1～C1-8;

And above-mentioned diluent B 1 and/or above-mentioned active components A 1 are by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C1;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (I～VI) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (I～II) is not more than 100 μ m;

And/or

This tablet comprises:

1), at least one pharmaceutically acceptable hydrophilic diluent B 2;

2), at least one is selected from following fusible adhesion agent C2:

C2-1: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid dispersion VII of 25 ℃ of temperature, above-mentioned solid dispersion VII contain at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature fusible binding agent D1 and and at least one active components A 2, above-mentioned fusible binding agent D1 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, and/or

C2-2: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid coating III of 25 ℃ of temperature, above-mentioned solid coating III comprise fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature cover thing D3 and by the above-mentioned fusible outer core core 3 that thing D3 coats that covers fusible outward, above-mentioned fusible outer cover thing D3 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, above-mentioned core core 3 comprises at least one active components A 2,

And above-mentioned diluent B 2 is by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C2;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (VII) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (III) is not more than 100 μ m.

2. the tablet of a performance improvement, this tablet comprises:

1), at least one active components A 1;

2), at least one pharmaceutically acceptable hydrophilic diluent B 1; And

3), at least one is selected from following fusible adhesion agent C1:

C1-10: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating IV of 25 ℃ of temperature, above-mentioned solid coating IV comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D4 and by the above-mentioned fusible outer core core 4 that fusing point that thing D4 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned core core 4 comprises the medical additive E3 that at least one fusing point is not less than 25 ℃ of temperature, above-mentionedly fusiblely outer cover thing D4 and comprise at least one following solid dispersion: contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) solid dispersion I that be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, or contain at least one fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion II of the surfactant E2 of above-mentioned medicinal lipid additive D2, or contain at least one fusing point (more above-mentioned diluent B 1 low but) solid dispersion III higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the hydrophilic surfactant E21 of 25 ℃ of temperature, or contain at least one fusing point (more above-mentioned diluent B 1 low but) higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the solid dispersion IV of the hydrophilic surfactant E21 of 25 ℃ of temperature or the solid dispersion VIII of their combination in any, above-mentioned solid dispersion (I～IV, VIII) the dispersed component particle in or dispersate particle or discontinuous phase average particle size are not more than 100 μ m, and/or

C1-11: at least one fusing point (more above-mentioned diluent B 1 low but) be not less than the fusible solid coating V of 25 ℃ of temperature, above-mentioned solid coating V comprise fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature cover thing D5 and by the above-mentioned fusible outer core core 5 that fusing point that thing D5 coats is not less than 25 ℃ of temperature that covers fusible outward, above-mentioned core core 5 comprises the hydrophilic medical additive E4 that at least one fusing point is not less than 25 ℃ of temperature, above-mentioned fusible outer cover thing D5 comprise contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion V of the hydrophilic medical additive E2 of 25 ℃ of temperature, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, dispersed component particle in above-mentioned solid dispersion (V) or dispersate particle or discontinuous phase average particle size are not more than 100 μ m,

And above-mentioned diluent B 1 and/or above-mentioned active components A 1 are by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C1;

And the core core mean diameter be wrapped by above-mentioned solid coating (IV～V) is not more than 100 μ m;

And/or

This tablet comprises:

1), at least one pharmaceutically acceptable hydrophilic diluent B 2;

2), at least one is selected from following fusible adhesion agent C2:

C2-3: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid dispersion IX of 25 ℃ of temperature, above-mentioned solid dispersion IX contain at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature fusible binding agent D2 and and at least one active components A 2, above-mentioned fusible binding agent D2 comprise at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, or at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the surfactant E2 of above-mentioned medicinal lipid additive D2, or at least one fusing point (more above-mentioned diluent B 2 low but) hydrophilic surfactant E21 higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, or at least one fusing point (more above-mentioned diluent B 2 low but) hydrophilic surfactant E21 higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than 25 ℃ of temperature, or at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than hydrophilic medical additive E2 or their combination in any of 25 ℃ of temperature, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or

C2-4: at least one fusing point (more above-mentioned diluent B 2 low but) be not less than the fusible solid coating VI of 25 ℃ of temperature, above-mentioned solid coating VI comprise fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature cover thing D6 and by the above-mentioned fusible outer core core 6 that thing D6 coats that covers fusible outward, above-mentioned core core 6 comprises at least one active components A 2, above-mentionedly fusiblely outer cover thing D6 and comprise at least one following solid dispersion: contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) solid dispersion I that be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point, or contain at least one fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion II of the surfactant E2 of above-mentioned medicinal lipid additive D2, or contain at least one fusing point (more above-mentioned diluent B 2 low but) solid dispersion III higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the hydrophilic surfactant E21 of 25 ℃ of temperature, or contain at least one fusing point (more above-mentioned diluent B 2 low but) solid dispersion IV higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the hydrophilic surfactant E21 of 25 ℃ of temperature, or contain at least one pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3 and at least one pharmaceutically acceptable fusing point be not less than the solid dispersion V of hydrophilic medical additive E2 of 25 ℃ of temperature or the solid dispersion X of their combination in any, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 2 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, above-mentioned solid dispersion (I～V, X) the dispersed component particle in or dispersate particle or discontinuous phase average particle size are not more than 100 μ m,

And above-mentioned diluent B 2 is by the bonding bridging of solidification of molten thing of above-mentioned fusible adhesion agent C2;

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (IX) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (VI) is not more than 100 μ m.

3. according to the tablet of claim 1 or 2, the porosity that it is characterized in that described tablet is 10 to 95%.

4. according to the tablet of claim 1 or 2, it is characterized in that described tablet does not absorb water when taking, in oral cavity basically only with saliva in 1 minute with interior disintegrate/or tablet of dissolving.

5. according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 are selected from the diluent that balance meltage in the water of 25 ℃ of temperature or dispersion amount are not less than 5mg/1ml.

6. according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 be selected from its pore volume divided by the determined porosity of cumulative volume higher than 0.14 or its weight divided by the determined density of cumulative volume lower than diluent O.86.

7. according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 are selected from the particulate matter that contains described diluent and disintegrating agent and/or can not form the sweller of strong gel.

8. according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 are selected from hydrophilic following medicinal diluent: saccharide diluent, pharmaceutically acceptable cyclodextrin diluent, salt diluent, aminoacid, edible peptide and their mixture.

9. according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 are selected from hydrophilic following medicinal diluent: triose, tetrose, pentose, hexose, heptose, disaccharidase, trisaccharide, tetrose, pentasaccharides, six to nine sugar, the oligosaccharide that the degree of polymerization is 10～100, the sugar alcohol of above-mentioned sugar, the derivant that methylates of above-mentioned sugar and sugar alcohol thereof, the methylolation derivant, the hydroxyethylation derivant, the hydroxypropylation derivant, hydroxyl butylation derivant or above-mentioned moiety combinations derivant, cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, derivant methylates, the modularization derivant of sulfobutyl ether derivant or above-mentioned group, tasteless or be the aminoacid of sweet or delicate flavour, tasteless or be the acidity of sweet or delicate flavour or the pharmaceutical salts of basic amino acid, edible 2～100 peptides, the pharmaceutical salts of edible acidity 2～100 peptides and alkalescence 2～100 peptides, and their combination or mixture.

10. according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 are selected from hydrophilic following medicinal diluent: glyceraldehyde, dihydroxy acetone, erythritol, ribose, ribitol, deoxyribose, xylose, xylitol, arabinose, 1,2,3,4,5-pentanepentol, glucose, galactose, galactitol, mannitol, mannose, inosite, rhamnose, altrose, allose, fructose, sorbose, sorbitol, Tagatose, lyxose, mannoheptulose, Perseitol, sedoheptulose, sedoheptose alcohol, chalcose, Quinovose, cymarose, fucose, gluconolactone, lactose, lactose, sucrose, cellobiose, 6-(.alpha.-D-galactosido)-D-glucose., the Sargassum disaccharide, lactitol, maltose, maltose alcohol, dextrinose, hydroxyl isomaltulose, isomaltulose, lactulose, 6-O-.alpha.-L-rhamnosyl-D-glucose., vicianose, Raffinose, cellotriose, melezitose, stachyose, cellotetrose, verbascose, Fructus Hordei Germinatus three is to pentasaccharides, cellopentaose, Fructus Hordei Germinatus six to nine sugar, fiber six to nine sugar, dextrates, the Polyfructose. of the degree of polymerization 2～100, the IMO of the degree of polymerization 2～100, the IMO alcohol of the degree of polymerization 2～100, dextrin, glucosan, pulullan polysaccharide, Tragacanth, starch, pregelatinized Starch, modified starch, microcrystalline Cellulose, hydroxyl second methylcellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, methyl-α-/or β-/or gamma-cyclodextrin, hydroxypropyl-α-/or β-/or gamma-cyclodextrin, hydroxyl butyl-α-/or β-/or gamma-cyclodextrin, hydroxyethyl-α-/or β-/or gamma-cyclodextrin, hydroxyl cyclobutenyl-α-/or β-/or gamma-cyclodextrin, glucosyl group-α-/or β-/or gamma-cyclodextrin, malt-base-α-/or β-/or gamma-cyclodextrin, galactosyl-α-/or β-/or gamma-cyclodextrin, Pyrusussuriensis glycosyl-α-/or β-/or gamma-cyclodextrin, mannose group-α-/or β-/or gamma-cyclodextrin, malt-base-α-/or β-/or gamma-cyclodextrin base-glucose, widow or polysaccharide side chain-α-/or β-/or gamma-cyclodextrin, sulfobutyl ether-α-/or β-/or gamma-cyclodextrin and pharmaceutical salts thereof, sodium chloride, potassium chloride, calcium hydrogen phosphate, calcium glycerophosphate, bicarbonate, percarbonate, dihydric phosphate, disulfate, lactate, mutate, glucosaccharic acid salt, malate, citrate, tartrate, dihydroxytartaric acid salt, gluconate, the galacturonic acid hydrochlorate, glucuronate, Ascorbate, dehydroascorbic acid salt, the deoxidation Ascorbate, glucoascorbic acid salt, erythorbate, carboxyglutamic acid salt, ferulate, the glucoheptose hydrochlorate, glycyrrhetate, hydroxyglutamic acid salt, Lactobionate, sorbate, clavulanate, ribonucleotide and salt thereof, Deoxydization nucleotide and salt thereof, inosinic acid and salt thereof, Alpha-Methyl furan inosinic acid and salt thereof, adenylic acid and salt thereof, guanyl and salt thereof, cytidylic acid and salt thereof, uridylic acid and salt thereof, thymidylic acid and salt thereof, inosine monophosphate, IMP and salt thereof, xanthylic acid and salt thereof, phosphorylated amino acid and salt thereof, glutamic acid and pharmaceutical salts thereof, D-trp, L and/or D-Thr, D-Leu, D-phenylalanine, the D-methionine, D-Ile, D-His, L and/or D-Ser, D-Val, L and/or D-alanine, glycine, the L-hydroxyproline, L-PROLINE, D-Lys and pharmaceutical salts thereof, D-Arg and pharmaceutical salts thereof, L-glutaminate, comprise L and/or D-Thr, L and/or D-alanine, glycine, the L-hydroxyproline, L-PROLINE, lysine and pharmaceutical salts thereof, the dipeptides of arginine and pharmaceutical salts thereof or tripeptides, derive from the legume seed-protein, seeds of gramineous crops protein, amaranth seed protein, Sargassum protein matter, Radix hemerocalis plicatae protein, tuber crops tuber or rhizome protein, livestock products protein, the fowl white matter of laying eggs, aquatic product protein matter, the edible peptide of fibroin, and their hydrate, and their combination or mixture, above-mentioned salt is selected from sodium salt, potassium salt, calcium salt or magnesium salt.

11., according to the tablet of claim 1 or 2, it is characterized in that described diluent B 1 and/or diluent B 2 are selected from as its 150mg by the drift with diameter 8mm with 10～50kg/cm ²pressure show the sugar of 0～2kg hardness while making tablet, and described fusible saccharide D3 and/or medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from as its 150mg by the drift with diameter 8mm with 10～50kg/cm ²pressure show the sugar of 2kg or the above hardness of 2kg while making tablet.

12., according to the tablet of claim 1 or 2, the fusing point that it is characterized in that described fusible surfactant D 1 and/or fusible medicinal lipid additive D2 and/or fusible saccharide D3 is 35 to 150 ℃; And/or

The fusing point of described fusible lipophilic surfactant D11 or fusible medicinal lipid additive D21 is 35 to 150 ℃.

13., according to the tablet of claim 1 or 2, it is characterized in that the more described diluent of fusing point of described fusible surfactant D 1 and/or fusible medicinal lipid additive D2 and/or fusible saccharide D3 and/or fusible lipophilic surfactant D11 or fusible medicinal lipid additive D21 and/or the fusing point of described active component at least hang down 10 ℃.

14. the tablet according to claim 1 or 2, the fusing point that it is characterized in that the fusible surfactant D 1 in the more described fusible adhesion agent C1-1 of fusing point of the medical additive E1 in described fusible adhesion agent C1-1 is at least high 10 ℃, and/or at least low 10 ℃ of the fusing points of more described diluent and/or described active component; And/or

The fusing point of fusible medicinal lipid additive D2 in the more described fusible adhesion agent C1-2 of the fusing point of surfactant E2 in described fusible adhesion agent C1-2 is at least high 10 ℃, and/or the fusing point of more described diluent and/or described active component at least hangs down 10 ℃; And/or

The fusing point of medical additive E2 in described fusible adhesion agent C1-5 is higher than the fusing point of the fusible saccharide D3 in described fusible adhesion agent C1-5; And/or

Core core 1 in described fusible adhesion agent C1-6 or the fusing point of medical additive E3 are higher than the described fusible outer fusing point that covers thing D1; And/or

Core core 2 in described fusible adhesion agent C1-7 or the fusing point of medical additive E4 are higher than the described fusible outer fusing point that covers thing D2; And/or

The fusing point of the more described active components A 2 of fusing point of the fusible binding agent D1 in described fusible adhesion agent C2-1 is low; And/or

The fusing point that fusible outer in described fusible adhesion agent C2-2 covers the more described active components A 2 of fusing point of thing D3 or core core 3 is low.

15., according to the tablet of claim 1 or 2, it is characterized in that described surfactant D 1 is selected from the fusible lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester, Polyethylene Glycol glycerol high-grade aliphatic ester, the higher fatty acids of bound to polyglycerol, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, Polyethylene Glycol sterol ethers surfactant, Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester, Polyethylene Glycol senior alkyl ether, the glycosyl high-grade aliphatic ester, Polyethylene Glycol senior alkyl phenol ether, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, Polyethylene Glycol, polyethylene glycol oxide, polyoxy ethylene-polyoxy propylene-based block copolymer, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant D 11 is selected from the lipophilic fusible lower surfactant of fusing point higher than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester, Polyethylene Glycol glycerol high-grade aliphatic ester, the higher fatty acids of bound to polyglycerol, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, Polyethylene Glycol sterol ethers surfactant, Polyethylene Glycol senior alkyl ether, the glycosyl high-grade aliphatic ester, Polyethylene Glycol senior alkyl phenol ether, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 10000Da to 20, the Polyethylene Glycol of 000Da, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E2 is selected from the lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester, Polyethylene Glycol glycerol high-grade aliphatic ester, the higher fatty acids of bound to polyglycerol, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, Polyethylene Glycol sterol ethers surfactant, Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester, Polyethylene Glycol senior alkyl ether, the glycosyl high-grade aliphatic ester, Polyethylene Glycol senior alkyl phenol ether, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, Polyethylene Glycol, polyethylene glycol oxide, polyoxy ethylene-polyoxy propylene-based block copolymer, ionic surfactant, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E21 is selected from the hydrophilic lower surfactant of fusing point lower than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester, Polyethylene Glycol glycerol high-grade aliphatic ester, the higher fatty acids of bound to polyglycerol, glycerol one high-grade aliphatic ester, Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester, Polyethylene Glycol senior alkyl ether, glycosyl list high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol list high-grade aliphatic ester, Polyethylene Glycol, polyoxy ethylene-polyoxy propylene-based block copolymer, the polybasic carboxylic acid list high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that single senior alkyl alcohol glycerol carbon number is C2～C6, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32.

