CN205411710U - Solid -state soft mouth that contains many units carrier dissolves spindle - Google Patents
Solid -state soft mouth that contains many units carrier dissolves spindle Download PDFInfo
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Abstract
The utility model provides a solid -state soft mouth that contains many units carrier dissolves spindle, its carrier that includes core, shell and carry active material. The heart is checked to the shell package, and the carrier distributes in core, shell or above -mentioned among the two. Solid state or the liquid material of active material for having biological activity. The utility model discloses a solid -state soft mouth dissolves the spindle and after chewing, can collapse in the oral cavity and loose or dissolve to disengage active material or nutrient that the carrier carried, in order to health absorption active material or nutrient, this solid state is dissolved the spindle for soft mouthful and can be made things convenient for aphetite disorder group to absorb some active material who has pharmacology or biological activity or nutrients.
Description
Technical field
This utility model relates to a kind of peroral dosage form, and in particular to a kind of soft peroral dosage form of solid-state.
Background technology
Along with the progress of preparation technique, type of preparation the most pharmaceutically is more and more various, from the medicinal liquid of the lozenge of solid-state to liquid, from Expidet to the various dosage forms controlling release, can do different designs according to required medicine effect.But, many medicines all have unpleasant taste, and therefore for old man with child, drug administration often becomes a kind of burden.
Capsule is initially intended for the dosage form of filling medicine, can quantitatively powdery or aqueous medicine take unit, and the offending sense of taste of medicine can be avoided.But, capsule of eating, to many dysphagia groups, such as child, child, old man, chronic and cancer patient, also becomes a burden.
Utility model content
Dysphagia group absorbs some and has pharmacology or bioactive active substance or nutrient for convenience, and the dosage form that can chew in the oral cavity is a kind of direction attempted.Provide below a kind of solid-state containing many units carrier molten ingot of soft mouth, after chewing, the molten ingot of the soft mouth of solid-state can disintegration or dissolving in the oral cavity, and disengage the active substance entrained by carrier or nutrient, in order to health absorbing activity material or nutrient.
Therefore, one side of the present utility model is to provide a kind of solid-state containing many units carrier molten ingot of soft mouth.The molten ingot of the soft mouth of above-mentioned solid-state comprises core, shell and multiple carrier.Its housing is coated on outside core, and carrier is then distributed among core, shell or said two devices.The main material of above-mentioned core is sugar alcohol, edible colloid or food starch, and the sweeting agent used by core is few candy or sugar alcohol.Above-mentioned carrier is used to carry at least one active substance, and active substance is for having bioactive solid-state or liquid.
Foundation one embodiment, the solid-state containing the many units carrier of the present utility model molten ingot of soft mouth, including: soft sweet core；Shell, is coated with described soft sweet core；And for carrying multiple carriers of at least one active substance, be distributed in described soft sweet core, described shell or a combination thereof, wherein said active substance is for having bioactive solid-state or liquid.
According to an embodiment, above-mentioned carrier includes microgranule, microsphere, micro-fat body, sponge line grain, drop pill or above-mentioned combination in any.
According to an embodiment, above-mentioned carrier there is coating at least partially.
According to an embodiment, further including a macromolecule and be positioned in the coating of those carriers, this macromolecule forms mucus in saliva, is retained in the intraoral time improving active substance.
According to an embodiment, above-mentioned macromolecule includes the copolymer of methacrylic acid, the copolymer of methacrylic acid aminoalkyl ester, the copolymer of methacrylate, the copolymer of alkyl methacrylate Arrcostab, hydroxypropyl cellulose, hydroxypropyl methylcellulose or its combination in any.
According to an embodiment, further include an absorption enhancer and be positioned among this core, this shell, those carriers or above-mentioned combination in any.
According to an embodiment, above-mentioned absorption enhancer includes interfacial agent, fatty acid, ethanol, azone, spherical chitosan, phospholipid, draws red dose and piperine or its combination in any.
According to an embodiment, above-mentioned fatty acid includes having the saturated of 8-20 carbon or unsaturated fatty acid.
According to an embodiment, above-mentioned phospholipid includes lecithin.
According to an embodiment, above-mentioned interfacial agent includes anionic interfacial agent or cationic interfacial agent.
According to an embodiment, above-mentioned draw red dose and include Rhizoma Zingiberis powder or its oil extract, Fructus Capsici powder and or oil extract, Cortex Cinnamomi powder, Oleum menthae, wintergreen oil or Oleum Cinnamomi.
According to an embodiment, further include an acid-base buffer agent and be positioned in this core, this shell, those carriers or above-mentioned combination in any.
According to an embodiment, above-mentioned acid-base buffer agent includes weak-type buffer agent, and this weak-type buffer agent includes citric acid, malic acid, tartaric acid, phosphoric acid, lactic acid, gluconic acid, glucuronic acid, vitamin C, acetic acid or salicylic acid.
According to an embodiment, above-mentioned acid-base buffer agent includes weak alkaline-type buffer, and this weak alkaline-type buffer includes bicarbonate.
