CN104383547B - Herba Saussureae Involueratae extract phosphatide complexes, oral disnitegration tablet and preparation method thereof - Google Patents
Herba Saussureae Involueratae extract phosphatide complexes, oral disnitegration tablet and preparation method thereof Download PDFInfo
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- CN104383547B CN104383547B CN201410423744.4A CN201410423744A CN104383547B CN 104383547 B CN104383547 B CN 104383547B CN 201410423744 A CN201410423744 A CN 201410423744A CN 104383547 B CN104383547 B CN 104383547B
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Abstract
The present invention relates to Herba Saussureae Involueratae extract technical field, is a kind of Herba Saussureae Involueratae extract phosphatide complexes, oral disnitegration tablet and preparation method thereof；The Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet, raw materials by weight portion include Herba Saussureae Involueratae extract phosphatide complexes, disintegrant, filler, adhesive, lubricant and flavouring；Organic solvent-free remains in Herba Saussureae Involueratae extract phosphatide complexes, and bioavilability is high, physical property and chemical property are relatively stable；The Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention that is obtained by Herba Saussureae Involueratae extract phosphatide complexes is convenient to take, it is rapid to work, the compliance of patient is improved simultaneously, Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention has good anti-inflammatory, analgesic activity, is used to treat rheumatism for it and rheumatoid arthritis provides pharmacology foundation.
Description
Technical field
The present invention relates to Herba Saussureae Involueratae extract technical field, is a kind of Herba Saussureae Involueratae extract phosphatide complexes, oral cavity
Disintegrated tablet and preparation method thereof.
Background technology
1st, phosphatide complexes progress and background introduction
Phosphatide complexes are found that early stage phosphatide is compound by Italian scholar Bombardelli when studying liposome
The medicine that thing research is related to is flavones or polyphenol components containing phenolic hydroxyl group mostly, and the later stage more studies confirmation, except phenol hydroxyl
Outside base, some alcoholic extract hydroxyl groups, amide groups or carbonyl isopolarity group are possible to and phosphatide or other matrix materials（As cholesterol,
Sodium taurocholate etc.）Water-wet side compound orbicule is formed by interactions such as intermolecular hydrogen bonding or Van der Waals forces.Whether it is close
Aqueous pharmaceutical or lipophilic drugs, as long as containing polar group that can be compound, it can all form lipid complex.
Phosphatide complexes are mostly unformed and micella can be formed in water, therefore can increase the water solubility of parent drug, and right
The fat-soluble increase of parent drug is then the stronger interaction in the polar group part of parent drug and phosphatide, is suppressed in molecule
Singly-bound freely rotates, and two long aliphatic chains of phosphatide are not involved in recombination reaction, can move freely, and has wrapped up the polarity of phosphatide
Part forms a lipophilic surface, shows phosphatide complexes stronger fat-soluble.Meanwhile phosphatide complexes are that class is thin
Born of the same parents' structure, therefore have certain compatibility to cell membrane, enhance the membrane permeability of medicine.Therefore, phosphatide complexes have good
Good developmental research prospect, for improving the development and utilization of natural drug and new Chinese medicine, accelerating showing for traditional Chinese medicine compound preparation
Generationization process, Chinese medicine preparation technical merit and clinical application quality are improved, is respectively provided with important theoretical and practical significance.
2nd, Herba Saussureae Involueratae preparation research background and the defects of prior art
Herba Saussureae Involueratae is the important medicinal plant of China western part alpine region, is the conventional one kind of Tibetan medicine Mongolian medicine Uygur medicine
Ethnic drug, its " warm-natured, slight bitter, function of expelling wind and eliminating dampness " is first appeared in Tibetan medicine document《Month king medicine is precious》, in the Qing Dynasty《Compendium of Materia Medica picks up
Lose》And《Chinese Herbal Medicine in Xinjiang》Also it is on the books.Xinjiang of China Tianshan Mountains and the band of Kun Lun Mountain one are distributed mainly on, is grown in more than snow line.