16., according to the tablet of claim 1 or 2, it is characterized in that described surfactant D 1 is selected from the fusible lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 200, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 100, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～20, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 2 to 100, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 100, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 2 to 100, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 800Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 10, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 5%～95%, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant D 11 is selected from the lipophilic fusible lower surfactant of fusing point higher than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 6, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 6, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 2 to 6, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 10,000Da to 20, the Polyethylene Glycol of 000Da, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E2 is selected from the lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 200, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 100, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～20, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 2 to 100, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 100, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 2 to 100, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 800Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 10, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 5%～95%, ionic surfactant, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E21 is selected from the hydrophilic lower surfactant of fusing point lower than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 80, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 60, single higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～20, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 60, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 8 to 80, glycosyl list high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol list high-grade aliphatic ester, the polybasic carboxylic acid list high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that single senior alkyl alcohol glycerol carbon number is C2～C6, the Polyethylene Glycol of mean molecule quantity from 200Da to 800Da, mean molecule quantity is 1000～3000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～95%, and their combination, wherein, described higher fatty acids is fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, described senior alkyl is alkyl or its hydroxylating alkyl that carbon number is C8～C32,

Wherein, the ionic surfactant in above-mentioned surfactant E2 is selected from senior alkyl three ammonium halogenide, senior alkyl trimethyl ammonium halogenide, senior alkyl trimethyl ammonium halogenide, senior alkyl ammonium halogenide, senior alkyl benzyl dimethyl ammonium medicinal salts, diisobutyl phenoxy group ethyoxyl dimethyl benzyl ammonium medicinal salts, senior alkyl pyridine medicinal salts, the betanin that comprises senior alkyl in molecular structure, in molecular structure, comprise senior alkyl by the amine of ethoxyquin, N-senior alkyl acylamino acid pharmaceutical salts, N-senior alkyl acylsarcosine pharmaceutical salts, the alkane esters pharmaceutical salts that the senior alkane acyl of N-basic amino acid carbon number is C1-C6, N-senior alkyl Gemini class basic amino acid pharmaceutical salts surfactant, the alkyl acyl that the N-carbon number is C1-C12-basic amino acid senior alkyl glyceride medicinal salts surfactant, senior alkyl 2-Sulfosuccinic acid pharmaceutical salts, senior alkyl ether-2 2-Sulfosuccinic acid pharmaceutical salts, the alkane sulfonic acid pharmaceutical salts that senior alkyl acyl methylamine carbon number is C1～C6, senior alkyl sulphuric acid pharmaceutical salts, senior alkyl carboxylic acid pharmaceutical salts, senior alkyl taurine pharmaceutical salts, senior alkyl ether sulphuric acid pharmaceutical salts, senior alkyl glyceryl ether sulfonic acid pharmaceutical salts esters, senior alkyl fatty alcohol-polyoxyethylene ether sulphuric acid pharmaceutical salts, the medicinal alkali of sulfonic acid is for succinic acid two higher alkyl esters, multi-carboxylate's pharmaceutical salts that senior alkyl acyl glycerol carbon number is C2～C6, the caseinic acid pharmaceutical salts, multi-carboxylate's pharmaceutical salts that senior alkyl acyl propylene glycol carbon number is C2～C6, multi-carboxylate's pharmaceutical salts that senior alkyl acyl group carbon number is C2～C6, senior alkyl acyl group lactic acid pharmaceutical salts, cholic acid medicinal salts surfactant, alginic acid pharmaceutical salts, and their mixture, wherein, the saturated or unsaturated alkyl that described senior alkyl is carbon number C8-C32 or its hydroxylating alkyl.

17., according to the tablet of claim 1 or 2, it is characterized in that described surfactant D 1 is selected from the fusible lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 150, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 10 to 60, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 4 to 50, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 60, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 4 to 60, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 4, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 20%～90%, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant D 11 is selected from the lipophilic fusible lower surfactant of fusing point higher than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 6, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 2 to 6, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 2 to 6, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 10,000Da to 20, the Polyethylene Glycol of 000Da, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E2 is selected from the lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 150, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 10 to 60, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 4 to 50, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 60, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 4 to 60, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 4, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 20%～90%, ionic surfactant, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E21 is selected from the hydrophilic lower surfactant of fusing point lower than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 60, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 10 to 60, single higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 40, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 8 to 60, glycosyl list high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol list high-grade aliphatic ester, the polybasic carboxylic acid list high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that single senior alkyl alcohol glycerol carbon number is C2～C6, the Polyethylene Glycol of mean molecule quantity from 200Da to 800Da, mean molecule quantity is 1000～3000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～90%, and their combination, wherein, described higher fatty acids be the carbon number side chain that is C8～C32 and/or unsaturated fatty acid or its hydroxylating fatty acid or be carbon number be C8～C14 saturated positive fatty acid or its hydroxylating fatty acid, described senior alkyl be the carbon number side chain that is C8～C32 and/or unsaturated alkyl or its hydroxylating alkyl or be carbon number be C8～C14 saturated positive alkyl or its hydroxylating alkyl,

Wherein, the ionic surfactant in above-mentioned surfactant E2 is selected from dioctyl 2-Sulfosuccinic acid pharmaceutical salts, octyl group 2-Sulfosuccinic acid pharmaceutical salts, the lauryl sulphate acid pharmaceutical salts, myristyl sulphuric acid pharmaceutical salts, ten to the octadecanoid acid pharmaceutical salts, the castor oil acid pharmaceutical salts, ten acid of acetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of acetyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of diacetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of diacetyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of oxalyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of oxalyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, mix acetic acid pharmaceutical salts and ten acid of tartaric acid pharmaceutical salts glycerol list to the behenic acid ester, mix two ten acid of acetic acid pharmaceutical salts and tartaric acid pharmaceutical salts glycerol to the behenic acid ester, ten acid of citric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of citric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of succinic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of succinic acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of lactic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of lactic acid pharmaceutical salts glycerol are to the behenic acid ester, ten to tadenan citric acid pharmaceutical salts glyceryl monoacetate, ten acid are to behenic acid acyl citric acid pharmaceutical salts ester, tartaric acid pharmaceutical salts Dan Shizhi docosane acyl ester, ten to docosane acyl butene dioic acid pharmaceutical salts, ten to docosane acyl propylene glycol succinate pharmaceutical salts, decoyl lactic acid pharmaceutical salts, caprinoyl lactic acid pharmaceutical salts, lauroyl lactic acid pharmaceutical salts, tetradecylic acid lactic acid pharmaceutical salts, hexadecylic acid lactic acid pharmaceutical salts, stearoyl lactic acid pharmaceutical salts, isostearoyl lactic acid pharmaceutical salts, oleoyl lactic acid pharmaceutical salts, cocos nucifera oil acyl lactic acid pharmaceutical salts, 12-hydroxyl stearoyl lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, Semen Ricini oleoyl lactic acid pharmaceutical salts, 20 to docosane acyl group lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, stearic acid lactic acid pharmaceutical salts, N-12 is to docosane acylglycine pharmaceutical salts, N-12 is to docosane acyl group alanine pharmaceutical salts, N-12 is to docosane acyl group valine pharmaceutical salts, N-12 is to docosane acyl glutamic acid pharmaceutical salts, N-12 is to docosane acyl acylaspartic acid pharmaceutical salts, N-12 is to docosane acyl group-N-methyl-Beta-alanine pharmaceutical salts, two-TEA-palmityl aspartic acid pharmaceutical salts, 12 to docosane acyl group sarcosine pharmaceutical salts, the cholic acid pharmaceutical salts, the taurocholic acid pharmaceutical salts, the deoxycholic acid pharmaceutical salts, the glycocholic acid pharmaceutical salts, the glycodesoxycholic acid pharmaceutical salts, the tauroursodeoxycholic acid pharmaceutical salts, the ursodesoxycholic acid pharmaceutical salts, the chenodeoxycholic acid pharmaceutical salts, the chenodeoxycholyltaurine pharmaceutical salts, the glycochenodeoxycholate pharmaceutical salts, 12 to docosane acyl glycyl for the propylhomoserin pharmaceutical salts, the caseinic acid pharmaceutical salts, N α-ten are to two lauroyl arginine pharmaceutical salts methyl ester, N α-ten are to two lauroyl arginine pharmaceutical salts ethyl esters, N α-ten are to two lauroyl lysine methyl esters, N α-ten are to two lauroyl ethyl ester of lysine, N α-ten are to two lauroyl histidine pharmaceutical salts methyl ester, N α-ten are to two lauroyl histidine pharmaceutical salts ethyl esters, N1, N3-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,3-propane diamine, N1, N6-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl arginine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl lysine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl histidine pharmaceutical salts)-1,9-nonamethylene diamine, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group histidyl-pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl histidyl-pharmaceutical salts) glycerol, N-Cortex cocois radicis acyl arginine-ethyl ester of lysine pharmaceutical salts, and composition thereof.

18., according to the tablet of claim 1 or 2, it is characterized in that described surfactant D 1 is selected from the fusible lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 100, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 10 to 50, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 4 to 40, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 40, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 4 to 50, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 1, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 30%～85%, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E2 is selected from the lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 100, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 10 to 50, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 4 to 40, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 40, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 4 to 50, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 1, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 30%～85%, ionic surfactant, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E21 is selected from the hydrophilic lower surfactant of fusing point lower than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 50, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 10 to 40, single higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 30, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 8 to 50, glycosyl list high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol list high-grade aliphatic ester, the polybasic carboxylic acid list high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that single senior alkyl alcohol glycerol carbon number is C2～C6, the Polyethylene Glycol of mean molecule quantity from 200Da to 800Da, mean molecule quantity is 1000～3000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～85%, and their combination, wherein, described higher fatty acids be the carbon number side chain that is C8～C32 and/or unsaturated fatty acid or its hydroxylating fatty acid or be carbon number be C8～C14 saturated positive fatty acid or its hydroxylating fatty acid, described senior alkyl be the carbon number side chain that is C8～C32 and/or unsaturated alkyl or its hydroxylating alkyl or be carbon number be C8～C14 saturated positive alkyl or its hydroxylating alkyl,

Wherein, the ionic surfactant in above-mentioned surfactant E2 is selected from dioctyl 2-Sulfosuccinic acid pharmaceutical salts, octyl group 2-Sulfosuccinic acid pharmaceutical salts, the lauryl sulphate acid pharmaceutical salts, myristyl sulphuric acid pharmaceutical salts, ten to the octadecanoid acid pharmaceutical salts, the castor oil acid pharmaceutical salts, ten acid of acetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of acetyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of diacetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of diacetyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of oxalyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of oxalyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, mix acetic acid pharmaceutical salts and ten acid of tartaric acid pharmaceutical salts glycerol list to the behenic acid ester, mix two ten acid of acetic acid pharmaceutical salts and tartaric acid pharmaceutical salts glycerol to the behenic acid ester, ten acid of citric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of citric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of succinic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of succinic acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of lactic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of lactic acid pharmaceutical salts glycerol are to the behenic acid ester, ten to tadenan citric acid pharmaceutical salts glyceryl monoacetate, ten acid are to behenic acid acyl citric acid pharmaceutical salts ester, tartaric acid pharmaceutical salts Dan Shizhi docosane acyl ester, ten to docosane acyl butene dioic acid pharmaceutical salts, ten to docosane acyl propylene glycol succinate pharmaceutical salts, decoyl lactic acid pharmaceutical salts, caprinoyl lactic acid pharmaceutical salts, lauroyl lactic acid pharmaceutical salts, tetradecylic acid lactic acid pharmaceutical salts, hexadecylic acid lactic acid pharmaceutical salts, stearoyl lactic acid pharmaceutical salts, isostearoyl lactic acid pharmaceutical salts, oleoyl lactic acid pharmaceutical salts, cocos nucifera oil acyl lactic acid pharmaceutical salts, 12-hydroxyl stearoyl lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, Semen Ricini oleoyl lactic acid pharmaceutical salts, 20 to docosane acyl group lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, stearic acid lactic acid pharmaceutical salts, N-12 is to docosane acylglycine pharmaceutical salts, N-12 is to docosane acyl group alanine pharmaceutical salts, N-12 is to docosane acyl group valine pharmaceutical salts, N-12 is to docosane acyl glutamic acid pharmaceutical salts, N-12 is to docosane acyl acylaspartic acid pharmaceutical salts, N-12 is to docosane acyl group-N-methyl-Beta-alanine pharmaceutical salts, two-TEA-palmityl aspartic acid pharmaceutical salts, 12 to docosane acyl group sarcosine pharmaceutical salts, the cholic acid pharmaceutical salts, the taurocholic acid pharmaceutical salts, the deoxycholic acid pharmaceutical salts, the glycocholic acid pharmaceutical salts, the glycodesoxycholic acid pharmaceutical salts, the tauroursodeoxycholic acid pharmaceutical salts, the ursodesoxycholic acid pharmaceutical salts, the chenodeoxycholic acid pharmaceutical salts, the chenodeoxycholyltaurine pharmaceutical salts, the glycochenodeoxycholate pharmaceutical salts, 12 to docosane acyl glycyl for the propylhomoserin pharmaceutical salts, N α-ten are to two lauroyl arginine pharmaceutical salts methyl ester, N α-ten are to two lauroyl arginine pharmaceutical salts ethyl esters, N α-ten are to two lauroyl lysine methyl esters, N α-ten are to two lauroyl ethyl ester of lysine, N α-ten are to two lauroyl histidine pharmaceutical salts methyl ester, N α-ten are to two lauroyl histidine pharmaceutical salts ethyl esters, N1, N3-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,3-propane diamine, N1, N6-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl arginine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl lysine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl histidine pharmaceutical salts)-1,9-nonamethylene diamine, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group histidyl-pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl histidyl-pharmaceutical salts) glycerol, the caseinic acid pharmaceutical salts, N-Cortex cocois radicis acyl arginine-ethyl ester of lysine pharmaceutical salts, and composition thereof, above-mentioned salt is selected from sodium salt, or potassium salt, or ammonium salt.

19., according to the tablet of claim 1 or 2, it is characterized in that described surfactant D 1 is selected from the fusible lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 60, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 20 to 50, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 8 to 40, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 20, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 8 to 40, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 500, the polyethylene glycol oxide of 000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～85%, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E2 is selected from the lower surfactant that fusing point is not less than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 60, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 20 to 50, the higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, propylene glycol or glycol monomethyl high-grade aliphatic ester, glycerol one high-grade aliphatic ester and glycerol two high-grade aliphatic esters, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 8 to 40, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 20, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 8 to 40, the glycosyl high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol high-grade aliphatic ester, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, lecithin, by hydroxylated lecithin, defat acid phosphatidyl choline, phosphatidylcholine, the phosphatidyl ethanolamine, the phosphatidyl glycerol, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 500, the polyethylene glycol oxide of 000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～85%, ionic surfactant, and their combination, wherein, described higher fatty acids is saturated positive fatty acid or its hydroxylating fatty acid that carbon number is C8～C32, and described senior alkyl is saturated positive alkyl or its hydroxylating alkyl that carbon number is C8～C32, and/or

Described surfactant E21 is selected from the hydrophilic lower surfactant of fusing point lower than 25 ℃ of temperature: the Polyethylene Glycol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 8 to 40, the Polyethylene Glycol glycerol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 20 to 50, single higher fatty acids of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10, the Polyethylene Glycol anhydrous sorbitol high-grade aliphatic ester that the average polymerization number of polyethylene glycol groups is 4 to 20, the polybasic carboxylic acid list high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that single senior alkyl alcohol glycerol carbon number is C2～C6, the Polyethylene Glycol senior alkyl ether that the average polymerization number of polyethylene glycol groups is 8 to 40, glycosyl list high-grade aliphatic ester, tetramethylolmethane or anhydrous sorbitol list high-grade aliphatic ester, the Polyethylene Glycol of mean molecule quantity from 200Da to 800Da, mean molecule quantity is 1000～3000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～85%, and their combination, wherein, described higher fatty acids be the carbon number side chain that is C8～C32 and/or unsaturated fatty acid or its hydroxylating fatty acid or be carbon number be C8～C14 saturated positive fatty acid or its hydroxylating fatty acid, described senior alkyl be the carbon number side chain that is C8～C32 and/or unsaturated alkyl or its hydroxylating alkyl or be carbon number be C8～C14 saturated positive alkyl or its hydroxylating alkyl,

Wherein, the hydrochlorate of selecting oneself of the ionic surfactant in above-mentioned surfactant E2, caprylate, caprate, laruate, myristate, palmitate, the Petiolus Trachycarpi oil hydrochlorate, oleate, ricinoleate, linoleate, linolenate, stearate, lauryl sulfate, tetradecyl sulfate, the lauryl sarcosinate, the dioctyl sulfosuccinate, cholate, taurocholate, glycocholate, dexycholate, taurodeoxycholate, glycodeoxycholate, ursodeoxycholate, chenodesoxy cholate, cattle sulphur chenodesoxy cholate, the glyceryl chenodesoxy cholate, CHOLYLSARCOSINE salt, N-formyl taurocholate, succinyl monoglyceride salt, stearoyl propylene glycol succinate, monoacylphosphine tartrate monoglyceride and diester, diacetyl group tartrate monoglyceride and diester, citrate monoglyceride diester, glycerol lactate high-grade aliphatic ester, ten to the octadecanoyl lactate, stearoyl-2 lactoyl salt, alginate, and composition thereof, above-mentioned salt is sodium salt, or potassium salt or ammonium salt.

20. the tablet according to claim 15 to any one in 19, it is characterized in that fatty acid in described surfactant D 1 and/or surfactant E2 or the carbon number of its hydroxylating fatty acid are C12～C22, the alkyl in described surfactant D 1 and/or surfactant E2 or the carbon number of its hydroxylating alkyl are C12～C22; And/or the fatty acid in described surfactant E21 be the carbon number side chain that is C8～C22 and/or unsaturated fatty acid or its hydroxylating fatty acid or be carbon number be C8～C12 saturated positive fatty acid or its hydroxylating fatty acid, the alkyl in described surfactant E21 be the carbon number side chain that is C8～C22 and/or unsaturated alkyl or its hydroxylating alkyl or be carbon number be C8～C12 saturated positive alkyl or its hydroxylating alkyl.