According to an embodiment, further include a stickum and be positioned in this carrier.
According to an embodiment, above-mentioned stickum includes gelatin, pectin, arabic gum, starch, polysaccharides, hydroxypropyl methyl cellulose, protein, polypeptide, dead bacterium or its combination in any.
Above-mentioned utility model content aims to provide the simplification summary of this disclosure, so that reader possesses basic understanding to this disclosure.The complete overview of this utility model content not this disclosure, and it is not intended to pointing out the key/critical element of this utility model embodiment or defining scope of the present utility model.After refering to following description, this utility model art has usually intellectual when will readily appreciate that essence spirit of the present utility model and other utility model purposes, and the technological means that used of this utility model and enforcement aspect.
Accompanying drawing explanation
For following and other purposes, feature, advantage of the present utility model can be become apparent with embodiment, being described as follows of appended accompanying drawing:
Fig. 1 is based on the cross-sectional view of a kind of solid-state containing many units carrier molten ingot of soft mouth of this utility model one embodiment；
Wherein, symbol description:
100: the molten ingot of the soft mouth of solid-state 102: core
104: shell 106: carrier.
Detailed description of the invention
As mentioned above, utilize that to add the carrier of many units in the solid-state molten ingot of soft mouth various at normal temperatures as solid-state or the active substance of liquid to carry, allow the sweet taste of the solid-state molten ingot of soft mouth and fragrance to process the offending sense of taste of active substance part, such as bitterness and astringent taste etc., allow dysphagia group that various active substance is easily administered orally.
Therefore it provides a kind of solid-state containing many units carrier molten ingot of soft mouth.In following narration, it will introduce the manufacture method that the exemplary configuration of the above-mentioned molten ingot of soft mouth of the solid-state containing many units carrier illustrates with it.In order to be readily understood by the event of described embodiment, many ins and outs are provided below.Certainly, not all embodiment all needs these ins and outs.Meanwhile, some structures being widely known by the people or element, only can draw the most in the accompanying drawings, suitably to simplify accompanying drawing content.
Structure containing many units carrier solid-state molten ingot of soft mouth
Due to soft sweet meeting disintegration and dissolving in the oral cavity after chewing a period of time, if can also directly swallow if even its size is the least.Therefore, if active substance can be added in soft sweet, make the solid-state molten ingot of soft mouth, then active substance can be allowed in mastication processes to disengage in saliva.But, active substance how will be allowed can to bear the various manufacturing conditions of the solid-state molten ingot of soft mouth without going bad, using carrier is a feasible solution.Therefore, a kind of solid-state containing many units carrier molten ingot of soft mouth and preparation method thereof is provided at this.
According to kind, water content and the processing procedure of coagulator used by it, the molten ingot of the soft mouth of solid-state is about divided into following several types: soft chew ingot, soft speed collapses ingot, fruit jelly soft sweet, elasticity jelly and speed collapse soft sweet.Its external form can determine into any shape needed for depending on, wherein simple external form can be ingot shape or spherical.
Fig. 1 is based on the cross-sectional view of a kind of solid-state containing many units carrier molten ingot of soft mouth of this utility model one embodiment.In FIG, the external form of the molten ingot of the soft mouth of solid-state 100 can be any required shape, the most spherical, diamond type or other any required forms.The structure of the molten ingot of the soft mouth of solid-state 100 includes core 102, the shell 104 being enclosed in core 102 surface and for carrying the carrier (multi-unitactivecarriers) 106 of various different activities material.Above-mentioned carrier 106 can be distributed in core 102, shell 104 or above-mentioned within both.
Above-mentioned a kind of soft sweet of core 102, containing sweeting agent and the coagulator being used for fixing shape.The water content of core 102 is 5-30wt%, such as, can be 10wt%.In addition to above-mentioned sweeting agent, it is also possible to add other various different acidic flavoring agent, spice and taste stimulation agent etc. as correctives.Furthermore it is also possible to interpolation absorption enhancer, to increase the buccal absorption amount of active substance.In addition, the acid-base buffer agent of weak-type can also be added, the molecule allowing some active substance is under electroneutral molecular state or free state (freeform), to help it can penetrate oral mucosa, absorbed via intracellular (intracellular) or the approach of iuntercellular (intercellular).
Above-mentioned shell 104 can be the structure of single or multiple lift, can be by the dried self-assembling formation shell 104 of core 102, or allowing core 102 additionally wrap up sugar-coat, film clothing or a combination thereof forms shell 104.Therefore the material of shell 104 includes correctives, such as sweeting agent, acidic flavoring agent, spice and taste stimulation agent.Additionally, the most optionally add absorption enhancer and the acid-base buffer agent of weak-type in shell 104.Owing to core 102 water content of the solid-state molten ingot of soft mouth is higher, so shell 104 can avoid core 102 to be adhered to one another, it is also possible to stablize the water content of core 102, it is to avoid core 102 is hardening.If additionally, shell 104 has various opaque color, it is also possible to side is positioned at the active substance shading of core 102, it is to avoid produce photochemical reaction.Additionally, the shell 104 of shades of colour may also provide the outward appearance relatively making us pleasing.