21. the tablet according to claim 15 to any one in 19, it is characterized in that fatty acid in described surfactant D 1 and/or surfactant E2 or the carbon number of its hydroxylating fatty acid are C14～C18, the alkyl in described surfactant D 1 and/or surfactant E2 or the carbon number of its hydroxylating alkyl are C14～C18; And/or the fatty acid in described surfactant E21 be the carbon number side chain that is C8～C18 and/or unsaturated fatty acid or its hydroxylating fatty acid or be carbon number be C8～C12 saturated positive fatty acid or its hydroxylating fatty acid, the alkyl in described surfactant E21 be the carbon number side chain that is C8～C18 and/or unsaturated alkyl or its hydroxylating alkyl or be carbon number be C8～C12 saturated positive alkyl or its hydroxylating alkyl.

22. the tablet according to claim 15 to any one in 19, it is characterized in that fatty acid in described surfactant D 1 and/or surfactant E2 or the carbon number of its hydroxylating fatty acid are C16～C18, the alkyl in described surfactant D 1 and/or surfactant E2 or the carbon number of its hydroxylating alkyl are C16～C18; And/or the fatty acid in described surfactant E21 be the carbon number side chain that is C16～C18 and/or unsaturated fatty acid or its hydroxylating fatty acid or be carbon number be C8～C12 saturated positive fatty acid or its hydroxylating fatty acid, the alkyl in described surfactant E21 be the carbon number side chain that is C16～C18 and/or unsaturated alkyl or its hydroxylating alkyl or be carbon number be C8～C12 saturated positive alkyl or its hydroxylating alkyl.

23., according to the tablet of claim 1 or 2, it is characterized in that described surfactant D 1 and/or surfactant E2 are selected from the lower surfactant that fusing point is not less than 25 ℃ of temperature: the polyglycol distearate that the average polymerization number of polyethylene glycol groups is 2 to 150, the Polyethylene Glycol cetylate that the average polymerization number of polyethylene glycol groups is 10 to 150, the polyethylene glycol laurate that the average polymerization number of polyethylene glycol groups is 20 to 120, the Polyethylene Glycol myristate that the average polymerization number of polyethylene glycol groups is 20 to 120, the polyoxyethylene hydrogenated Oleum Ricini condensation substance that polyoxyethylene groups average polymerization number is 40 to 200, the polyoxyethylene castor oil condensation substance that polyoxyethylene groups average polymerization number is 90 to 200, the Polyethylene Glycol lauryl alcohol that the average polymerization number of polyethylene glycol groups is 23 to 100, the Polyethylene Glycol Semen Myristicae alcohol ether that the average polymerization number of polyethylene glycol groups is 23 to 100, the Polyethylene Glycol spermaceti alcohol ether that the average polymerization number of polyethylene glycol groups is 2 to 100, the stearic alcohol ether of the Polyethylene Glycol that the average polymerization number of polyethylene glycol groups is 2 to 100, the Polyethylene Glycol oleyl alcohol ether that the average polymerization number of polyethylene glycol groups is 20 to 100, the polyethylene glycol glycerol stearate that the average polymerization number of polyethylene glycol groups is 10 to 100, the polyethylene glycol glycerol cetylate that the average polymerization number of polyethylene glycol groups is 10 to 100, the polyethylene glycol glycerol myristate that the average polymerization number of polyethylene glycol groups is 20 to 100, the polyethylene glycol glycerol lauric acid acid esters that the average polymerization number of polyethylene glycol groups is 20 to 100, Polyethylene Glycol (4) sorbitan monostearate, Polyethylene Glycol (20) anhydrous sorbitol tristearate, the anhydrous sorbitol monopalmitate, sorbitan monostearate, No. 4, POGE-A POGE-B POGE-C Polyglycerin palmitate, polyglycereol-6 stearate, the Natrulon H-10 stearate, the Natrulon H-10 distearate, fertility base PEG-1000 succinate (TPGS), sucrose monostearate, sucrose palmitic acid ester, sucrose list myristate, sucrose monolaurate, Macrogol15Hydroxystearate, glycerol list myristate, glycerol mono laurate acid esters, glycerol Dan Zhengkui acid esters, glycerol list caprylic acid ester, ten acid of acetyl tartaric acid glycerol list are to the behenic acid ester, two ten acid of acetyl tartaric acid glycerol are to the behenic acid ester, ten acid of diacetyl tartaric acid glycerol list are to the behenic acid ester, two ten acid of diacetyl tartaric acid glycerol are to the behenic acid ester, ten acid of oxalyl tartaric acid glycerol list are to the behenic acid ester, two ten acid of oxalyl tartaric acid glycerol are to the behenic acid ester, mix acetic acid and ten acid of tartaric acid glycerol list to the behenic acid ester, mix two ten acid of acetic acid and tartaric acid glycerol to the behenic acid ester, ten acid of citric acid glycerol list are to the behenic acid ester, two ten acid of citric acid glycerol are to the behenic acid ester, two ten acid of succinic acid glycerol are to the behenic acid ester, ten acid of succinic acid glycerol list are to the behenic acid ester, ten acid of tartaric acid glycerol list are to the behenic acid ester, two ten acid of tartaric acid glycerol are to the behenic acid ester, ten acid of lactic acid glycerol list are to the behenic acid ester, two ten acid of lactic acid glycerol are to the behenic acid ester, ten to tadenan citric acid glyceryl monoacetate, ten to tadenan citric acid glycerol bisgallic acid ester, tetradecylic acid is to behenic acid acyl citrate, tartaric acid Dan Shisi is to docosane acyl ester, 14 to docosane acyl butene dioic acid, 12 to docosane acyl propylene glycol succinate, N α-ten are to two lauroyl arginine methyl esters, N α-ten are to two lauroyl arginine ethyl esters, N α-ten are to two lauroyl lysine methyl esters, N α-ten are to two lauroyl ethyl ester of lysine, N α-ten are to two lauroyl histidine methyl ester, N α-ten are to two lauroyl histidine ethyl esters, N1, N3-bis-(N-ten to two lauroyl arginine/or lysine/or histidine)-1, the 3-propane diamine, N1, N3-bis-(N-ten to two lauroyl arginine)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl lysines)-1,3-propane diamine, N1, N6-bis-(N-ten to two lauroyl histidine)-1,6-hexamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl arginine)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl lysines)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl histidine)-1,9-nonamethylene diamine, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group arginyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group lysyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group histidyl-) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl arginyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl lysyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl histidyl-) glycerol, N-ten to two lauroyl arginine-ethyl ester of lysine, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 100, the polyethylene glycol oxide of 000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～85%, and their combination, and/or

Described surfactant D 11 is selected from the lipophilic lower surfactant of fusing point higher than 25 ℃ of temperature: Span60, the anhydrous sorbitol cetylate, xylitol acid anhydride stearic acid fat, sucrose stearate, sucrose palmitate, glycerol list myristate, the two myristates of glycerol, glycerol dilaurate acid esters, glycerol mono laurate acid esters, the two positive certain herbaceous plants with big flowers acid esters of glycerol, glycerol Dan Zhengkui acid esters, propylene glycol monostearate, the propylene glycol hydroxy stearic acid ester, the stearic acid ethylene glycol ester, the Palmic acid ethylene glycol ester, stearic acid diethylene glycol monoesters, ten acid of acetyl tartaric acid glycerol list are to the behenic acid ester, two ten acid of acetyl tartaric acid glycerol are to the behenic acid ester, ten acid of diacetyl tartaric acid glycerol list are to the behenic acid ester, two ten acid of diacetyl tartaric acid glycerol are to the behenic acid ester, ten acid of oxalyl tartaric acid glycerol list are to the behenic acid ester, two ten acid of oxalyl tartaric acid glycerol are to the behenic acid ester, mix acetic acid and ten acid of tartaric acid glycerol list to the behenic acid ester, mix two ten acid of acetic acid and tartaric acid glycerol to the behenic acid ester, ten acid of citric acid glycerol list are to the behenic acid ester, two ten acid of citric acid glycerol are to the behenic acid ester, ten acid of succinic acid glycerol list are to the behenic acid ester, two ten acid of succinic acid glycerol are to the behenic acid ester, ten acid of tartaric acid glycerol list are to the behenic acid ester, two ten acid of tartaric acid glycerol are to the behenic acid ester, ten acid of lactic acid glycerol list are to the behenic acid ester, two ten acid of lactic acid glycerol are to the behenic acid ester, ten to tadenan citric acid glyceryl monoacetate, ten to tadenan citric acid glycerol bisgallic acid ester, tetradecylic acid is to behenic acid acyl citrate, tartaric acid Dan Shisi is to docosane acyl ester, 14 to docosane acyl butene dioic acid, 12 to docosane acyl propylene glycol succinate, the surfactant that molecular structural formula and commodity Gelucire-46/07 or Gelucire-48/09 or Gelucire-50/02 or Gelucire-62/05 are identical, mean molecule quantity is from 10,000Da to 20, the Polyethylene Glycol of 000Da, and their combination, and/or

Described surfactant E21 is selected from the hydrophilic lower surfactant of fusing point lower than 25 ℃ of temperature: the polyethylene glycol laurate that the average polymerization number of polyethylene glycol groups is 8 to 15, the polyoxyethylene hydrogenated Oleum Ricini condensation substance that polyoxyethylene groups average polymerization number is 8 to 35, the polyoxyethylene castor oil condensation substance that polyoxyethylene groups average polymerization number is 8 to 60, the Polyethylene Glycol lauryl alcohol that the average polymerization number of polyethylene glycol groups is 8 to 15, the Polyethylene Glycol oleyl alcohol ether that the average polymerization number of polyethylene glycol groups is 8 to 15, the polyoxyethylene oleate that polyoxyethylene groups average polymerization number is 6 to 15, the sorbitol four olein polyoxyethylene ether that polyoxyethylene groups average polymerization number is 8 to 60, the sorbitol tetrastearate polyoxyethylene ether that polyoxyethylene groups average polymerization number is 12 to 60, the sorbitol four cetylate polyoxyethylene ether that polyoxyethylene groups average polymerization number is 12 to 60, the sorbitol four myristate polyoxyethylene ether that polyoxyethylene groups average polymerization number is 12 to 60, sorbitol cinnamic acid in the April acid esters polyoxyethylene ether that polyoxyethylene groups average polymerization number is 12 to 60, Emulsifier LT-60M, polyoxyethylene xylitol acid anhydride monopalmitate, polyoxyethylene xylitol acid anhydride list myristate, polyoxyethylene xylitol acid anhydride mono laurate acid esters, the Polyethylene Glycol dehydration Pyrusussuriensis mono laurate acid esters that the average polymerization number of polyethylene glycol groups is 4 to 20, the Polyethylene Glycol dehydration Pyrusussuriensis monoleate that the average polymerization number of polyethylene glycol groups is 4 to 20, the Polyethylene Glycol dehydration Pyrusussuriensis monostearate that the average polymerization number of polyethylene glycol groups is 12 to 20, the Polyethylene Glycol dehydration Pyrusussuriensis monopalmitate that the average polymerization number of polyethylene glycol groups is 12 to 20, the Polyethylene Glycol dehydration Pyrusussuriensis mono laurate acid esters that the average polymerization number of polyethylene glycol groups is 12 to 20, the Polyethylene Glycol dehydration Pyrusussuriensis list myristate that the average polymerization number of polyethylene glycol groups is 12 to 20, the Polyethylene Glycol dehydration Pyrusussuriensis trioleate that the average polymerization number of polyethylene glycol groups is 12 to 22, the Polyethylene Glycol glycerol oils acid esters that the average polymerization number of polyethylene glycol groups is 8 to 20, Linoleoyl and oleoyl polyoxylglycerides, No. 4, polyglycereol laurate, No. 4, polyglycerol acrylate, sorbitan monooleate, sucrose base monoleate, N α-ten are to two lauroyl arginine methyl esters, N α-ten are to two lauroyl arginine ethyl esters, N α-ten are to two lauroyl lysine methyl esters, N α-ten are to two lauroyl ethyl ester of lysine, N α-ten are to two lauroyl histidine methyl ester, N α-ten are to two lauroyl histidine ethyl esters, N1, N3-bis-(N-ten to two lauroyl arginine)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl lysines)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl histidine)-1,3-propane diamine, N1, N6-bis-(N-ten to two lauroyl arginine)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl lysines)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl histidine)-1,6-hexamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl arginine)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl lysines)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl histidine)-1,9-nonamethylene diamine, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group arginyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group lysyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group histidyl-) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl arginyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl lysyl) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl histidyl-) glycerol, N-ten to two lauroyl arginine-ethyl ester of lysine, the Polyethylene Glycol of mean molecule quantity from 200Da to 800Da, mean molecule quantity is 1000～3000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 40%～85%, and their combination.

24., according to the tablet of claim 1 or 2, it is characterized in that described medicinal lipid additive D2 is selected from the fusible following medical additive that fusing point is not less than 25 ℃ of temperature: carbon number is C8 or more senior higher fatty acids glyceride, carbon number is C16 or more senior higher fatty acids propylene glycol ester, carbon number is C14 or more senior higher fatty acids glycol ester, carbon number is C16 or more senior higher fatty acids binaryglycol ester, carbon number is C10 or more senior higher fatty acids, carbon number is C12 or more senior high fatty alcohol, carbon number is that C14 or more senior higher fatty acids and carbon number are the fat that C14 or more senior high fatty alcohol form, the higher fatty acids that carbon number is C12 and carbon number are the fat that C18 or more senior high fatty alcohol form, carbon number is the fat that high fatty alcohol that C18 or more senior higher fatty acids and carbon number are C12 forms, carbon number is C31 or more senior aliphatic hydrocarbon, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof, and their combination, and/or

Described medicinal lipid additive D21 is selected from the fusible following medical additive of fusing point higher than 25 ℃ of temperature: carbon number is C8 or more senior higher fatty acids glyceride, carbon number is C16 or more senior higher fatty acids propylene glycol ester, carbon number is C14 or more senior higher fatty acids glycol ester, carbon number is C16 or more senior higher fatty acids binaryglycol ester, carbon number is C10 or more senior higher fatty acids, carbon number is C12 or more senior high fatty alcohol, carbon number is that C14 or more senior higher fatty acids and carbon number are the fat that C14 or more senior high fatty alcohol form, the higher fatty acids that carbon number is C12 and carbon number are the fat that C18 or more senior high fatty alcohol form, carbon number is the fat that high fatty alcohol that C18 or more senior higher fatty acids and carbon number are C12 forms, carbon number is C31 or more senior aliphatic hydrocarbon, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof, and their combination.

25., according to the tablet of claim 1 or 2, it is characterized in that described medicinal lipid additive D2 is selected from the fusible following medical additive that fusing point is not less than 25 ℃ of temperature: the higher fatty acids glyceride that carbon number is C8～C32, the higher fatty acids propylene glycol ester that carbon number is C16～C32, the higher fatty acids glycol ester that carbon number is C14～C32, the higher fatty acids binaryglycol ester that carbon number is C16～C32, the higher fatty acids that carbon number is C10～C32, the high fatty alcohol that carbon number is C14～C32, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C14～C36 and carbon number are C14～C36 forms, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C12 and carbon number are C18～C36 forms, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C18～C36 and carbon number are C12 forms, the aliphatic hydrocarbon that carbon number is C31～C70, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof, and their combination, and/or

Described medicinal lipid additive D21 is selected from the fusible following medical additive of fusing point higher than 25 ℃ of temperature: the higher fatty acids glyceride that carbon number is C8～C32, the higher fatty acids propylene glycol ester that carbon number is C16～C32, the higher fatty acids glycol ester that carbon number is C14～C32, the higher fatty acids binaryglycol ester that carbon number is C16～C32, the higher fatty acids that carbon number is C10～C32, the high fatty alcohol that carbon number is C14～C32, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C14～C36 and carbon number are C14～C36 forms, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C12 and carbon number are C18～C36 forms, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C18～C36 and carbon number are C12 forms, the aliphatic hydrocarbon that carbon number is C31～C70, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof, and their combination.

26. the tablet according to claim 1 or 2, it is characterized in that described medicinal lipid additive D2 is selected from the fusible following medical additive that fusing point is not less than 25 ℃ of temperature: the higher fatty acids glyceride that carbon number is C8～C22, the higher fatty acids propylene glycol ester that carbon number is C16～C22, the higher fatty acids glycol ester that carbon number is C14～C22, the higher fatty acids binaryglycol ester that carbon number is C16～C22, the higher fatty acids that carbon number is C10～C22, the high fatty alcohol that carbon number is C14～C22, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C16～C36 and carbon number are C16～C36 forms, the aliphatic hydrocarbon that carbon number is C41～C70, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof, and their combination, and/or

Described medicinal lipid additive D21 is selected from the fusible following medical additive of fusing point higher than 25 ℃ of temperature: the higher fatty acids glyceride that carbon number is C10～C22, the higher fatty acids propylene glycol ester that carbon number is C18～C22, the higher fatty acids glycol ester that carbon number is C18～C22, the higher fatty acids binaryglycol ester that carbon number is C18～C22, the higher fatty acids that carbon number is C14～C22, the high fatty alcohol that carbon number is C16～C22, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C16～C36 and carbon number are C16～C36 forms, the aliphatic hydrocarbon that carbon number is C41～C57, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof, and their combination.

27. according to claim 24,25,26 tablet, it is characterized in that described natural product and processed goods thereof are selected from Synthetic Spermacet, spermaceti, Brazil wax, bayberry wax, candelilla wax, yellow beeswax or cera alba, montan wax, rice bran wax, Cera Chinensis, shellac wax, sugarcane wax, Japanese fine wax, Chinese haze tallow, castor oil hydrogenated, hydrogenated vegetable oil, and their mixture.

28., according to the tablet of claim 1 or 2, it is characterized in that described fusible saccharide D3 is selected from monosaccharide and sugar alcohol, disaccharide and sugar alcohol thereof, trisaccharide and sugar alcohol thereof, and their combination.

29. the tablet according to claim 1 or 2, it is characterized in that described fusible saccharide D3 is selected from glyceraldehyde, dihydroxy acetone, erythritol, ribose, ribitol, deoxyribose, xylose, xylitol, arabinose, 1,2,3,4,5-pentanepentol, glucose, galactose, galactitol, mannitol, mannose, rhamnose, altrose, allose, fructose, sorbose, sorbitol, Tagatose, lyxose, mannoheptulose, Perseitol, sedoheptulose, chalcose, Quinovose, cymarose, fucose, gluconolactone, sucrose, 6-(.alpha.-D-galactosido)-D-glucose., the Sargassum disaccharide, lactitol, maltose, maltose alcohol, dextrinose, hydroxyl isomaltulose, isomaltulose, lactulose, 6-O-.alpha.-L-rhamnosyl-D-glucose., Raffinose, melezitose, and their combination.

30., according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from disintegrating agent and/or can not form the sweller of strong gel.

31. according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E3 are selected from the following additive that fusing point is not less than 25 ℃ of temperature: medicinal lipid additive, medicinal surfactant class additive, medicinal carbohydrate additive, medicinal cyclodextrin additive, amino acids additive, edible peptide class additive, medicinal salts additive, medicinal bases additive, medicinal acids additive or their combination; And/or

Described medical additive E2 is selected from the hydrophilic following additive that fusing point is not less than 25 ℃ of temperature: medicinal carbohydrate additive, medicinal cyclodextrin additive, amino acids additive, edible peptide class additive, medicinal ionic surfactant, medicinal salts additive, medicinal bases additive, medicinal acids additive or their combination; And/or

Described medical additive E4 is selected from the hydrophilic following additive that fusing point is not less than 25 ℃ of temperature: medicinal carbohydrate additive, medicinal cyclodextrin additive, amino acids additive, edible peptide class additive, the medicinal nonionic surfactant class of hydrophilic additive, medicinal ionic surfactant class additive, medicinal salts additive, medicinal bases additive, medicinal acids additive or their combination.

32. according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E3 are selected from the following medical additive that fusing point is not less than 25 ℃ of temperature: carbon number is C8 or more senior higher fatty acids glyceride, carbon number is C16 or more senior higher fatty acids propylene glycol ester, carbon number is C14 or more senior higher fatty acids glycol ester, carbon number is C16 or more senior higher fatty acids binaryglycol ester, carbon number is C10 or more senior higher fatty acids, carbon number is C12 or more senior high fatty alcohol, carbon number is that C14 or more senior higher fatty acids and carbon number are the fat that C14 or more senior high fatty alcohol form, the higher fatty acids that carbon number is C12 and carbon number are the fat that C18 or more senior high fatty alcohol form, carbon number is the fat that high fatty alcohol that C18 or more senior higher fatty acids and carbon number are C12 forms, carbon number is C31 or more senior aliphatic hydrocarbon, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include natural product and the processed goods thereof of above-mentioned lipid,

The high-grade aliphatic ester that the Polyethylene Glycol carbon number is C8～C32, the high-grade aliphatic ester that Polyethylene Glycol glycerol carbon number is C8～C32, the higher fatty acids that the carbon number of bound to polyglycerol is C8～C32, Polyethylene Glycol sterol ethers surfactant, the high-grade aliphatic ester that Polyethylene Glycol anhydrous sorbitol carbon number is C8～C32, the senior alkyl ether that the Polyethylene Glycol carbon number is C8～C32, the high-grade aliphatic ester that the glycosyl carbon number is C8～C32, the senior alkyl phenol ether that the Polyethylene Glycol carbon number is C8～C32, the high-grade aliphatic ester that tetramethylolmethane or anhydrous sorbitol carbon number are C8～C32, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, Polyethylene Glycol, polyethylene glycol oxide, polyoxy ethylene-polyoxy propylene-based block copolymer,

The carbon number of monosaccharide or its sugar alcohol, oligosaccharide or its sugar alcohol, polysaccharide or its sugar alcohol and above-mentioned sugar or its sugar alcohol is that C1～C4 alkyl ether derivative, hydroxyl carbon number are the modularization derivant that C1～C4 alkyl ether derivative, carbon number are C1～C4 alkyl derivative or above-mentioned group, the modularization derivant that cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, the derivant that methylates, sulfobutyl ether derivant or above-mentioned group

Tasteless or be the aminoacid of sweet or delicate flavour, edible 2～100 peptides,

White carbon black, silicon dioxide, titanium dioxide,

The oxide of sodium and hydroxide and pharmaceutical salts, the oxide of potassium and hydroxide and pharmaceutical salts, the oxide of calcium and hydroxide and pharmaceutical salts, the oxide of magnesium and hydroxide and pharmaceutical salts, the oxide of zinc and hydroxide and pharmaceutical salts, the oxide of ferrum and hydroxide and pharmaceutical salts, ferrous oxide and hydroxide and pharmaceutical salts, the oxide of aluminum and hydroxide and pharmaceutical salts, oxide and hydroxide and the pharmaceutical salts of gold, oxide and hydroxide and the pharmaceutical salts of silver, the oxide of lithium and hydroxide and pharmaceutical salts, the oxide of copper and hydroxide and pharmaceutical salts, cuprous oxide and hydroxide and pharmaceutical salts,

Medicinal osamine, amino acid whose carbonate, carbonate containing glycosyl, phosphoric acid, along or coelonychia base butene dioic acid, dihydroxy along or fumaric acid, maleic acid, fumaric acid, galactosaccharic acid, glucosaccharic acid, itaconic acid, malic acid, oxalic acid, malonic acid, succinic acid, citric acid, tartaric acid, citramalic acid, dihydroxytartaric acid, gluconic acid, glycolic, ethylene lactic acid, hydroxybutyric acid, the hydroxyl valeric acid, hydroxycaproic acid, the hydroxyl enanthic acid, dihydrochalcone, galacturonic acid, glucuronic acid, ascorbic acid, dehydroascorbic acid, the deoxidation ascorbic acid, glucoascorbic acid, arabo-ascorbic acid, carboxyglutamic acid, ferulic acid, phenylpropionic acid, p-hydroxybenzoic acid, phthalic acid, mandelic acid, phenylacetic acid, protocatechuic acid, gallic acid, resorcylic acid, dihydroxyphenyl acetic acid, glucoheptonic acid, taurine, glycyrrhizic acid, hydroxyglutamic acid, lactobionic acid, sorbic acid, edetic acid, pentaacetic acid, clavulanic acid, ribonucleotide, Deoxydization nucleotide, inosinic acid, Alpha-Methyl furan inosinic acid, adenylic acid, guanyl, cytidylic acid, uridylic acid, thymidylic acid, inosine monophosphate, IMP, xanthylic acid, phosphorylated amino acid, medicinal acidic polymer, medicinal alkaline polymer, polyvinyl alcohol, polyvidone, polyvinylpolypyrrolidone, celluloid, three cellulose valerates, the lacceroic acid cellulose, three Palmic acid celluloses, two Palmic acid celluloses, Merlon, poly-methyl methacrylate or second or propyl ester, ethyl acrylate-Methyl metacrylate 99 polymer, poly-(ethyl acrylate-methyl methacrylate-trimethyl amino methyl ethyl acrylate chloride), polyvinylacetate, vinyl acetate-vinyl chloride copolymer, the terpolymer of vinyl chloride-ethylene alcohol-vinylacetate, polrvinyl chloride, polyethylene, polyisobutylene, and their hydrate or their combination, and/or

Described medical additive E2 is selected from the hydrophilic following medical additive that fusing point is not less than 25 ℃ of temperature: monosaccharide or its sugar alcohol, oligosaccharide or its sugar alcohol, the methyl ether derivant of polysaccharide or its sugar alcohol and above-mentioned sugar or its sugar alcohol, the modularization derivant that the hydroxyl carbon number is C1～C4 alkyl ether derivative or above-mentioned group, cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, derivant methylates, the modularization derivant of sulfobutyl ether derivant or above-mentioned group, polyvinyl alcohol, polyvidone, tasteless or be the aminoacid of sweet or delicate flavour, edible 2～10 peptides,

The pharmaceutical salts of the pharmaceutical salts of sodium, the pharmaceutical salts of potassium, calcium, the pharmaceutical salts of magnesium,

Medicinal osamine, amino acid whose carbonate, carbonate containing glycosyl, along or coelonychia base butene dioic acid, dihydroxy along or fumaric acid, maleic acid, fumaric acid, galactosaccharic acid, glucosaccharic acid, itaconic acid, malic acid, oxalic acid, malonic acid, succinic acid, citric acid, tartaric acid, citramalic acid, dihydroxytartaric acid, gluconic acid, glycolic, ethylene lactic acid, hydroxybutyric acid, the hydroxyl valeric acid, hydroxycaproic acid, the hydroxyl enanthic acid, dihydrochalcone, galacturonic acid, glucuronic acid, ascorbic acid, dehydroascorbic acid, the deoxidation ascorbic acid, glucoascorbic acid, arabo-ascorbic acid, carboxyglutamic acid, ferulic acid, phenylpropionic acid, p-hydroxybenzoic acid, phthalic acid, mandelic acid, phenylacetic acid, protocatechuic acid, gallic acid, resorcylic acid, dihydroxyphenyl acetic acid, glucoheptonic acid, taurine, glycyrrhizic acid, hydroxyglutamic acid, lactobionic acid, sorbic acid, edetic acid, pentaacetic acid, clavulanic acid, ribonucleotide, Deoxydization nucleotide, inosinic acid, Alpha-Methyl furan inosinic acid, adenylic acid, guanyl, cytidylic acid, uridylic acid, thymidylic acid, inosine monophosphate, IMP, xanthylic acid, phosphorylated amino acid, medicinal acidic polymer, medicinal alkaline polymer, and their hydrate or their combination, and/or

Described medical additive E4 is selected from the hydrophilic following medical additive that fusing point is not less than 25 ℃ of temperature: monosaccharide or its sugar alcohol, oligosaccharide or its sugar alcohol, the methyl ether derivant of polysaccharide or its sugar alcohol and above-mentioned sugar or its sugar alcohol, the modularization derivant that the hydroxyl carbon number is C1～C4 alkyl ether derivative or above-mentioned group, cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, derivant methylates, the modularization derivant of sulfobutyl ether derivant or above-mentioned group, polyvinyl alcohol, polyvidone, tasteless or be the aminoacid of sweet or delicate flavour, edible 2～10 peptides,

The high-grade aliphatic ester that the Polyethylene Glycol carbon number is C8～C32, the high-grade aliphatic ester that Polyethylene Glycol glycerol carbon number is C8～C32, the higher fatty acids that the carbon number of bound to polyglycerol is C8～C32, Polyethylene Glycol sterol ethers surfactant, the high-grade aliphatic ester that Polyethylene Glycol anhydrous sorbitol carbon number is C8～C32, the senior alkyl ether that the Polyethylene Glycol carbon number is C8～C32, the high-grade aliphatic ester that the glycosyl carbon number is C8～C32, the senior alkyl phenol ether that the Polyethylene Glycol carbon number is C8～C32, the high-grade aliphatic ester that tetramethylolmethane or anhydrous sorbitol carbon number are C8～C32, higher fatty acids glycerol lactate, higher fatty acids propylene glycol lactate, higher fatty acids lactoyl ester, monoacylated glycerol high-grade aliphatic ester, diacetyl glycerol high-grade aliphatic ester, the polybasic carboxylic acid high-grade aliphatic ester that the glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl alcohol glycerol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl propylene glycol carbon number is C2～C6, the multi-carboxylate that senior alkyl acyl group carbon number is C2～C6, the acid of senior alkyl phosphoglyceride, the senior alkyl Phosphatidylserine, N-senior alkyl acyl group neutrality or acidic amino acid, N-senior alkyl acylsarcosine, senior alkyl acyl-peptide condensation substance, Polyethylene Glycol, polyethylene glycol oxide, polyoxy ethylene-polyoxy propylene-based block copolymer,

The pharmaceutical salts of the pharmaceutical salts of sodium, the pharmaceutical salts of potassium, calcium, the pharmaceutical salts of magnesium,

Medicinal osamine, amino acid whose carbonate, carbonate containing glycosyl, along or coelonychia base butene dioic acid, dihydroxy along or fumaric acid, maleic acid, fumaric acid, galactosaccharic acid, glucosaccharic acid, itaconic acid, malic acid, oxalic acid, malonic acid, succinic acid, citric acid, tartaric acid, citramalic acid, dihydroxytartaric acid, gluconic acid, glycolic, ethylene lactic acid, hydroxybutyric acid, the hydroxyl valeric acid, hydroxycaproic acid, the hydroxyl enanthic acid, dihydrochalcone, galacturonic acid, glucuronic acid, ascorbic acid, dehydroascorbic acid, the deoxidation ascorbic acid, glucoascorbic acid, arabo-ascorbic acid, carboxyglutamic acid, ferulic acid, phenylpropionic acid, p-hydroxybenzoic acid, phthalic acid, mandelic acid, phenylacetic acid, protocatechuic acid, gallic acid, resorcylic acid, dihydroxyphenyl acetic acid, glucoheptonic acid, taurine, glycyrrhizic acid, hydroxyglutamic acid, lactobionic acid, sorbic acid, edetic acid, pentaacetic acid, clavulanic acid, ribonucleotide, Deoxydization nucleotide, inosinic acid, Alpha-Methyl furan inosinic acid, adenylic acid, guanyl, cytidylic acid, uridylic acid, thymidylic acid, inosine monophosphate, IMP, xanthylic acid, phosphorylated amino acid, medicinal acidic polymer, medicinal alkaline polymer, and their hydrate or their combination.

33., according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E3 are selected from the following medical additive that fusing point is not less than 25 ℃ of temperature: the higher fatty acids glyceride that carbon number is C8～C32, the higher fatty acids propylene glycol ester that carbon number is C16～C32, the higher fatty acids glycol ester that carbon number is C14～C32, the higher fatty acids binaryglycol ester that carbon number is C16～C32, the higher fatty acids that carbon number is C10～C32, the high fatty alcohol that carbon number is C14～C32, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C14～C36 and carbon number are C14～C36 forms, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C12 and carbon number are C18～C36 forms, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C18～C36 and carbon number are C12 forms, the aliphatic hydrocarbon that carbon number is C31～C70, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof,

The high-grade aliphatic ester that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 2 to 200 is C8～C32, the high-grade aliphatic ester that the Polyethylene Glycol glycerol carbon number that the average polymerization number of polyethylene glycol groups is 2 to 100 is C8～C32, the higher fatty acids that the carbon number of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～20 is C8～C32, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 2 to 100, the high-grade aliphatic ester that the Polyethylene Glycol anhydrous sorbitol carbon number that the average polymerization number of polyethylene glycol groups is 2 to 100 is C8～C32, the senior alkyl ether that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 2 to 100 is C8～C32, the high-grade aliphatic ester that the glycosyl carbon number is C8～C32, the senior alkyl phenol ether that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 2 to 100 is C8～C32, the high-grade aliphatic ester that tetramethylolmethane or anhydrous sorbitol carbon number are C8～C32, the higher fatty acids glycerol lactate that carbon number is C8～C32, the higher fatty acids propylene glycol lactate that carbon number is C8～C32, the higher fatty acids lactoyl ester that carbon number is C8～C32, the high-grade aliphatic ester that list or diacetyl glycerol carbon number are C8～C32, the high-grade aliphatic ester that the polybasic carboxylic acid carbon number that the glycerol carbon number is C2～C6 is C8～C32, the multi-carboxylate that the senior alkyl alcohol glycerol carbon number that carbon number is C8～C32 is C2～C6, the multi-carboxylate that the senior alkyl acyl propylene glycol carbon number that carbon number is C8～C32 is C2～C6, the multi-carboxylate that the senior alkyl acyl group carbon number that carbon number is C8～C32 is C2～C6, the senior alkyl phosphoglyceride acid that carbon number is C8～C32, the senior alkyl Phosphatidylserine that carbon number is C8～C32, senior alkyl acyl group neutrality or acidic amino acid that the N-carbon number is C8～C32, the senior alkyl acylsarcosine that the N-carbon number is C8～C32, the senior alkyl acyl that carbon number is C8～C32-peptide condensation substance, mean molecule quantity is from 800Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 10, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 5%～95%,

Triose, tetrose, pentose, hexose, heptose, disaccharidase, trisaccharide, tetrose, pentasaccharides, six to nine sugar, the oligosaccharide that the degree of polymerization is 10～100, the sugar alcohol of above-mentioned sugar, the derivant that methylates of above-mentioned sugar and sugar alcohol thereof, the methylolation derivant, the hydroxyethylation derivant, the hydroxypropylation derivant, the modularization derivant of hydroxyl butylation derivant or above-mentioned group, cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, derivant methylates, the modularization derivant of sulfobutyl ether derivant or above-mentioned group, water solublity or hydrophilic tasteless or aminoacid that be sweet or delicate flavour, edible 2～10 peptides,