Above-mentioned carrier 106 is containing active substance, and it can comprise synthetic, have bioactive chemical substance (such as health food, nutriment or medicine) or biological substance (such as enzyme, born of the same parents' device or dead bacterium) from natural goods extraction or by any available of bioconversion.Therefore, when chewing the solid-state molten ingot 100 of soft mouth, can allow carrier 106 in the case of pressing close to oral mucosa, disengage the active substance of high concentration, and then improve the oral mucosa absorbtivity to active substance.In core 102, the addition of carrier 106 may be up to as 95wt%.
The diameter of carrier 106 is about 0.03-3,000 μm, and according to an embodiment, it can be 100-1,000 μm.Generally, when the diameter of carrier 106 is less than 150 μm, the sense of touch of oral cavity and tongue is i.e. difficult to discover.When the diameter of carrier 106 is less than 450 μm, it is difficult to when chewing be broken by the teeth by tooth at short notice, therefore the absorbance of oral cavity transmission system can be improved with longer chew time, make its can slow release slowly absorbing activity material, so the steady concentration of active substance in blood can be maintained in the long period.
Above-mentioned active substance includes maincenter type appetite suppressant, and it can be such as Africa Fructus Mangifera Indicae extract or bigarabe extract, and wherein bigarabe extract can also improve metabolism.Above-mentioned active substance can be the most also the inductor of Vitamin B1, such as benfotiamine (benfotiamine).
Additionally, carrier 106 is also selectively included absorption enhancer, acid-base buffer agent, the macromolecule that can form mucus in saliva and stickum.Wherein, macromolecule and stickum can increase active substance residence time in the oral cavity, to increase the buccal absorption rate of various different activities material.Such as can increase and be belonging respectively to Biopharmaceutics Classification system first and second and the highly-water-soluble of three classes (biopharmaceuticalclassificationsystemI, IIandIII) and high mucosa penetrance, low aqueous solubility but high mucosa penetrance and highly-water-soluble but the buccal absorption rate of the active substance of low mucosa penetrance.
The form of carrier
Above-mentioned carrier 106 can be any temperature that can bear the soft mouth of solid-state molten ingot manufacture process and pressure the carrier that be enough to protect active substance, such as, can be to meet the microgranule (pellet) of above-mentioned condition, sponge line grain (Spongellet), microsphere (microsphere), drop pill (droppingpill), micro-fat body (liposome) or above-mentioned combination in any.
Above-mentioned microgranule is the microspheres that is combined into excipient (excipients) of a kind of powder by active substance or liquid or globoid, and its size is typically smaller than 2.5mm.Microgranule is usually to be prepared by extrusion spheronization mode, liquid layered manner, powder body layered manner or a combination thereof can also be used to be coated with the multilamellar material with difference in functionality on core particle, even also can be coated with one or more layers coating at outermost layer again, and reach to increase the degree of stability of active substance entrained by it, control its release including active substance or control the purpose of its absorption external substance.The type of above-mentioned coating can be sugar-coat or film clothing.
For sugar-coat, the main material of sugar-coat can be such as single candy, double candy, few candy or sugar alcohol, is therefore possible not only to improve outside the sense of taste, also can increase stability and the hardness of microgranule.
For film clothing, its type such as can be divided into time controlled release type, pH dependent form, moistureproof wet type, elastic force Anti-pressure, long-acting type and large intestine release type.The material of film clothing can be such as macromolecule, or has fatty acid or its esters of 5-50 carbon.Therefore, in addition to can increasing the stability of microgranule, it is also possible to control the disintegrate under particular circumstances of film clothing, allow asperity contact external environment, discharge active substance.
Such as, when film clothing is elastic force Anti-pressure (its material is usually elastic fibers or elastin), the active substance (such as viable bacteria, reactive protein and polysaccharides etc.) that crushing resistance is less can be helped, the pressure born when manufacturing process is with molding with the opposing solid-state molten ingot of soft mouth, and still can keep its activity.
Such as, when film clothing belongs to moistureproof wet type, it is also possible to protection meeting is deactivated active substance (such as carnitine etc.) to moisture-sensitive, active substance is made can to maintain its activity during the manufacture process of the solid-state molten ingot of soft mouth and storage.
Such as, when film clothing belongs to pH dependent form, the sourest insoluble type, then can protect the active substance sensitive to pH, make active substance can maintain its activity during solid-state soft mouth molten ingot manufacture process and storage.
Such as, when film clothing belongs to time controlled release type, its perforated membrane clothing that can use insoluble in gastric juice Yu intestinal juice, utilize the number of hole number to control the rate of release of active substance.For example, during slow release formulation, it is possible to decrease the unhappy sense of taste such as bitterness that active substance was discharged within the unit interval, astringent taste, fishy smell.If during fast dissolving dosage form, then can comparatively fast discharge the joyful sense of taste of the sweet taste of active substance, tart flavour, fragrance so that it is with the sense of taste that the active substance with the unhappy sense of taste competes oral cavity.So utilizing this machine to turn, it is possible to resolve the born abnormal flavour of draft extract, food additives and medicine in major part active substance.