Polyvinyl alcohol, polyvidone, polyvinylpolypyrrolidone,

White carbon black, silicon dioxide, titanium dioxide,

Magnesium oxide, magnesium hydroxide, zinc oxide, zinc hydroxide, ferrum oxide, hydrated ferric oxide., ferrous oxide, ferrous hydroxide, aluminium oxide, aluminium hydroxide,

Deoxystreptamine, deoxy-glucose amine, fucosamine, galactosamine, glucamine, glucosamine, meglumine, Portugal's ethamine, neamine, trehalosamine, streptobiosamine, 4-O-(2-Amino-2-deoxy-.beta.-D-glucosyl)-D-glucosamine., oligochitosan amine, amino acid whose carbonate, containing the carbonate of glycosyl, phosphoric acid

Carbonate, basic carbonate, bicarbonate, percarbonate, sulphite, thiosulfate, phosphate, dihydric phosphate, hydrophosphate, hydrochlorate, sulfate, disulfate, nitrate, bisulfites, sulphite, pyrosulfate, pyrosulfite, silicate, trisilicate, acetate, propionate, butyrate, isobutyrate, valerate, isovalerate, valproate, caproate, dissident's hydrochlorate, positive enanthate, isoamyl acetic acid salt, acrylates, butenoate, methacrylate, pivalate, 2, 2-dihydromethyl propionic acid salt, hydroxyl acetate, hydracrylate, hydroxybutyric acid salt, hydroxypentanoic acid salt, hydroxycaproic acid salt, the hydroxyl enanthate,

Along or coelonychia base butene dioic acid and salt thereof, dihydroxy along or fumaric acid and salt thereof, maleic acid and salt thereof, fumaric acid and salt thereof, galactosaccharic acid and salt thereof, glucosaccharic acid and salt thereof, itaconic acid and salt thereof, malic acid and salt thereof, oxalic acid and salt thereof, malonic acid and salt thereof, succinic acid and salt thereof, citric acid and salt thereof, tartaric acid and salt thereof, citramalic acid and salt thereof, dihydroxytartaric acid and salt thereof, gluconic acid and salt thereof, glycolic and salt thereof, ethylene lactic acid and salt thereof, hydroxybutyric acid and salt thereof, hydroxyl valeric acid and salt thereof, hydroxycaproic acid and salt thereof, hydroxyl enanthic acid and salt thereof, dihydrochalcone and salt thereof, galacturonic acid and salt thereof, glucuronic acid and salt thereof, ascorbic acid and salt thereof, dehydroascorbic acid and salt thereof, deoxidation ascorbic acid and salt thereof, glucoascorbic acid and salt thereof, arabo-ascorbic acid and salt thereof, carboxyglutamic acid and salt thereof, ferulic acid and salt thereof, phenylpropionic acid and salt thereof, p-hydroxybenzoic acid and salt thereof, phthalic acid and salt thereof, mandelic acid and salt thereof, phenylacetic acid and salt thereof, protocatechuic acid and salt thereof, gallic acid and salt thereof, resorcylic acid and salt thereof, dihydroxyphenyl acetic acid and salt thereof, glucoheptonic acid and salt thereof, taurine and salt thereof, glycyrrhizic acid and salt thereof, hydroxyglutamic acid and salt thereof, lactobionic acid and salt thereof, sorbic acid and salt thereof, edetic acid and salt thereof, pentaacetic acid and salt thereof, clavulanic acid and salt thereof, ribonucleotide and salt thereof, Deoxydization nucleotide and salt thereof, inosinic acid and salt thereof, Alpha-Methyl furan inosinic acid and salt thereof, adenylic acid and salt thereof, guanyl and salt thereof, cytidylic acid and salt thereof, uridylic acid and salt thereof, thymidylic acid and salt thereof, inosine monophosphate, IMP and salt thereof, xanthylic acid and salt thereof, phosphorylated amino acid and salt thereof, benzoate, the caffeiate, methyl salicylate, Salicylate, acetylsalicylate, nicotinate, .gamma.-pyridinecarboxylic acid salt, creatine salt, saccharin salt, tasteless or be the acidity of sweet or delicate flavour or the pharmaceutical salts of basic amino acid, the salt of edible acidity 2～10 peptides and alkalescence 2～10 peptides, medicinal acidic polymer and salt thereof, medicinal alkaline polymer and salt thereof, and their hydrate or their combination, wherein, above-mentioned salt is selected from sodium salt, potassium salt, calcium salt, magnesium salt, zinc salt, iron salt, ferrous salt, aluminum salt and golden salt, above-mentioned medicinal acidic polymer is selected from carboxyl alkyl cellulose, cellulose derivative with monoester bond of binary acid, polyvinyl derivant with dibasic acid monoester key, its polymers of maleic acid-ethylene, acrylic polymer or their combination in any, above-mentioned medicinal alkaline polymer is selected from the cellulose derivative with list or disubstituted amido, polythene derivative with list or disubstituted amido, acrylate copolymer with mono-substituted amino, chitosan or their combination in any, and/or

Described medical additive E2 is selected from the hydrophilic following medical additive that fusing point is not less than 25 ℃ of temperature: triose, tetrose, pentose, hexose, heptose, disaccharidase, trisaccharide, tetrose, pentasaccharides, six to nine sugar, the oligosaccharide that the degree of polymerization is 10～100, the sugar alcohol of above-mentioned sugar, the derivant that methylates of above-mentioned sugar and sugar alcohol thereof, the methylolation derivant, the hydroxyethylation derivant, the hydroxypropylation derivant, the modularization derivant of hydroxyl butylation derivant or above-mentioned group, cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, derivant methylates, the modularization derivant of sulfobutyl ether derivant or above-mentioned group, tasteless or be the aminoacid of sweet or delicate flavour, edible 2～10 peptides,

Polyvinyl alcohol, polyvidone, magnesium hydroxide, zinc hydroxide, hydrated ferric oxide., ferrous oxide, ferrous hydroxide, aluminium hydroxide,

Deoxystreptamine, deoxy-glucose amine, fucosamine, galactosamine, glucamine, glucosamine, meglumine, Portugal's ethamine, neamine, trehalosamine, streptobiosamine, 4-O-(2-Amino-2-deoxy-.beta.-D-glucosyl)-D-glucosamine., oligochitosan amine, amino acid whose carbonate, carbonate containing glycosyl, carbonate, basic carbonate, bicarbonate, percarbonate, sulphite, thiosulfate, phosphate, dihydric phosphate, hydrophosphate, hydrochlorate, sulfate, disulfate, nitrate, bisulfites, sulphite, pyrosulfate, pyrosulfite, silicate, trisilicate, acetate, propionate, butyrate, isobutyrate, valerate, isovalerate, valproate, caproate, dissident's hydrochlorate, positive enanthate, isoamyl acetic acid salt, acrylates, butenoate, methacrylate, pivalate, 2, 2-dihydromethyl propionic acid salt, hydroxyl acetate, hydracrylate, hydroxybutyric acid salt, hydroxypentanoic acid salt, hydroxycaproic acid salt, the hydroxyl enanthate,

Along or coelonychia base butene dioic acid and salt thereof, dihydroxy along or fumaric acid and salt thereof, maleic acid and salt thereof, fumaric acid and salt thereof, galactosaccharic acid and salt thereof, glucosaccharic acid and salt thereof, itaconic acid and salt thereof, malic acid and salt thereof, oxalic acid and salt thereof, malonic acid and salt thereof, succinic acid and salt thereof, citric acid and salt thereof, tartaric acid and salt thereof, citramalic acid and salt thereof, dihydroxytartaric acid and salt thereof, gluconic acid and salt thereof, glycolic and salt thereof, ethylene lactic acid and salt thereof, hydroxybutyric acid and salt thereof, hydroxyl valeric acid and salt thereof, hydroxycaproic acid and salt thereof, hydroxyl enanthic acid and salt thereof, dihydrochalcone and salt thereof, galacturonic acid and salt thereof, glucuronic acid and salt thereof, ascorbic acid and salt thereof, dehydroascorbic acid and salt thereof, deoxidation ascorbic acid and salt thereof, glucoascorbic acid and salt thereof, arabo-ascorbic acid and salt thereof, carboxyglutamic acid and salt thereof, ferulic acid and salt thereof, phenylpropionic acid and salt thereof, p-hydroxybenzoic acid and salt thereof, phthalic acid and salt thereof, mandelic acid and salt thereof, phenylacetic acid and salt thereof, protocatechuic acid and salt thereof, gallic acid and salt thereof, resorcylic acid and salt thereof, dihydroxyphenyl acetic acid and salt thereof, glucoheptonic acid and salt thereof, taurine and salt thereof, glycyrrhizic acid and salt thereof, hydroxyglutamic acid and salt thereof, lactobionic acid and salt thereof, sorbic acid and salt thereof, edetic acid and salt thereof, pentaacetic acid and salt thereof, clavulanic acid and salt thereof, ribonucleotide and salt thereof, Deoxydization nucleotide and salt thereof, inosinic acid and salt thereof, Alpha-Methyl furan inosinic acid and salt thereof, adenylic acid and salt thereof, guanyl and salt thereof, cytidylic acid and salt thereof, uridylic acid and salt thereof, thymidylic acid and salt thereof, inosine monophosphate, IMP and salt thereof, xanthylic acid and salt thereof, phosphorylated amino acid and salt thereof, benzoate, the caffeiate, methyl salicylate, Salicylate, acetylsalicylate, nicotinate, .gamma.-pyridinecarboxylic acid salt, creatine salt, saccharin salt, tasteless or be the acidity of sweet or delicate flavour or the pharmaceutical salts of basic amino acid, the salt of edible acidity 2～10 peptides and alkalescence 2～10 peptides, medicinal acidic polymer salt, medicinal alkaline polymer salt, and their hydrate or their combination, above-mentioned salt is selected from sodium salt, potassium salt, and/or

Described medical additive E4 is selected from the hydrophilic following medical additive that fusing point is not less than 25 ℃ of temperature: triose, tetrose, pentose, hexose, heptose, disaccharidase, trisaccharide, tetrose, pentasaccharides, six to nine sugar, the oligosaccharide that the degree of polymerization is 10～100, the sugar alcohol of above-mentioned sugar, the derivant that methylates of above-mentioned sugar and sugar alcohol thereof, the methylolation derivant, the hydroxyethylation derivant, the hydroxypropylation derivant, the modularization derivant of hydroxyl butylation derivant or above-mentioned group, cyclodextrin and hydroxyl carbon number thereof are C1～C4 alkyl derivative, monosaccharide groups or oligosaccharyl derivant, derivant methylates, the modularization derivant of sulfobutyl ether derivant or above-mentioned group, tasteless or be the aminoacid of sweet or delicate flavour, edible 2～10 peptides,

Polyvinyl alcohol, polyvidone, magnesium hydroxide, zinc hydroxide, hydrated ferric oxide., ferrous oxide, ferrous hydroxide, aluminium hydroxide,

The high-grade aliphatic ester that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 8 to 200 is C8～C32, the high-grade aliphatic ester that the Polyethylene Glycol glycerol carbon number that the average polymerization number of polyethylene glycol groups is 8 to 100 is C8～C32, the higher fatty acids that the carbon number of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～20 is C8～C32, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 8 to 100, the high-grade aliphatic ester that the Polyethylene Glycol anhydrous sorbitol carbon number that the average polymerization number of polyethylene glycol groups is 4 to 100 is C8～C32, the senior alkyl ether that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 8 to 100 is C8～C32, the high-grade aliphatic ester that the glycosyl carbon number is C8～C32, the high-grade aliphatic ester that tetramethylolmethane or anhydrous sorbitol carbon number are C8～C32, the high-grade aliphatic ester that the polybasic carboxylic acid carbon number that the glycerol carbon number is C2～C6 is C8～C32, the multi-carboxylate that the senior alkyl alcohol glycerol carbon number that carbon number is C8～C32 is C2～C6, mean molecule quantity is from 800Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20, 000Da to 10, 000, the polyethylene glycol oxide of 000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 5%～95%,

Deoxystreptamine, deoxy-glucose amine, fucosamine, galactosamine, glucamine, glucosamine, meglumine, Portugal's ethamine, neamine, trehalosamine, streptobiosamine, 4-O-(2-Amino-2-deoxy-.beta.-D-glucosyl)-D-glucosamine., oligochitosan amine, amino acid whose carbonate, carbonate containing glycosyl, carbonate, basic carbonate, bicarbonate, percarbonate, sulphite, thiosulfate, phosphate, dihydric phosphate, hydrophosphate, hydrochlorate, sulfate, disulfate, nitrate, bisulfites, sulphite, pyrosulfate, pyrosulfite, silicate, trisilicate, acetate, propionate, butyrate, isobutyrate, valerate, isovalerate, valproate, caproate, dissident's hydrochlorate, positive enanthate, isoamyl acetic acid salt, acrylates, butenoate, methacrylate, pivalate, 2, 2-dihydromethyl propionic acid salt, hydroxyl acetate, hydracrylate, hydroxybutyric acid salt, hydroxypentanoic acid salt, hydroxycaproic acid salt, the hydroxyl enanthate,

Along or coelonychia base butene dioic acid and salt thereof, dihydroxy along or fumaric acid and salt thereof, maleic acid and salt thereof, fumaric acid and salt thereof, galactosaccharic acid and salt thereof, glucosaccharic acid and salt thereof, itaconic acid and salt thereof, malic acid and salt thereof, oxalic acid and salt thereof, malonic acid and salt thereof, succinic acid and salt thereof, citric acid and salt thereof, tartaric acid and salt thereof, citramalic acid and salt thereof, dihydroxytartaric acid and salt thereof, gluconic acid and salt thereof, glycolic and salt thereof, ethylene lactic acid and salt thereof, hydroxybutyric acid and salt thereof, hydroxyl valeric acid and salt thereof, hydroxycaproic acid and salt thereof, hydroxyl enanthic acid and salt thereof, dihydrochalcone and salt thereof, galacturonic acid and salt thereof, glucuronic acid and salt thereof, ascorbic acid and salt thereof, dehydroascorbic acid and salt thereof, deoxidation ascorbic acid and salt thereof, glucoascorbic acid and salt thereof, arabo-ascorbic acid and salt thereof, carboxyglutamic acid and salt thereof, ferulic acid and salt thereof, phenylpropionic acid and salt thereof, p-hydroxybenzoic acid and salt thereof, phthalic acid and salt thereof, mandelic acid and salt thereof, phenylacetic acid and salt thereof, protocatechuic acid and salt thereof, gallic acid and salt thereof, resorcylic acid and salt thereof, dihydroxyphenyl acetic acid and salt thereof, glucoheptonic acid and salt thereof, taurine and salt thereof, glycyrrhizic acid and salt thereof, hydroxyglutamic acid and salt thereof, lactobionic acid and salt thereof, sorbic acid and salt thereof, edetic acid and salt thereof, pentaacetic acid and salt thereof, clavulanic acid and salt thereof, ribonucleotide and salt thereof, Deoxydization nucleotide and salt thereof, inosinic acid and salt thereof, Alpha-Methyl furan inosinic acid and salt thereof, adenylic acid and salt thereof, guanyl and salt thereof, cytidylic acid and salt thereof, uridylic acid and salt thereof, thymidylic acid and salt thereof, inosine monophosphate, IMP and salt thereof, xanthylic acid and salt thereof, phosphorylated amino acid and salt thereof, benzoate, the caffeiate, methyl salicylate, Salicylate, acetylsalicylate, nicotinate, .gamma.-pyridinecarboxylic acid salt, creatine salt, saccharin salt, tasteless or be the acidity of sweet or delicate flavour or the pharmaceutical salts of basic amino acid, the salt of edible acidity 2～10 peptides and alkalescence 2～10 peptides, medicinal acidic polymer salt, medicinal alkaline polymer salt, and their hydrate or their combination, above-mentioned salt is selected from sodium salt, potassium salt.

34. the tablet according to claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E3 are selected from the following medical additive that fusing point is not less than 25 ℃ of temperature: the higher fatty acids glyceride that carbon number is C8～C22, the higher fatty acids propylene glycol ester that carbon number is C16～C22, the higher fatty acids glycol ester that carbon number is C14～C22, the higher fatty acids binaryglycol ester that carbon number is C16～C22, the higher fatty acids that carbon number is C10～C22, the high fatty alcohol that carbon number is C14～C22, the fat that the high fatty alcohol that the higher fatty acids that carbon number is C16～C36 and carbon number are C16～C36 forms, the aliphatic hydrocarbon that carbon number is C41～C70, terpene resin, p-Hydroxybenzoate, epicatechol gallate, acid ascorbyl ester, the arabo-ascorbic acid ester, benzyl p-hydroxybenzoate and include their natural product and processed goods thereof,

The high-grade aliphatic ester that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 4 to 150 is C8～C22, the high-grade aliphatic ester that the Polyethylene Glycol glycerol carbon number that the average polymerization number of polyethylene glycol groups is 10 to 60 is C8～C22, the higher fatty acids that the carbon number of the bound to polyglycerol that the degree of polymerization of polyglyceryl is 2～10 is C8～C22, the Polyethylene Glycol sterol ethers surfactant that the average polymerization number of polyethylene glycol groups is 4 to 50, the high-grade aliphatic ester that the Polyethylene Glycol anhydrous sorbitol carbon number that the average polymerization number of polyethylene glycol groups is 4 to 60 is C8～C22, the senior alkyl ether that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 4 to 60 is C8～C22, the high-grade aliphatic ester that the glycosyl carbon number is C8～C22, the senior alkyl phenol ether that the Polyethylene Glycol carbon number that the average polymerization number of polyethylene glycol groups is 10 to 100 is C8～C22, the high-grade aliphatic ester that tetramethylolmethane or anhydrous sorbitol carbon number are C8～C22, the higher fatty acids glycerol lactate that carbon number is C8～C22, the higher fatty acids propylene glycol lactate that carbon number is C8～C22, the higher fatty acids lactoyl ester that carbon number is C8～C22, the high-grade aliphatic ester that list or diacetyl glycerol carbon number are C8～C22, the high-grade aliphatic ester that the polybasic carboxylic acid carbon number that the glycerol carbon number is C2～C6 is C8～C22, the multi-carboxylate that the senior alkyl alcohol glycerol carbon number that carbon number is C8～C22 is C2～C6, the multi-carboxylate that the senior alkyl acyl propylene glycol carbon number that carbon number is C8～C22 is C2～C6, the multi-carboxylate that the senior alkyl acyl group carbon number that carbon number is C8～C22 is C2～C6, the senior alkyl phosphoglyceride acid that carbon number is C8～C22, the senior alkyl Phosphatidylserine that carbon number is C8～C22, senior alkyl acyl group neutrality or acidic amino acid that the N-carbon number is C8～C22, the senior alkyl acylsarcosine that the N-carbon number is C8～C22, the senior alkyl acyl that carbon number is C8～C22-peptide condensation substance, mean molecule quantity is from 1000Da to 20, the Polyethylene Glycol of 000Da, mean molecule quantity is from 20,000Da to 4, the polyethylene glycol oxide of 000,000Da, mean molecule quantity is 5000～20000 and the mass ratio that accounts in molecule of the oxyethylene group polyoxy ethylene-polyoxy propylene-based block copolymer that is 20%～90%,

Glyceraldehyde, dihydroxy acetone, erythritol, ribose, ribitol, deoxyribose, xylose, xylitol, arabinose, 1,2,3,4,5-pentanepentol, glucose, galactose, galactitol, mannitol, mannose, inosite, rhamnose, altrose, allose, fructose, sorbose, sorbitol, Tagatose, lyxose, mannoheptulose, Perseitol, sedoheptulose, sedoheptose alcohol, chalcose, Quinovose, cymarose, fucose, gluconolactone, lactose, lactose, sucrose, cellobiose, 6-(.alpha.-D-galactosido)-D-glucose., the Sargassum disaccharide, lactitol, maltose, maltose alcohol, dextrinose, hydroxyl isomaltulose, isomaltulose, lactulose, 6-O-.alpha.-L-rhamnosyl-D-glucose., vicianose, Raffinose, cellotriose, melezitose, stachyose, cellotetrose, verbascose, Fructus Hordei Germinatus three is to pentasaccharides, cellopentaose, Fructus Hordei Germinatus six to nine sugar, fiber six to nine sugar, dextrates, the Polyfructose. of the degree of polymerization 2～100, the IMO of the degree of polymerization 2～100, the IMO alcohol of the degree of polymerization 2～100, dextrin, glucosan, pulullan polysaccharide, Tragacanth, starch, pregelatinized Starch, modified starch, microcrystalline Cellulose, silicified microcrystalline cellulose, the micropowder cellulose, cellulose acetate, hydroxyl second methylcellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, methyl-α-/or β-/or gamma-cyclodextrin, hydroxypropyl-α-/or β-/or gamma-cyclodextrin, hydroxyl butyl-α-/or β-/or gamma-cyclodextrin, hydroxyethyl-α-/or β-/or gamma-cyclodextrin, hydroxyl cyclobutenyl-α-/or β-/or gamma-cyclodextrin, glucosyl group-α-/or β-/or gamma-cyclodextrin, malt-base-α-/or β-/or gamma-cyclodextrin, galactosyl-α-/or β-/or gamma-cyclodextrin, Pyrusussuriensis glycosyl-α-/or β-/or gamma-cyclodextrin, mannose group-α-/or β-/or gamma-cyclodextrin, malt-base-α-/or β-/or gamma-cyclodextrin base-glucose, widow or polysaccharide side chain-α-/or β-/or gamma-cyclodextrin, sulfobutyl ether-α-/or β-/or gamma-cyclodextrin and pharmaceutical salts thereof,

L and/or D-cystine, D-Tyrosine, aspartic acid and pharmaceutical salts thereof, glutamic acid and pharmaceutical salts thereof, D-trp, L and/or D-Thr, D-Leu, D-phenylalanine, the D-methionine, D-Ile, L and/or D-His, L and/or D-Ser, D-Val, L and/or D-alanine, glycine, L and/or D-hydroxyproline, L and/or D-PROLINE, D-Lys and pharmaceutical salts thereof, D-Arg and pharmaceutical salts thereof, L and/or D-Gln, D-Asn, comprise L and/or D-Thr, L and/or D-alanine, glycine, L and/or D-hydroxyproline, L and/or D-PROLINE, L and/or D-Lys and pharmaceutical salts thereof, the dipeptides of L and/or D-Arg and pharmaceutical salts thereof or tripeptides, derive from the legume seed-protein, seeds of gramineous crops protein, amaranth seed protein, Sargassum protein matter, Radix hemerocalis plicatae protein, tuber crops tuber or rhizome protein, livestock products protein, the fowl white matter of laying eggs, aquatic product protein matter, the edible peptide of fibroin,

Polyvinyl alcohol, polyvidone, polyvinylpolypyrrolidone, celluloid, three cellulose valerates, the lacceroic acid cellulose, three Palmic acid celluloses, two Palmic acid celluloses, Merlon, poly-methyl methacrylate or second or propyl ester, ethyl acrylate-Methyl metacrylate 99 polymer, poly-(ethyl acrylate-methyl methacrylate-trimethyl amino methyl ethyl acrylate chloride), polyvinylacetate, vinyl acetate-vinyl chloride copolymer, the terpolymer of vinyl chloride-ethylene alcohol-vinylacetate, polrvinyl chloride, polyethylene, polyisobutylene, dimethicone,

White carbon black, silicon dioxide, titanium dioxide,

Magnesium oxide, magnesium hydroxide, zinc oxide, zinc hydroxide, ferrum oxide, hydrated ferric oxide., ferrous oxide, ferrous hydroxide, aluminium oxide, aluminium hydroxide,

Deoxystreptamine, deoxy-glucose amine, fucosamine, galactosamine, glucamine, glucosamine, meglumine, Portugal's ethamine, neamine, trehalosamine, streptobiosamine, 4-O-(2-Amino-2-deoxy-.beta.-D-glucosyl)-D-glucosamine., oligochitosan amine, amino acid whose carbonate, containing the carbonate of glycosyl, phosphoric acid

Carbonate, basic carbonate, bicarbonate, percarbonate, sulphite, thiosulfate, phosphate, dihydric phosphate, hydrophosphate, hydrochlorate, sulfate, disulfate, nitrate, bisulfites, sulphite, pyrosulfate, pyrosulfite, silicate, trisilicate, acetate, propionate, butyrate, isobutyrate, valerate, isovalerate, valproate, caproate, dissident's hydrochlorate, positive enanthate, isoamyl acetic acid salt, acrylates, butenoate, methacrylate, pivalate, 2, 2-dihydromethyl propionic acid salt, hydroxyl acetate, hydracrylate, hydroxybutyric acid salt, hydroxypentanoic acid salt, hydroxycaproic acid salt, the hydroxyl enanthate,

Along or coelonychia base butene dioic acid and salt thereof, dihydroxy along or fumaric acid and salt thereof, maleic acid and salt thereof, fumaric acid and salt thereof, galactosaccharic acid and salt thereof, glucosaccharic acid and salt thereof, itaconic acid and salt thereof, malic acid and salt thereof, oxalic acid and salt thereof, malonic acid and salt thereof, succinic acid and salt thereof, citric acid and salt thereof, tartaric acid and salt thereof, citramalic acid and salt thereof, dihydroxytartaric acid and salt thereof, gluconic acid and salt thereof, glycolic and salt thereof, ethylene lactic acid and salt thereof, hydroxybutyric acid and salt thereof, hydroxyl valeric acid and salt thereof, hydroxycaproic acid and salt thereof, hydroxyl enanthic acid and salt thereof, dihydrochalcone and salt thereof, galacturonic acid and salt thereof, glucuronic acid and salt thereof, ascorbic acid and salt thereof, dehydroascorbic acid and salt thereof, deoxidation ascorbic acid and salt thereof, glucoascorbic acid and salt thereof, arabo-ascorbic acid and salt thereof, carboxyglutamic acid and salt thereof, ferulic acid and salt thereof, phenylpropionic acid and salt thereof, p-hydroxybenzoic acid and salt thereof, phthalic acid and salt thereof, mandelic acid and salt thereof, phenylacetic acid and salt thereof, protocatechuic acid and salt thereof, gallic acid and salt thereof, resorcylic acid and salt thereof, dihydroxyphenyl acetic acid and salt thereof, glucoheptonic acid and salt thereof, taurine and salt thereof, glycyrrhizic acid and salt thereof, hydroxyglutamic acid and salt thereof, lactobionic acid and salt thereof, sorbic acid and salt thereof, edetic acid and salt thereof, pentaacetic acid and salt thereof, clavulanic acid and salt thereof, ribonucleotide and salt thereof, Deoxydization nucleotide and salt thereof, inosinic acid and salt thereof, Alpha-Methyl furan inosinic acid and salt thereof, adenylic acid and salt thereof, guanyl and salt thereof, cytidylic acid and salt thereof, uridylic acid and salt thereof, thymidylic acid and salt thereof, inosine monophosphate, IMP and salt thereof, xanthylic acid and salt thereof, phosphorylated amino acid and salt thereof, benzoate, the caffeiate, methyl salicylate, Salicylate, acetylsalicylate, nicotinate, .gamma.-pyridinecarboxylic acid salt, creatine salt, saccharin salt, the salt of edible acidity 2～10 peptides and alkalescence 2～10 peptides, medicinal acidic polymer and salt thereof, medicinal alkaline polymer and salt thereof, and their hydrate or their combination, wherein, above-mentioned medicinal acidic polymer is selected from carboxymethyl cellulose, carboxymethylethylcellulose, the phthalic acid ester acid cellulose, the succinic acid acetyl cellulose, O-phthalic acid methyl cellulose ester, phthalic acid hydroxymethyl ethyl cellulose esters, phthalic acid hydroxypropyl emthylcellulose ester, succinic acid hydroxypropyl emthylcellulose ester, the dibasic acid monoester of polyvinyl, the phthalic acid polyvinyl alcohol ester, phthalic acid polyethylene butyl ester, acetyl group acetal phthalic acid polyvinyl ester, Vinyl acetate-maleic anhydride copolymer, butyl vinyl ether-copolymer-maleic anhydride, the styrene-maleic acid monoester copolymer, acrylic acid methyl ester .-methacrylic acid copolymer, the styrene-propene acid copolymer, acrylic acid methyl ester .-methacrylic acid-1-Octyl acrylate copolymer, the polymer that structural formula and Eudragit L or Eudragit S or Eudragit FS are identical, alginic acid, Lac or their combination in any, above-mentioned medicinal alkaline polymer is selected from the benzylamino-methyl cellulose, diethylamino methyl cellulose, the piperidyl ethylhydroxyethylcellulose, cellulose acetate diethylamino acetate, vinyl diethylamide-vinyl acetate co-polymer, ethylene benzyl amine-vinyl acetate co-polymer, poly-acetal acetic acid diethylamino vinyl acetate, ethylene piperidyl-acetyl acetal ethylene copolymer, poly-diethylamino methyl styrene, methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymer, the polymethylacrylic acid dimethylamino ethyl ester, chitosan or their combination in any, above-mentioned salt is selected from sodium salt, potassium salt, calcium salt, magnesium salt, and/or

Described medical additive E2 and/or medical additive E4 are selected from the hydrophilic following medical additive that fusing point is not less than 25 ℃ of temperature: glyceraldehyde, dihydroxy acetone, erythritol, ribose, ribitol, deoxyribose, xylose, xylitol, arabinose, 1,2,3,4,5-pentanepentol, glucose, galactose, galactitol, mannitol, mannose, inosite, rhamnose, altrose, allose, fructose, sorbose, sorbitol, Tagatose, lyxose, mannoheptulose, Perseitol, sedoheptulose, sedoheptose alcohol, chalcose, Quinovose, cymarose, fucose, gluconolactone, lactose, lactose, sucrose, cellobiose, 6-(.alpha.-D-galactosido)-D-glucose., the Sargassum disaccharide, lactitol, maltose, maltose alcohol, dextrinose, hydroxyl isomaltulose, isomaltulose, lactulose, 6-O-.alpha.-L-rhamnosyl-D-glucose., vicianose, Raffinose, cellotriose, melezitose, stachyose, cellotetrose, verbascose, Fructus Hordei Germinatus three is to pentasaccharides, cellopentaose, Fructus Hordei Germinatus six to nine sugar, fiber six to nine sugar, dextrates, the Polyfructose. of the degree of polymerization 2～100, the IMO of the degree of polymerization 2～100, the IMO alcohol of the degree of polymerization 2～100, dextrin, glucosan, pulullan polysaccharide, Tragacanth, amylose, pregelatinized Starch, modified starch, hydroxyl second methylcellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, methyl-α-/or β-/or gamma-cyclodextrin, hydroxypropyl-α-/or β-/or gamma-cyclodextrin, hydroxyl butyl-α-/or β-/or gamma-cyclodextrin, hydroxyethyl-α-/or β-/or gamma-cyclodextrin, hydroxyl cyclobutenyl-α-/or β-/or gamma-cyclodextrin, glucosyl group-α-/or β-/or gamma-cyclodextrin, malt-base-α-/or β-/or gamma-cyclodextrin, galactosyl-α-/or β-/or gamma-cyclodextrin, Pyrusussuriensis glycosyl-α-/or β-/or gamma-cyclodextrin, mannose group-α-/or β-/or gamma-cyclodextrin, malt-base-α-/or β-/or gamma-cyclodextrin base-glucose, widow or polysaccharide side chain-α-/or β-/or gamma-cyclodextrin, sulfobutyl ether-α-/or β-/or gamma-cyclodextrin and pharmaceutical salts thereof,

Aspartic acid and pharmaceutical salts thereof, glutamic acid and pharmaceutical salts thereof, D-trp, L and/or D-Thr, D-Leu, D-phenylalanine, D-methionine, D-Ile, L and/or D-His, L and/or D-Ser, D-Val, L and/or D-alanine, glycine, L and/or D-hydroxyproline, L and/or D-PROLINE, D-Lys and pharmaceutical salts thereof, D-Arg and pharmaceutical salts thereof, L and/or D-Gln, D-Asn

The dipeptides or the tripeptides that comprise L and/or D-Thr, L and/or D-alanine, glycine, L and/or D-hydroxyproline, L and/or D-PROLINE, L and/or D-Lys and pharmaceutical salts, L and/or D-Arg and pharmaceutical salts thereof,

Derive from the lay eggs edible peptide of white matter, aquatic product protein matter, fibroin of legume seed-protein, seeds of gramineous crops protein, amaranth seed protein, Sargassum protein matter, Radix hemerocalis plicatae protein, tuber crops tuber or rhizome protein, livestock products protein, fowl, polyvinyl alcohol, polyvidone

Magnesium hydroxide, zinc hydroxide, hydrated ferric oxide., ferrous oxide, ferrous hydroxide, aluminium hydroxide,

Deoxystreptamine, deoxy-glucose amine, fucosamine, galactosamine, glucamine, glucosamine, meglumine, Portugal's ethamine, neamine, trehalosamine, streptobiosamine, 4-O-(2-Amino-2-deoxy-.beta.-D-glucosyl)-D-glucosamine., oligochitosan amine, amino acid whose carbonate, carbonate containing glycosyl

Carbonate, basic carbonate, bicarbonate, percarbonate, sulphite, thiosulfate, phosphate, dihydric phosphate, hydrophosphate, hydrochlorate, sulfate, disulfate, nitrate, bisulfites, sulphite, pyrosulfate, pyrosulfite, silicate, trisilicate, acetate, propionate, butyrate, isobutyrate, valerate, isovalerate, valproate, caproate, dissident's hydrochlorate, positive enanthate, isoamyl acetic acid salt, acrylates, butenoate, methacrylate, pivalate, 2, 2-dihydromethyl propionic acid salt, hydroxyl acetate, hydracrylate, hydroxybutyric acid salt, hydroxypentanoic acid salt, hydroxycaproic acid salt, the hydroxyl enanthate,

Along or coelonychia base butene dioic acid and salt thereof, dihydroxy along or fumaric acid and salt thereof, maleic acid and salt thereof, fumaric acid and salt thereof, galactosaccharic acid and salt thereof, glucosaccharic acid and salt thereof, itaconic acid and salt thereof, malic acid and salt thereof, oxalic acid and salt thereof, malonic acid and salt thereof, succinic acid and salt thereof, citric acid and salt thereof, tartaric acid and salt thereof, citramalic acid and salt thereof, dihydroxytartaric acid and salt thereof, gluconic acid and salt thereof, glycolic and salt thereof, ethylene lactic acid and salt thereof, hydroxybutyric acid and salt thereof, hydroxyl valeric acid and salt thereof, hydroxycaproic acid and salt thereof, hydroxyl enanthic acid and salt thereof, dihydrochalcone and salt thereof, galacturonic acid and salt thereof, glucuronic acid and salt thereof, ascorbic acid and salt thereof, dehydroascorbic acid and salt thereof, deoxidation ascorbic acid and salt thereof, glucoascorbic acid and salt thereof, arabo-ascorbic acid and salt thereof, carboxyglutamic acid and salt thereof, ferulic acid and salt thereof, phenylpropionic acid and salt thereof, p-hydroxybenzoic acid and salt thereof, phthalic acid and salt thereof, mandelic acid and salt thereof, phenylacetic acid and salt thereof, protocatechuic acid and salt thereof, gallic acid and salt thereof, resorcylic acid and salt thereof, dihydroxyphenyl acetic acid and salt thereof, glucoheptonic acid and salt thereof, taurine and salt thereof, glycyrrhizic acid and salt thereof, hydroxyglutamic acid and salt thereof, lactobionic acid and salt thereof, sorbic acid and salt thereof, edetic acid and salt thereof, pentaacetic acid and salt thereof, clavulanic acid and salt thereof, ribonucleotide and salt thereof, Deoxydization nucleotide and salt thereof, inosinic acid and salt thereof, Alpha-Methyl furan inosinic acid and salt thereof, adenylic acid and salt thereof, guanyl and salt thereof, cytidylic acid and salt thereof, uridylic acid and salt thereof, thymidylic acid and salt thereof, inosine monophosphate, IMP and salt thereof, xanthylic acid and salt thereof, phosphorylated amino acid and salt thereof, benzoate, the caffeiate, methyl salicylate, Salicylate, acetylsalicylate, nicotinate, .gamma.-pyridinecarboxylic acid salt, creatine salt, saccharin salt, the salt of edible acidity 2～10 peptides and alkalescence 2～10 peptides, and their hydrate or their combination, wherein, above-mentioned salt is selected from sodium salt, potassium salt.