Above-mentioned sponge line grain is the wire pharmaceutical carrier of a kind of porous, and it prepares method generally allows active substance and highly-water-soluble material mix with appropriate water and in addition after extrusion molding, then forms the sponge line grain with loose structure with various different seasonings.Because sponge line grain has loose structure, it is possible to form composite construction with various microgranules, micro-fat body with microsphere.
The material of the porous matrix of sponge line grain is usually cellulose, starch, water-soluble substances or a combination thereof.Above-mentioned celluloses can be such as hydroxypropyl methylcellulose (hydroxypropylmethylcellulose；HPMC), hydroxypropyl cellulose (hydroxypropylcellulose；HPC), hydroxyethyl cellulose (hydroxyethylcellulose；HEC), microcrystalline Cellulose (microcrystallinecellulose, MCC) or its combination in any.Above-mentioned water-soluble substances can be such as aminoacid or sugar alcohol (molecular weight is many less than 200D).Owing to sponge line grain has porous matrix, the active substance of liquid or solid-state, the active substance being such as dissolved in fluid oil (such as highly purified phylloxanthin and the composition such as the extract of zeaxanthin or additive) or the nanometer fine powder to secondary micron is received with depositing so can be used to adsorb.Therefore, for liquid or the active substance of suspended state, the structure of sponge line grain can protect it from running off in the extruding action of the soft mouth of solid-state molten ingot manufacture process and retaining.For the solid active material of fine powder class, the structure of sponge line grain can maintain its after processing with the activity in mastication processes.Above-mentioned sponge line grain is the same with microgranule, it is possible to have the coating of various difference in functionalitys or film clothing, to reach to increase the degree of stability of active substance, control the release of active substance and control the purpose of absorption external substance.
Above-mentioned microsphere is a kind of pharmaceutical carrier allowing medicine be dispersed in polymer matrix, and its size is usually nanometer to micron grade, e.g., less than 800 μm.The material of common polymer matrix includes starch, albumin (albumin), gelatin (gelatin), spherical chitosan (chitosan), polylactic acid (polylactide；And ring polylactic acid (cyclicpolylactate PLA)；CPL) etc..Its preparation method is typically to allow active substance be dissolved or dispersed in macromolecular solution, and the mode that recycling is spray-dried forms microsphere solid.
Above-mentioned drop pill, be medicine is uniformly mixed with excipient or is dispersed into a liquid system after, then instill indissoluble liquid shape, so it can form thin film in the outside of class spherosome.Therefore, drop pill is also a kind of pharmaceutical carrier, is used for carrying applicable active substance.
Above-mentioned micro-fat body is a kind of spherical imitated vesicle structure, can be used to accommodate medicine inside it.Micro-fat body can be present in the hole of microgranule, microsphere or sponge line grain in liquid form, or can be by processing and be present in the main body of microsphere and drop pill.
From the above, carrier 106 is used to carry active substance and and then be applied to the solid-state molten ingot of soft mouth, the most following benefit.First, the deenergized period of active substance can be increased.For example, the deenergized period when active substance makes powder is typically less than 5 minutes；If make diameter 1mm microgranule, its deenergized period is about 10～15 minutes；If make diameter 0.45mm microgranule, its deenergized period is about 7.5～10 minutes.
Secondly, carrier 106 can increase the steady chemical structure of the active substance with unstable chemical constitution.For the active substance that chemical constitution is unstable; whether sensitive to oxygen, dampness, light, temperature, pressure or other factors active substance; the various different qualities of carrier 106 can be modified by various different modes; there is the active substance of various different qualities with protection; will not lose activity during allowing it in the manufacturing process of the solid-state molten ingot of soft mouth and storing, and play its complete effect when chewing the solid-state molten ingot of soft mouth.
Coming, carrier 106 can be used to carry the active substance being not suitable for putting together again.Such as, chemical reaction can be carried out after contacting with each other and destroy its activity or produce the active substance of toxicity, when can carry respectively with different carriers 106, will not contact each other during just can allowing it in the manufacturing process of the solid-state molten ingot of soft mouth and storing, thus keep its original activity, until just play its complete effect when chewing the solid-state molten ingot of soft mouth.
The material of each composition
What above-mentioned coagulator was conventional has sugar alcohol, food starch, edible colloid or above-mentioned combination in any.Above-mentioned sugar alcohol, such as, can be mannitol (mannitol).Conventional food starch such as has tapioca (maniocstarch), corn starch (cornstarch), potato starch (potatostarch) and raw rice starch (uncookedricestarch).Conventional edible colloid can divide animal glue and plant gum according to source.Common animal glue has gelatin (gelatin), Colla Corii Asini (donkey-hidegelatin) and fish glue (fishgelatin).Common plant gum has Eucheuma gelatinosum glue (agar), antler glue (carrageenan), alginate jelly (alginatejelly), arabic gum (Gumarabic), close China's locust beam gum (guargum), cellulose (cellulose), angle bean fruit (carobfruit), Oryza glutinosa glue (glutinousriceglue), the poly-candy in β-Portugal (β-glucan), pectin (pectin), arabic gum (Acaciagum) and xanthan gum (xanthan).
Above-mentioned Sweetening agents is as being single candy, double candy, few candy, sugar alcohol or above-mentioned combination in any.Single candy can be such as pentose or hexose, and common pentose has arabinose and xylose, common hexose to have idose, glucose, fructose and galactose.Double candys can be such as sucrose, lactose, maltose or trehalose.Few candy is typically to be made up of 3-9 single candy unit, such as, can be oligofructose, oligomeric galactose, IMO, soybean oligo saccharide or oligomeric xylose.The aldehyde radical of sugar alcohol typically glycan molecule or ketone group are formed after being reduced into alcohol radical, such as, can be glucitol, xylitol, Sorbitol, maltose alcohol, erithritol, lactose or mannitol.
The major function of sweeting agent is for providing the sweet taste of the solid-state molten ingot of soft mouth, and part sweeting agent also has the effect assisting solidification, and some sweeting agent also has other physiological function.The few candy of such as part or sugar alcohol have the function of similar water soluble dietary fiber, can promote the health of the intestines and stomach and help to breed enteral probiotic bacteria.Sugar alcohol then can assist diabetics to control blood glucose, and assists obese patient to control the picked-up of heat.
Correctives in addition to sweeting agent, can be any available acidic flavoring agent, spice, taste stimulation agent, savory agent or its combination in any.Acidic flavoring agent can be such as citric acid, malic acid, lactic acid, gluconic acid etc..Spice can be such as various natural fruit flavorings, edible plants spice and edible artificial flavors.Taste stimulation agent includes coolant agent and draws red dose, and wherein coolant agent can be such as Herba Menthae, and drawing red dose can be Rhizoma Zingiberis powder or its oil extract, Fructus Capsici powder or oil extract, Zanthoxyli Bungeani powder or oil extract, Cortex Cinnamomi powder, Oleum menthae, wintergreen oil or Oleum Cinnamomi etc..Savory agent can be Sal.The most frequently used person can be such as natural fruit juice or milk.
Above-mentioned acid-base buffer agent can be divided into weak-type and weak base type two class.The acid-base buffer agent of weak-type can be such as citric acid, malic acid, tartaric acid, phosphoric acid, lactic acid, gluconic acid, glucuronic acid, vitamin C, acetic acid or salicylic acid.Weak-type acid-base buffer agent is except can be used to control intraoral pH-value, and improve outside the dissolubility of weak-type or weak base type active substance, also can reduce the sense of taste sensitivity to abnormal flavour (such as bitterness), and assist the molecule of some active substance to be in electroneutral free state (freefrom), absorbed in order to it penetrates oral mucosa.The acid-base buffer agent of weak base type includes bicarbonate, such as sodium bicarbonate or potassium bicarbonate.The acid-base buffer agent of weak base type, in addition to can be used to control intraoral pH-value, also can stablize some active substances, if can be with aerogenesis, it is also possible to increases the rate of release of active substance.When the solid-state molten ingot of soft mouth need to be simultaneously introduced weak-type and weak alkaline-type buffer, weak-type and weak base type are necessarily present in the diverse location of the solid-state molten ingot of soft mouth.Most common situation is that weak acid is present in the solid-state molten ingot of soft mouth, many units carrier, and weak base is present in carrier.
nullThe above-mentioned macromolecule that can form mucus in saliva is primarily used to form the coating of carrier 106，Its material includes the copolymer (methacrylicacidcopolymer) of methacrylic acid、The copolymer (aminoalkylmethacrylatecopolymer) of methacrylic acid aminoalkyl ester、The copolymer (methacrylatecopolymer) of methacrylate、The copolymer (alkylmethacrylatecopolymer) of alkyl methacrylate Arrcostab、Hydroxypropyl cellulose (hydroxylpropylcellulose)、Hydroxypropyl methylcellulose (hydroxypropylmethylcellulose) or its combination in any.nullThe copolymer of above-mentioned methacrylic acid can be such as poly-(methacrylic acid-co-ethyl acrylate) 1:1 [Poly (methacrylicacid-co-ethylacrylate) 1:1]、Poly-(methacrylic acid-co-methyl methacrylate) 1:1 [Poly (methacylicacid-co-methylmethacrylate) 1:1]、Poly-(methacrylic acid-co-methyl methacrylate) 1:2 [Poly (methacylicacid-co-methylmethacrylate) 1:2] or poly-(acrylic acid methyl ester.-co-methyl methacrylate-co-methacrylic acid) 7:3:1 [Poly (methylacrylate-co-methylmethacrylate-co-methacrylicacid) 7:3:1].Above-mentioned coating substance, by different treatment coatings steps, thus can form different film clothing layer or outer shell.