35. the tablet according to any one in claim 24 to 26 or 32 to 34, it is characterized in that described higher fatty acids is the hydroxylating higher fatty acids, and/or described high fatty alcohol is the hydroxylating high fatty alcohol, and/or described senior alkyl is the hydroxylating senior alkyl.

36., according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from senior alkyl three ammonium halogenide, senior alkyl trimethyl ammonium halogenide, senior alkyl trimethyl ammonium halogenide, senior alkyl ammonium halogenide, senior alkyl benzyl dimethyl ammonium medicinal salts, diisobutyl phenoxy group ethyoxyl dimethyl benzyl ammonium medicinal salts, senior alkyl pyridine medicinal salts, the betanin that comprises senior alkyl in molecular structure, in molecular structure, comprise senior alkyl by the amine of ethoxyquin, N-senior alkyl acylamino acid pharmaceutical salts, N-senior alkyl acylsarcosine pharmaceutical salts, the alkane esters pharmaceutical salts that the senior alkane acyl of N-basic amino acid carbon number is C1-C6, N-senior alkyl Gemini class basic amino acid pharmaceutical salts surfactant, the alkyl acyl that the N-carbon number is C1-C12-basic amino acid senior alkyl glyceride medicinal salts surfactant, senior alkyl 2-Sulfosuccinic acid pharmaceutical salts, senior alkyl ether-2 2-Sulfosuccinic acid pharmaceutical salts, the alkane sulfonic acid pharmaceutical salts that senior alkyl acyl methylamine carbon number is C1～C6, senior alkyl sulphuric acid pharmaceutical salts, senior alkyl carboxylic acid pharmaceutical salts, senior alkyl taurine pharmaceutical salts, senior alkyl ether sulphuric acid pharmaceutical salts, senior alkyl glyceryl ether sulfonic acid pharmaceutical salts esters, senior alkyl fatty alcohol-polyoxyethylene ether sulphuric acid pharmaceutical salts, the medicinal alkali of sulfonic acid is for succinic acid two higher alkyl esters, multi-carboxylate's pharmaceutical salts that senior alkyl acyl glycerol carbon number is C2～C6, multi-carboxylate's pharmaceutical salts that senior alkyl acyl propylene glycol carbon number is C2～C6, multi-carboxylate's pharmaceutical salts that senior alkyl acyl group carbon number is C2～C6, senior alkyl acyl group lactic acid pharmaceutical salts, cholic acid medicinal salts surfactant, the caseinic acid pharmaceutical salts, alginic acid pharmaceutical salts, and their mixture, wherein, the saturated or unsaturated alkyl that described senior alkyl is carbon number C8-C32 or its hydroxylating alkyl.

37., according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from dioctyl 2-Sulfosuccinic acid pharmaceutical salts, octyl group 2-Sulfosuccinic acid pharmaceutical salts, the lauryl sulphate acid pharmaceutical salts, myristyl sulphuric acid pharmaceutical salts, ten to the octadecanoid acid pharmaceutical salts, the castor oil acid pharmaceutical salts, ten acid of acetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, ten acid of acetyl tartaric acid pharmaceutical salts diglycerol are to the behenic acid ester, ten acid of diacetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, ten acid of diacetyl tartaric acid pharmaceutical salts diglycerol are to the behenic acid ester, ten acid of oxalyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of oxalyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, mix acetic acid pharmaceutical salts and ten acid of tartaric acid pharmaceutical salts glycerol list to the behenic acid ester, mix acetic acid pharmaceutical salts and ten acid of tartaric acid pharmaceutical salts diglycerol to the behenic acid ester, ten acid of citric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of citric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of succinic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of succinic acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of lactic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of lactic acid pharmaceutical salts glycerol are to the behenic acid ester, ten to tadenan citric acid pharmaceutical salts glyceryl monoacetate, ten acid are to behenic acid acyl citric acid pharmaceutical salts ester, tartaric acid pharmaceutical salts Dan Shizhi docosane acyl ester, ten to docosane acyl butene dioic acid pharmaceutical salts, ten to docosane acyl propylene glycol succinate pharmaceutical salts,

Decoyl lactic acid pharmaceutical salts, caprinoyl lactic acid pharmaceutical salts, lauroyl lactic acid pharmaceutical salts, tetradecylic acid lactic acid pharmaceutical salts, hexadecylic acid lactic acid pharmaceutical salts, stearoyl lactic acid pharmaceutical salts, isostearoyl lactic acid pharmaceutical salts, oleoyl lactic acid pharmaceutical salts, cocos nucifera oil acyl lactic acid pharmaceutical salts, 12-hydroxyl stearoyl lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, Semen Ricini oleoyl lactic acid pharmaceutical salts, 20 to docosane acyl group lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, stearic acid lactic acid pharmaceutical salts,

N-12 to docosane acylglycine pharmaceutical salts, N-12 to docosane acyl group alanine pharmaceutical salts, N-12 to docosane acyl group valine pharmaceutical salts, N-12 to docosane acyl glutamic acid pharmaceutical salts, N-12 to docosane acyl acylaspartic acid pharmaceutical salts, N-12 to docosane acyl group-N-methyl-Beta-alanine pharmaceutical salts, two-TEA-palmityl aspartic acid pharmaceutical salts, 12 to docosane acyl group sarcosine pharmaceutical salts,

Cholic acid pharmaceutical salts, taurocholic acid pharmaceutical salts, deoxycholic acid pharmaceutical salts, glycocholic acid pharmaceutical salts, glycodesoxycholic acid pharmaceutical salts, tauroursodeoxycholic acid pharmaceutical salts, ursodesoxycholic acid pharmaceutical salts, chenodeoxycholic acid pharmaceutical salts, chenodeoxycholyltaurine pharmaceutical salts, glycochenodeoxycholate pharmaceutical salts, 12 to docosane acyl glycyl for propylhomoserin pharmaceutical salts, caseinic acid pharmaceutical salts,

N α-ten are to two lauroyl arginine pharmaceutical salts methyl ester, N α-ten are to two lauroyl arginine pharmaceutical salts ethyl esters, N α-ten are to two lauroyl lysine methyl esters, N α-ten are to two lauroyl ethyl ester of lysine, N α-ten are to two lauroyl histidine pharmaceutical salts methyl ester, N α-ten are to two lauroyl histidine pharmaceutical salts ethyl esters, N1, N3-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,3-propane diamine, N1, N6-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl arginine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl lysine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl histidine pharmaceutical salts)-1,9-nonamethylene diamine, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group histidyl-pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl histidyl-pharmaceutical salts) glycerol, N-Cortex cocois radicis acyl arginine-ethyl ester of lysine pharmaceutical salts, and composition thereof.

38., according to the tablet of claim 1 or 2, it is characterized in that described medical additive E1 and/or medical additive E2 and/or medical additive E3 and/or medical additive E4 are selected from dioctyl 2-Sulfosuccinic acid pharmaceutical salts, octyl group 2-Sulfosuccinic acid pharmaceutical salts, the lauryl sulphate acid pharmaceutical salts, myristyl sulphuric acid pharmaceutical salts, ten to the octadecanoid acid pharmaceutical salts, the castor oil acid pharmaceutical salts, ten acid of acetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, ten acid of acetyl tartaric acid pharmaceutical salts diglycerol are to the behenic acid ester, ten acid of diacetyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, ten acid of diacetyl tartaric acid pharmaceutical salts diglycerol are to the behenic acid ester, ten acid of oxalyl tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of oxalyl tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, mix acetic acid pharmaceutical salts and ten acid of tartaric acid pharmaceutical salts glycerol list to the behenic acid ester, mix acetic acid pharmaceutical salts and ten acid of tartaric acid pharmaceutical salts diglycerol to the behenic acid ester, ten acid of citric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of citric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of succinic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of succinic acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of tartaric acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of tartaric acid pharmaceutical salts glycerol are to the behenic acid ester, ten acid of lactic acid pharmaceutical salts glycerol list are to the behenic acid ester, two ten acid of lactic acid pharmaceutical salts glycerol are to the behenic acid ester, ten to tadenan citric acid pharmaceutical salts glyceryl monoacetate, ten acid are to behenic acid acyl citric acid pharmaceutical salts ester, tartaric acid pharmaceutical salts Dan Shizhi docosane acyl ester, ten to docosane acyl butene dioic acid pharmaceutical salts, ten to docosane acyl propylene glycol succinate pharmaceutical salts,

Decoyl lactic acid pharmaceutical salts, caprinoyl lactic acid pharmaceutical salts, lauroyl lactic acid pharmaceutical salts, tetradecylic acid lactic acid pharmaceutical salts, hexadecylic acid lactic acid pharmaceutical salts, stearoyl lactic acid pharmaceutical salts, isostearoyl lactic acid pharmaceutical salts, oleoyl lactic acid pharmaceutical salts, cocos nucifera oil acyl lactic acid pharmaceutical salts, 12-hydroxyl stearoyl lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, Semen Ricini oleoyl lactic acid pharmaceutical salts, 20 to docosane acyl group lactic acid pharmaceutical salts, stearoyl-2-lactic acid pharmaceutical salts, stearic acid lactic acid pharmaceutical salts,

N-12 to docosane acylglycine pharmaceutical salts, N-12 to docosane acyl group alanine pharmaceutical salts, N-12 to docosane acyl group valine pharmaceutical salts, N-12 to docosane acyl glutamic acid pharmaceutical salts, N-12 to docosane acyl acylaspartic acid pharmaceutical salts, N-12 to docosane acyl group-N-methyl-Beta-alanine pharmaceutical salts, two-TEA-palmityl aspartic acid pharmaceutical salts, 12 to docosane acyl group sarcosine pharmaceutical salts,

Cholic acid pharmaceutical salts, taurocholic acid pharmaceutical salts, deoxycholic acid pharmaceutical salts, glycocholic acid pharmaceutical salts, glycodesoxycholic acid pharmaceutical salts, tauroursodeoxycholic acid pharmaceutical salts, ursodesoxycholic acid pharmaceutical salts, chenodeoxycholic acid pharmaceutical salts, chenodeoxycholyltaurine pharmaceutical salts, glycochenodeoxycholate pharmaceutical salts, 12 to docosane acyl glycyl for propylhomoserin pharmaceutical salts, caseinic acid pharmaceutical salts,

N α-ten are to two lauroyl arginine pharmaceutical salts methyl ester, N α-ten are to two lauroyl arginine pharmaceutical salts ethyl esters, N α-ten are to two lauroyl lysine methyl esters, N α-ten are to two lauroyl ethyl ester of lysine, N α-ten are to two lauroyl histidine pharmaceutical salts methyl ester, N α-ten are to two lauroyl histidine pharmaceutical salts ethyl esters, N1, N3-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,3-propane diamine, N1, N3-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,3-propane diamine, N1, N6-bis-(N-ten to two lauroyl arginine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl lysine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N6-bis-(N-ten to two lauroyl histidine pharmaceutical salts)-1,6-hexamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl arginine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl lysine pharmaceutical salts)-1,9-nonamethylene diamine, N1, N9-bis-(N-ten to two dodecanoyl histidine pharmaceutical salts)-1,9-nonamethylene diamine, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-acetyl group histidyl-pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl arginyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl lysyl pharmaceutical salts) glycerol, 1,2-bis-(ten to two dodecanoyls)-3-(N-formoxyl histidyl-pharmaceutical salts) glycerol, N-Cortex cocois radicis acyl arginine-ethyl ester of lysine pharmaceutical salts, and composition thereof, above-mentioned salt is selected from sodium salt, or potassium salt, or ammonium salt.

39., according to the tablet of claim 7 or 30, it is characterized in that described disintegrating agent is selected from low hydroxypropyl cellulose, carboxymethyl cellulose salt, polyvinylpolypyrrolidone, cross-linked carboxymethyl cellulose salt, cellulose fibre, cross linked polyacrylate and salt thereof, crosslinked Amberlite resin, alginate, carboxymethyl starch or the Microcrystalline Starch replaced, microcrystalline Cellulose and composition thereof; And/or

Described sweller is selected from the homopolymer of the homopolymer of the homopolymer of unsaturated acids or its salt or copolymer, unsaturated amides or copolymer, ethylene imine or copolymer, polyvinyl pyrrolidone, Ju Yi Xi oxazolidinone, Ju Yi thiazolinyl methyl oxazolidinone, polyvinylamine, polyvinylpyridine, polysaccharide sweller, alkyl glycol, polyalkylene oxide, oxygen vinyl alkyl ether and and their mixture.

40., according to the tablet of claim 7 or 30, it is characterized in that described sweller is selected from alginate jelly, pectin, xanthan gum, guar gum, Tragacanth, Radix Acaciae senegalis, glucosan, pectin, locust bean gum, carrageenin, starch, modified starch, Microcrystalline Starch, microcrystalline Cellulose, the cellulose of modification, the pharmaceutical salts of above-mentioned acidic polysaccharose, weight average molecular weight is greater than the following polymers that the degree of neutralization of 100000 acidity and/or basic functionality is 30～100 % by mole: acrylate copolymer, poly-carbon number is C1～C4 alkyl acrylic, poly-hydroxyl carbon number is C1～C4 alkyl acrylic, acrylic acid-acrylate polymer, polyvinyl alcohol-acrylic block copolymers, the starch graft acrylic acid polymer, the cellulose graft acrylate copolymer, humic acids, polycarbophil, alginic acid, poly-aspartate, polyglutamic acid, the poly-aspartic acid that mixes, the poly-glutamic acid that mixes, polyamine or poly-imines, polymine, polypropylene amine, polyethylenepolyamine, the polypropylene carbon number is C1～C4 alkylamine, poly-carbon number is C1～C4 alkyl allylamine, poly-carbon number is that C1～C4 alkyl propylene carbon number is C1～C4 alkylamine, poly-hydroxyl carbon number is C1～C4 alkyl allylamine, poly-hydroxyl carbon number is that C1～C4 alkyl propylene atomic number is C1～C4 alkylamine, aminopolysaccharide, chitin, chitosan, poly-asparagine, polyglutamine, polylysine, poly arginine, the poly-lysine that mixes, the poly-arginine that mixes, and their mixture.

41., according to the tablet of claim 1 or 2, it is characterized in that described active component is selected from central stimulants, analgesic, antipyretic, anti-inflammatory agent, antigout drug, antiparkinsonian drug, psychosis, antianxiety drugs, antidepressant, antuepileptic, tranquilizer, hypnotic, anticonvulsant, calcium antagonists, the medicine for the treatment of chronic cardiac insufficiency, anti-arrhythmic, control angina pectoris medicine, peripheral vasodilators, hypotensor, regulate blood fat medicine and antiatherosclerotic, the respiratory medicine thing, drugs for antiacid and peptic ulcer diseases, the gastrointestinal antispasmodic medicine, digestant, Bendectin, emetic and the intestines and stomach promote medicine, the liver and gall diseases adjuvant drug, medicine for urological system, act on the medicine of blood and hemopoietic system, allergy preparations, anaphylaxis medium sustained-release agent, adrenocortical hormone and thyroliberin, gonadal hormone and short gonadal hormone, hypoglycemic medicine, thyroid hormones medicine and antithyroid drug, antimicrobial agents, antitumor drug, strengthen or reduce the medicine of body's immunity, protein drug, Amitin, appetrol, Chinese herbal medicine powder and the Chinese herbal medicine extract that contains active component, and their combination.