Above-mentioned stickum can be such as gelatin, pectin, arabic gum, starch, polysaccharides, hydroxypropyl methyl cellulose, protein, polypeptide, dead bacterium or its combination in any.Above-mentioned starch can be such as corn starch, tapioca, Rhizoma Dioscoreae starch, sweet potato starch or raw rice starch.The source of polysaccharides can be such as plant extraction, or is obtained by yeast or fungi fermentation.Above-mentioned protein can be such as collagen protein or glucoprotein.
Preparation method containing many units carrier solid-state molten ingot of soft mouth
Preparation method containing the soft mouth of many units carrier solid-state molten ingot core 102 can be by die methods or beat ingot method.
In die methods, first carry out the step of batch mixing stirring, the action that required raw material (sweeting agent, coagulator, carrier and other required additives) utilizes stirring is homogenously mixed together.Then carry out the step heated, be cooked into syrup.Then, after allowing syrup be cooled to uniform temperature in bigger mould, form solid, then cut or be pressed into appropriately sized, form core 102.
In beating ingot method, by required dried powder (sweeting agent, coagulator, carrier and other the required additives) mix homogeneously needing raw material, then utilize Ingot pressing machine to carry out playing ingot, then improved its moisture by outside, form core 102 through particular process program.
Finally, may choose whether to wrap again sugar-coat or the film clothing including desired additives, form shell 104, complete the making of the solid-state molten ingot of soft mouth 100.
Embodiment one:
In this embodiment, the core weight of the solid-state molten ingot of soft mouth of per unit is about 0.55g, and size is about 1.0 × 0.8 × 0.5mm3Square micro-ingot.Coagulator is the mixture of gelatin and starch.Sweeting agent is sucrose and maltose alcohol, and spice is caramel spice.Carrier is bigarabe extract compound recipe microsphere, vitamin C microsphere and the absorption enhancer microsphere of weight ratio 8:1:1, and absorption enhancer used is phospholipid serine and the mixture of phospholipid choline of weight ratio 1:1).
In this embodiment, it is prepared for several different shell.The coating that first three shell is predominantly formed by the mixture of maltose alcohol and sucrose.Different according to other adding ingredients, can be divided into following 3 kinds of coatings: without pigment transparent monolayer coating, add the single coats of caramel color, rose pink double-layer coatings (ground floor adds the calcium pyrophosphate of 1wt%, and second layer coating is the rose pink coating of the OPC containing 0.5wt% anthocyanidin).And the 4th kind of shell is the dark chocolate single coats melted.After having added shell, the weight gain of the molten ingot of the soft mouth of solid-state is about 0.15g (monolayer), 0.23g (double-deck) and 0.18g (chocolate).Material used by this embodiment is listed in following table one.Addressed table one from above, even same core material, shell still can have a variety of changes.
Additionally, in this embodiment, also change carrier content in solid-state mouth molten ingot core, and test its mouthfeel, acquired results is listed in table below two.From the result of table two, the content of carrier is the highest, and the mouthfeel of the molten ingot of the soft mouth of solid-state can be the softest.
Table one
* the composition of absorption enhancer is phospholipid serine and the phospholipid choline of weight ratio 1:1
Table two
| Carrier content (%) in the core | Mouthfeel |
| 0 | Closely knit |
| 10 | The loosest |
| 15 | Loosely |
| 20 | Loose |
| 50 | The loosest, graininess mouthfeel is obvious |
Embodiment two:
In this embodiment, coagulator changes belonging to the mixture of the pectin of plant gum and arabic gum into, replace the gelatin that tradition uses, allow core shape.The core size of the molten ingot of the soft mouth of solid-state is about 1.0 × 0.8 × 0.5mm3Square, weight is about 1.0g.Carrier used is bigarabe extract compound recipe microsphere, and addition is 10wt%.The single coats that shell is predominantly formed by the mixture of maltose alcohol and sucrose.Material used by this embodiment is listed in following table three.
Table three
Embodiment three:
In this embodiment, each composition asks for an interview table below four, but coagulator changes mannitol into, sweeting agent change into diabetics can sorbitol, maltose alcohol, oligofructose and Fructus Hordei Germinatus widow's candy.Carrier used is bigarabe extract compound recipe microsphere, and addition is 10wt%.
Table four
Embodiment four:
In this embodiment, each composition used looks at table below five, and wherein carrier changes the benfotiamine microsphere of weight ratio 8:1:1, vitamin C microsphere and absorption enhancer microsphere into.The composition of above-mentioned benfotiamine microsphere is the benfotiamine of weight ratio 70:10:8:1.5:0.5, microcrystalline Cellulose, instant coffee powder, hydroxypropyl methylcellulose and Sucralose.And benfotiamine microsphere can also further be dipped in the solution of sucrose solution or other sweeting agents, sucrose solution or sweetener soln is allowed to penetrate in the hole of benfotiamine microsphere.
In this embodiment, it is used for improving the benfotiamine (Benfotiamine) of diabetics clinical treatment side effect, its abnormal flavour can be modified by the raw material of benfotiamine microsphere and release characteristics, add the sweeting agent and spice added in the solid-state molten ingot of soft mouth and its core, the abnormal flavour of benfotiamine can be covered the most completely.
Table five
* the composition of benfotiamine microsphere is the benfotiamine of weight ratio 70:10:8:1.5:0.5, microcrystalline Cellulose, instant coffee powder, hydroxypropyl methylcellulose and Sucralose.
Embodiment five:
In this embodiment, active substance used is the oily solution of 20wt% lutein ester, and the detailed content of material therefor asks for an interview table below six.After being prepared as lutein ester microsphere, owing to its hardness is more than 7H, even across 100 DEG C and 400Kg/cm of the solid-state molten ingot of soft mouth2High Temperature High Pressure processing procedure, microsphere outward appearance remains in that well, it is sufficient to maintain lutein ester oily solution stability.
Table six:
* the composition of lutein ester microsphere is the lutein ester oily solution of weight ratio 30:65:5, microcrystalline Cellulose and hydroxypropyl methyl cellulose (hydroxylpropylmethylcellulose；HPMC).
Embodiment six:
Verdoflavin, in acidity has the environment of water, can carry out isomerization reaction, therefore can variable color have abnormal flavour.In this embodiment, the raw material of the carrier of experimental group is the vitamin C of weight ratio 75:5:20, Verdoflavin and microcrystalline Cellulose.Matched group is then the mixture of above-mentioned raw materials, and the weight ratio of vitamin C, Verdoflavin and microcrystalline Cellulose is also 75:5:20.
The preparation method of the molten ingot of the soft mouth of solid-state is to take carrier or the above-mentioned raw materials mixture of 100g, is separately added into 60g gelatin, 270g sucrose and 300g water, is stirred and heated to about 100 DEG C, forms uniform syrup mixture.It is cooled to room temperature and dried at normal temperatures, is further continued for cold preservation 12 hours.After taking-up, cutting into size is 1.0 × 0.8 × 0.5cm3Square, obtain the solid-state molten ingot of soft mouth.The raw material of matched group, also through identical process conditions, makes the solid-state molten ingot of soft mouth.Below the various materials used by this embodiment listed by table seven.
Below in table eight, the cosmetic variation after observing manufacture process and storing 14 days, to understand preparation and the storage stability of the solid-state molten ingot of soft mouth.From the result of table eight, in Verdoflavin puts into carrier, even if in the environment of acidity has water, also it is not easy to go bad, increases its stability.
Table seven:
* composition is the vitamin C of weight ratio 75:5:20, Verdoflavin and microcrystalline Cellulose.
Table eight:
Embodiment seven:
In this embodiment, test the dosage form of several different oral cavity release active substance, compare the length of its active substance the most sustainable release time.Active substance used herein is vitamin C, so being test tart flavour residence time length in the oral cavity.First gargle with drinking water before test, to have enough and constant wettability and relatively stationary temperature in maintaining oral cavity.Dosage form that each experimental example tested is set forth below, and acquired results arranges in the following table.
Experimental group is the molten ingot of soft mouth of the solid-state containing vitamin C and the microsphere of Verdoflavin.The raw material of microsphere is identical with the microsphere of above-described embodiment 11.Other raw materials of the molten ingot of the soft mouth of solid-state are the sucrose of weight ratio 7:1:1:1, gelatin, starch and water.The size of the molten ingot of the soft mouth of solid-state is 1.0 × 0.9 × 0.6cm3, weight is about 0.65g.Every solid-state molten ingot of soft mouth contains the vitamin C of 17wt% and the Verdoflavin of 1.1wt%.Detailed materials asks for an interview table below nine.
Table nine:
* composition is the vitamin C of weight ratio 75:5:20, Verdoflavin and microcrystalline Cellulose.
Matched group then has sublingual absorption type capsule described below, Sublingual Tablet, mouth collapse ingot and suck ingot.
The capsule of sublingual absorption capsule has the hole that 6 diameters are about 0.37mm, and inclusions is lactose and the vitamin C of 115mg of 115mg.
The diameter of Sublingual Tablet is about 6mm, its lactose containing 115mg and the vitamin C of 115mg.
Mouth collapses ingot and is contained within the disintegrating agent (sodium starch glycollate) of the lactose of 100mg, the vitamin C of 100mg and 30mg.
The diameter sucking ingot is about 10mm, its lactose containing 115mg and the vitamin C of 115mg.
Acquired results, as shown in following table ten.
Table ten:
aWith tongue touch feeling preparation resolution time
bWith tongue touch feeling preparation resolution time
cSome particles is swallowed with saliva
Embodiment eight:
In this embodiment, test the dosage form of several different oral cavity release active substance, compare the time length that in the absorption rate of its active substance and blood, valid density maintains.Active substance used herein is Verdoflavin, so vitamin B residence time in vivo can be learnt by the color of urine.