42 The tablet of claim 1 or 2, characterized in that said active ingredient is selected from piracetam , Soft thiol, vinpocetine , dimebolin , aniracetam , cloth flunarizine , D buprenorphine , DHE , floctafenine , bicuculline , codeine, Rotundine , morphine, ergotamine, meptazinol , methadone, Nefopam , pethidine , horses minoxidil fixed , oxycodone, hydromorphone alcohol , tramadol , sumatriptan , tetrahydro Pama Ding , propoxyphene , dextromethorphan , levorphanol , left you pull amines , aspirin, acetaminophen , non- phenacetin , oxyphenbutazone , Tiaramide , magnesium salicylate, imidazole, isopropyl antipyrine , Amin ketoprofen, acemetacin , apazone , Ampiroxicam , Augustine protein , olsalazine , benorilate , topiramate ketoprofen , ibuprofen, bucillamine , aceclofenac , bufexamac , diflunisal , fenbufen , flurbiprofen , fluorine mefenamic acid, guanidine cetirizine Liu , clidanac , mefenamic acid , meclofenamic acid, sulfur glucose gold , auranofin , leflunomide, baclofen that acid loxoprofen , MA Aristolochic acid, meloxicam , mesalamine , nabumetone , naproxen, niflumic acid , etodolac , Zaltoprofen , healing blue oil hydrocarbons , according tolfenamic acid , isoxicam , ketoprofen, tenoxicam , zaleplon , zopiclone , zolpidem , betahistine , Changchun amines, flunarizine , fluorine America ketene , fluticasone Seoul , ring mandelic acid, adipic pentoxifylline , methanesulfonic dihydroergotamine , rizatriptan , methysergide , naratriptan , Nicole Xanthinol , nicergoline , kallikrein , niacin, iprindole , according to triptan , epoprostenol , isopropyl Zorro , papaverine, zolmitriptan , levetiracetam , anipamil , barnidipine , benidipine , bepridil , verapamil to Laval , Falipami , cinnarizine , lacidipine , manidipine , thiophene verapamil , verapamil, and right verapamil, oxyfedrine , isosorbide mononitrate , Chuan Shao hydrochloride , diltiazem , Ding four nitrate ester , benzene trihexyphenidyl fixed , cyclic adenosine monophosphate , lidoflazine , musk ketone , dipyridamole, pentaerythritol tetranitrate , nitroglycerin, Imo Lamine , according to his benzophenone , cyclic adenosine monophosphate , apovincamine , Changchun amines, pinacidil , vinconate , Changchun Pei alcohol, daga pamidronate , buflomedil , fasudil , Golovin verapamil , hydralazine , hydralazine cards , meters minoxidil , nicorandil , naftidrofuryl , trapidil , hydralazine , urapidil , bromine vincamine , inositol, niacin , according to the horizon , isopropyl , the isopropyl fluvoxamine , poppy Lin , steroid cutting to Seoul , levemopamil , Zuole Ting , alfuzosin , alacepril , A peptide that legislation , amlodipine her flat , fixed times Thani , benazepril , farthings ricin , bunazosin , methimazole , delapril , come lol , Ding topiramate amine test , doxazosin , irbesartan, felodipine, fosinopril, tetrandrine , methyl dopa, daidzein , ammonium tartrate spray care , captopril , candesartan , quinapril , clonidine, lisinopril, ramiprilat , Rilmenidine , reserpine , spirapril , lofexidine , mecamylamine , nilvadipine , nicardipine , nimodipine, nitrendipine, nisoldipine, pargyline , perindopril , trandolapril , terazosin , temocapril , Tuoluo Ni set , cilazapril , nifedipine, valsartan, isradipine , according Lisha Tan , enalkiren , enalapril , enalaprilat , according to the general Chastain , indoramin , left lofexidine , zofenopril ,Zofenoprilat , telmisartan, aminophylline, ambroxol , orciprenaline , former Austrian pull set , benproperine Lin , bitolterol , benzonatate , pirbuterol , ground cloth , sodium acetate to Mae Sot , deptropine , erdosteine , fenoterol , Pholcodine , hyssop that Lin , clenbuterol , neoprene for Connaught , mabuterol , montelukast , horse test piperazine forest , terbutaline , guaifenesin , potassium guaiacol , xamoterol , left propoxyphene , iso Mini Er , half- acetyl sarcosine, ketotifen , terbutaline , tulobuterol , according to Michel ketone , terpineol, omeprazole, balsalazide , Ohno prostaglandin , enprostil , famotidine, Gan hydroxyl aluminum, bismuth potassium citrate , lansoprazole , rabeprazole, sucralfate, Almagate , aluminum , bismuth , aluminum magnesium carbonate , Rosa epoprostenol , roxatidine , misoprostol , nizatidine , pirenzepine , plow Noto , pantoprazole, Xi Qu Pat , sofalcone , telenzepine , Irsogladine , ecabet , A to Fanning , acrivastine , alimemazine , astemizole , oxatomide , oxolumazine , diphenhydramine , phenindamine , propiomazine , Booker force hydrochloride , dimenhydrinate , tea acid promethazine, azelastine , Dingfu Rollins , Duozhasiting , doxylamine , embramine Pheniramine , fexofenadine , dimetindene , loratadine , clemastine , cloperastine , chlorpheniramine maleate , Mebhydrolin , meclizine , mequitazine , Ni Pula triazine, cyproheptadine, Secretary he Sting, ebastine , emedastine , epinastine , dexbrompheniramine , zafirlukast, levocabastine , azatadine , amlexanox , lodoxamide , tranilast , cromolyn sodium , cetirizine , zaprinast , Puck Romi , proxicromil , tazanolast , amoxicillin , ampicillin, bacampicillin , oxacillin , fluorine chlorine resistant, hetacillin , cyclohexanone amoxicillin , sulbenicillin card indene amoxicillin , cloxacillin , lenampicillin , nafcillin , pivampicillin , horses Mecillinam , penicillin V, sultamicillin , dicloxacillin , talampicillin , loracarbef , cephalexin, cefprozil , cefpodoxime , ceftibuten , cefaclor , cefixime , cephradine , Cefbuperazone , cephalosporins meters star, cefadroxil band , cephalosporins sand set , cephalosporins Telun , cefdinir , clavulanic acid, sulbactam, tazobactam bromine , paromomycin , kanamycin , gentamicin , neomycin, demeclocycline , doxycycline , guanidine a prostacyclin , metacycline , minocycline , oxytetracycline, tetracycline , chloramphenicol , azithromycin, troleandomycin , erythromycin , erythromycin, erythromycin ethylsuccinate , kitasamycin , josamycin , clarithromycin , roxithromycin, rokitamycin , spiramycin, meleumycinum , Midecamycin , propionate erythromycin estolate , Acetylspiramycin , levofloxacin, ofloxacin, ciprofloxacin, norfloxacin , polymyxin E, clindamycin, lincomycin, fosfomycin , Mika neomycin , nystatin , palmatine , Berberis alkali , snow choline , sodium houttuyfonate , acyclovir, famciclovir , valacyclovir , lamivudine , ribavirin, Moroxydine , zidovudine , doxifluridine go didanosine , zalcitabine , finasteride , epristeride , epalrestat , vitamins , and combinations thereof .

43. the tablet according to claim 1 or 2, the consumption that it is characterized in that described active components A 1 is 0.0001%(wt./wt.) to 90%(wt./wt.), the consumption of described diluent B 1 is 1%(wt./wt.) to 99%(wt./wt.), the consumption of described fusible adhesion agent C1 is 0.5%(wt./wt.) to 90%(wt./wt.), above percentage by weight is based on the gross weight of tablet; And/or

The consumption of described diluent B 2 is 1%(wt./wt.) to 99.5%(wt./wt.), the consumption of described fusible adhesion agent C2 is 0.5%(wt./wt.) to 99%(wt./wt.), above percentage by weight is based on the gross weight of tablet.

44. the tablet according to claim 1 or 2, it is characterized in that the medical additive E1 in described fusible adhesion agent C1-1, and/or the surfactant E2 in described fusible adhesion agent C1-2, and/or the medical additive E2 in described fusible adhesion agent C1-5, and/or the medical additive E3 in described fusible adhesion agent C1-6 or described core core 1, and/or the medical additive E4 in described fusible adhesion agent C1-7 or described core core 2, and/or the active components A 2 in described fusible adhesion agent C2-1, and/or the ratio that the active components A 2 in described fusible adhesion agent C2-2 or described core core 3 account in the fusible adhesion agent at its place is 0.005(wt./wt.) to 0.995(wt./wt.), surfactant D 1 in described fusible adhesion agent C1-1, and/or the medicinal lipid additive D2 in described fusible adhesion agent C1-2, and/or the fusible saccharide D3 in described fusible adhesion agent C1-5, and/or the fusible outer thing D1 that covers in described fusible adhesion agent C1-6, and/or the fusible outer thing D2 that covers in described fusible adhesion agent C1-7, and/or the fusible binding agent D1 in described fusible adhesion agent C2-1, and/or fusible outer in described fusible adhesion agent C2-2 to cover the ratio that thing D3 accounts in the fusible adhesion agent at its place be 0.005(wt./wt.) to 0.995(wt./wt.), above part by weight all is based on the gross weight of fusible adhesion agent, and/or

Described fusible adhesion agent C1-3, and/or the ratio that the hydrophilic surfactant E21 in fusible adhesion agent C1-4 accounts in the fusible adhesion agent at its place is 0.005(wt./wt.) to 0.25(wt./wt.), lipophilic surfactant D11 in described fusible adhesion agent C1-3, and/or the ratio that in fusible adhesion agent C1-4, medicinal lipid additive D21 accounts in the fusible adhesion agent at its place is 0.75(wt./wt.) to 0.995(wt./wt.), above part by weight all is based on the gross weight of fusible adhesion agent.

45. the preparation method according to the tablet of any one in claim 1 to 44 is characterized in that the method comprises:

(1), be selected from the operation of the fusible adhesion agent C1 of following preparation and/or C2:

Make to comprise at least one pharmaceutically acceptable fusing point (more described diluent B 1 low but) supplementary material that be not less than 25 ℃ of temperature and fusible surfactant D 1 and the high medical additive E1 of the more above-mentioned fusible surfactant D 1 of at least one pharmaceutically acceptable fusing point form fusing point (more described diluent B 1 low but) the fusible solid dispersion I that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-1, perhaps

Make to comprise at least one fusing point (more described diluent B 1 low but) supplementary material that be not less than 25 ℃ of temperature and that fusible medicinal lipid additive D2 and at least one pharmaceutically acceptable fusing point are not less than the surfactant E2 of above-mentioned medicinal lipid additive D2 form fusing point (more described diluent B 1 low but) the fusible solid dispersion II that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-2, perhaps

Make to comprise at least one fusing point (more described diluent B 1 low but) higher than pharmaceutically acceptable lipophilic surfactant D11 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the supplementary material of the hydrophilic surfactant E21 of 25 ℃ of temperature form fusing point (more described diluent B 1 low but) the fusible solid dispersion III that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-3, perhaps

Make to comprise at least one fusing point (more described diluent B 1 low but) higher than medicinal lipid additive D21 25 ℃ of temperature and fusible and at least one pharmaceutically acceptable fusing point lower than the supplementary material of the hydrophilic surfactant E21 of 25 ℃ of temperature form fusing point (more described diluent B 1 low but) the fusible solid dispersion IV that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-4, perhaps

Make to comprise at least one pharmaceutically acceptable fusing point (more described diluent B 1 low but) supplementary material that be not less than 25 ℃ of temperature and that fusible saccharide D3 and at least one pharmaceutically acceptable fusing point are not less than the hydrophilic medical additive E2 of 25 ℃ of temperature form fusing point (more described diluent B 1 low but) the fusible solid dispersion V that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-5, above-mentioned medical additive E2 do not comprise pharmaceutically acceptable fusing point (more above-mentioned diluent B 1 low and) more above-mentioned fusible saccharide D3 low but be not less than 25 ℃ of temperature and fusible surfactant D 1, perhaps,

Make at least one fusing point (more described diluent B 1 low but) be not less than 25 ℃ of temperature fusible outer cover thing D1 be overlying on outward core core 1 that fusing point is not less than 25 ℃ of temperature form fusing point (more described diluent B 1 low but) the fusible solid coating I that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-6, above-mentioned fusible outer cover thing D1 comprise at least one pharmaceutically acceptable fusing point (more described diluent B 1 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, above-mentioned core core 1 comprises the medical additive E3 that at least one fusing point is not less than 25 ℃ of temperature, perhaps,

Make at least one fusing point (more described diluent B 1 low but) be not less than 25 ℃ of temperature fusible outer cover thing D2 be overlying on outward core core 2 that fusing point is not less than 25 ℃ of temperature form fusing points (more described diluent B 1 low but) the fusible solid coating II that is not less than 25 ℃ of temperature obtains fusible adhesion agent C1-7, above-mentioned fusible outer cover thing D2 comprise at least one pharmaceutically acceptable fusing point (more described diluent B 1 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, above-mentioned core core 2 comprises the hydrophilic medical additive E4 that at least one fusing point is not less than 25 ℃ of temperature, perhaps,

Make the further combination in any formation of the solid dispersion solid dispersion VI in above-mentioned fusible adhesion agent C1-1～C1-5 obtain fusible adhesion agent C1-8, or,

Make two or more in above-mentioned fusible adhesion agent C1-1～C1-8 be mixed to get fusible adhesion agent C1-9;

And/or

Make to comprise at least one active components A 2 and at least one fusing point (more described diluent B 2 low but) supplementary material that is not less than the fusible binding agent D1 of 25 ℃ of temperature form fusing point (more described diluent B 2 low but) the fusible solid dispersion VII that is not less than 25 ℃ of temperature obtains fusible adhesion agent C2-1, above-mentioned fusible binding agent D1 comprise at least one pharmaceutically acceptable fusing point (more described diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1, and/or at least one pharmaceutically acceptable fusing point (more described diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, and/or

Make at least one fusing point (more described diluent B 2 low but) be not less than 25 ℃ of temperature fusible outer cover thing D3 be overlying on outward core core 3 form fusing points (more described diluent B 2 low but) the fusible solid coating III that is not less than 25 ℃ of temperature obtains fusible adhesion agent C2-2, above-mentioned fusible outer cover thing D3 comprise at least one pharmaceutically acceptable fusing point (more described diluent B 2 low but) be not less than 25 ℃ of temperature and fusible surfactant D 1 and/or at least one pharmaceutically acceptable fusing point (more described diluent B 2 low but) be not less than 25 ℃ of temperature and fusible saccharide D3, above-mentioned core core 3 comprises at least one active components A 2,

And the core core mean diameter be wrapped by the dispersed component particle in above-mentioned solid dispersion (I～VII) or dispersate particle or discontinuous phase particle and/or above-mentioned solid coating (I～III) is not more than 100 μ m;

(2) the tablet supplementary material that, makes to comprise described active components A 1, described diluent B 1, described fusible adhesion agent C1 mixes and makes it to have the operation of pharmaceutically acceptable tablet spatial shape;

And/or

Make the tablet supplementary material that comprises described diluent B 2, described fusible adhesion agent C2 mix and make it to there is the operation of pharmaceutically acceptable tablet spatial shape;

(3) the tablet form thing that, will be obtained by operation (2) is heated to the melt temperature of the melting composition in above-mentioned fusible adhesion agent C1 and/or C2 or the operation that above temperature makes its fusing;

(4), by the operation of the melting composition cooled and solidified in the above-mentioned fusible adhesion agent C1 melted in the tablet form thing that operation (3) obtain and/or C2.

46., according to the method for claim 45, it is characterized in that described operation (2) adopts non-pressing process.

47., according to the method for claim 45, it is characterized in that heating at the tablet form thing that obtained by operation (2) in described operation (3) temperature below the melt temperature of the melt temperature of described melting composition or above temperature and described diluent (B) and described active component (A).

48. the method according to claim 45, it is characterized in that active component, diluent and the fusible adhesion agent described in described operation (3) heating process do not degraded or non-volatile, perhaps, described active component, diluent and above-mentioned fusible adhesion agent degraded and/or the amount of volatilizing are no more than 10% of the front amount of preparation.

49., according to the method for claim 45, it is characterized in that describedly making to comprise that described tablet supplementary material mixes and make in its operation with pharmaceutically acceptable tablet spatial shape (2) fusion by the volatile component of removing and/or the component that can be biodegradable into innocuous gas.

50. the method according to claim 49, the component that it is characterized in that described volatile component and/or can be biodegradable into innocuous gas is selected from benzoic acid, benzoate, vanillin, ethyl vanillin, raceme Camphora, levo-camphor, gum camphor, the raceme Mentholum, levorotatory menthol, the dextrorotation menthol, natural or synthetic borneol, raceme Borneolum Syntheticum, L-Borneol, dextro Borneolum Syntheticum, the raceme isoborneol, left-handed isoborneol, the dextrorotation isoborneol, dithiooxamide, 6-methyl-2-deracil, azulene sulfonic acid, butylated hydroxyarisol, the di-tert-butyl hydroxy-methylbenzene, salicylic acid, aspirin, ethenzamide, the caffeine hydrate, the caffeine anhydride, caffeine citrate, caffeine benzoate, caffeine salicylate, the aspirin caffeine, alanine, leucine, isoleucine, valine, phenylalanine, carbamide, urethane, ammonium halide, ammonium bicarbonate, ammonium carbonate, ammonium acetate or their mixture.