Experimental group is the solid-state molten ingot of soft mouth, and its used carrier is sponge line grain or the microsphere of Verdoflavin compound recipe.The solid-state molten ingot of soft mouth of every 450mg contains the Verdoflavin of 25mg.
The preparation method of above-mentioned Verdoflavin compound recipe sponge line grain is as described below.First Verdoflavin and Sucralose being dissolved among the glyceride of 60-70 DEG C, Verdoflavin, Sucralose are 50:5:45 with the weight ratio of glyceride, and gross weight is 500g.Uniformly after mixing, allow mixture quickly cool down, form thin piece of yellow.Thin piece of gained yellow crosses No. 40 sieves after pulverizing with pulverizer, and obtains yellow fine powder.Then, allowing yellow fine powder and glycine mix, the weight ratio of yellow fine powder and glycine is 3:7.Then extrude add the 10wt% distilled water of raw material gross weight with single screw extrusion machine after, be placed in proof cabinet after drying in the shade about 48 hours, form the sponge line grain containing Verdoflavin (15wt%).
The preparation method of above-mentioned Verdoflavin compound recipe microsphere is as described below.It is the Verdoflavin of 50:5:40:5, Sucralose, microcrystalline Cellulose, hydroxypropyl methyl cellulose mixing by weight ratio, is dried after extrusion spheronization, forms Verdoflavin compound recipe microsphere.
Matched group is sublingual absorption capsule and mouth collapses ingot.Sublingual absorption capsule is No. 3 capsules, has 6 holes that diameter is about 0.67mm.Each capsule charge has the Verdoflavin compound recipe sponge line grain of 230mg, wherein contains the Verdoflavin of 25mg.Above-mentioned mouth collapse ingot be mixed by the Verdoflavin preparation (glyceride and the mixture of Verdoflavin) of 230mg, 30mg sodium starch glycollate and 40mg lactose after play ingot and form.A diameter of 10mm of ingot sheet, thickness is 2.5mm, and hardness is about 4H.
Method of testing, for allowing same people, when the morning 9 of different five days, is first drunk 300mL drinking water, then is taken the Verdoflavin of the various peroral dosage forms of experimental example 3-1 to 3-5 respectively.Then, urine color is tested in different time points (09:00,09:15,09:30,10:30,13:00 and 15:00).
Urine is to compare in color method, and the standard substance in color method please be shown in Table 11.The urine of 09:00 when wherein standard substance E is not take Verdoflavin, and standard substance A～D is standard substance E adds made by different amounts of Verdoflavin.And according to the color of standard substance listed by table 11, gained urine test result asks for an interview table below 12.
Table 11: urine is the standard of comparison of color method
| In colour standard | A | B | C | D | E |
| Verdoflavin (ppm) | 10 | 1 | 0.1 | 0.01 | 0 |
Table 12:
From the result of table 12 above, taking mouth and collapse ingot and carrier is the soft mouth of the solid-state molten ingot person of microsphere, its urine just started at 90 minutes to turn yellow, display Verdoflavin many by intestinal absorption after, just metabolism discharging via kidney.And take sublingual absorption capsule and the soft mouth of solid-state molten ingot person that carrier is instant capacity sponge line grain, its urine began at 15-30 minute turn yellow.Both displays are by sublingual mucosal absorption, enter blood circulation soon, so the speed discharged by kidney is very fast.
From the foregoing, the active substance being dissolved in saliva can act locally on oral cavity, or absorbed by oral mucosa (including cheeks mucosa, hypoglossis mucous membrane and vestibule of mouth) further.Had the advantage that by oral mucosal absorption active substance, such as can just produce onset effect (onset) within 5 minutes, the valid density in blood and the highest blood level can be reached with less taking dose, systemic circulation can be put into without the first-pass metabolism of liver and small intestinal and produce pharmacological action, the decomposition of gastric acid and intestines and stomach digestive enzyme and digestion can be required no and cause deactivation, and after absorption can directly via the superior vena cava system transfer such as jugular vein be recycled to during heart, brain, lungs and skin etc. organize.
Although this utility model is disclosed above with embodiment; so it is not limited to this utility model; any it is familiar with this those skilled in the art; without departing from spirit and scope of the present utility model; when being used for a variety of modifications and variations, protection domain the most of the present utility model is when being as the criterion depending on the defined person of appended claims.
Claims (3)
1. the solid-state molten ingot of soft mouth containing many units carrier, including:
Soft sweet core；
Shell, is coated with described soft sweet core；And
For carrying multiple carriers of at least one active substance, being distributed in described soft sweet core, described shell or a combination thereof, wherein said active substance is for having bioactive solid-state or liquid.
2. the solid-state molten ingot of soft mouth as claimed in claim 1, wherein said carrier is microgranule, microsphere, sponge line grain, drop pill or above-mentioned combination in any.
3. the solid-state molten ingot of soft mouth as claimed in claim 1, wherein said carrier there is coating at least partially.
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