It is among the people warm-natured, mildly bitter flavor, to enter liver,spleen,kidney three and pass through with all herbal medicine, the work(such as there is warming kidney and enhancing yang, expelling wind and eliminating dampness, restore menstrual flow and invigorate blood circulation
Can, for treating the diseases such as rheumatism numbness pain, rheumatoid arthritis, cold and pain in the lower abdomen, irregular menstruation.Due to its important medicinal valency
Value, turn into the object that people pay close attention to and studied always for many years.
Saussurea involucrata is conducted in-depth research both at home and abroad, Phenylpropanoid Glycosides, flavones, alkaloid, terpene, interior are mainly contained in saussurea involucrata
Ester, polysaccharide, volatile oil chemical composition, modern pharmacology experiment show that flavones, Phenylpropanoid Glycosides are the work of main anti-inflammatory and antalgic in saussurea involucrata
Property composition.
Standard No. is to have recorded its preparation method in WS3-B-3334-98 Herba Saussureae Involueratae injection：Pass through 14 days alcohol dippings
Extracted, in the standing by 1 month to 3 months, separate the impurity of some macromoleculars.This method to a certain extent can
Active ingredient in extraction separation saussurea involucrata, but the required production cycle is oversize, and for the producer, this operation is brought very
Burden, therefore, it is the problem that medical personal needs to face that new, the short time extraction separation method is invented in research.
Publication No. CN1634508A, the patent document of entitled " Saussurea involucrata drop pill and preparation method thereof " are disclosed only in
Medicine is into based on square saussurea involucrata oral liquid extraction process, and with reference to dripping pill, preparation technology is prepared.Although employ alcohol reflux to carry
Take, shorten extraction time, but extract is not further purified, and without clear and definite efficient liquid phase Con trolling index.
Publication No. CN1500500A, entitled " a kind of saussurea involucrata freeze drying powder injection for being used to be injected intravenously and its preparation side
The patent document of method " discloses following method：" extracted with suitable solvent, then with different adsorption column separations ", the party
Method is brief introduction, do not point out solvent used why solvent, how adsorption column used to operate, therefore,
Can not be replicated in actual production process, and the patent only active ingredient general flavone is defined, limit scope as 5mg extremely
20mg, highest with minimum poor 4 times, scope is wider, and to another active ingredient Phenylpropanoid Glycosides class of saussurea involucrata progress content restriction.
Publication No. CN1686357A, the patent document of entitled " a kind of Saussurea involucrate powder injection and preparation method thereof " disclose
Following method：" active component is obtained from Chinese medicine saussurea involucrata extraction purification, controls general flavone（In terms of rutin, Syringin）, control is always
Alkaloid（In terms of colchicum）", this control method is less reasonable：1. rutin belongs to flavonoids from compound structure, and
Syringin belongs to Phenylpropanoid Glycosides class, and the Phenylpropanoid Glycosides active component chlorogenic acid for also having another content higher in saussurea involucrata is not controlled
System.2. consulting the document about Herba Saussureae Involueratae both at home and abroad, the isolated colchicin Structural Identification from Herba Saussureae Involueratae there are no
Report, with HPLC multi-methods measure also do not detect colchicin, the patent does not conform to by blank determination total alkali of colchicin
Reason.3. the content of total alkali is little in document report saussurea involucrata, using fluorescence spectrophotometer light method measurement system error itself with regard to larger.
Publication No. CN101209274 B are disclosed " a kind of Saussurea involucrata extract and its production method ", but the non-pin of the patent
To the dissolution properties of active component in Saussurea involucrata extract, there is provided a kind of medicament for increasing active ingredient solubility in Saussurea involucrata extract
Method, meanwhile, also without for active component drug action in Saussurea involucrata extract, there is provided one kind meets that Saussurea involucrata extract is transdermal
The formulation of administration.
Publication No. CN101890067A discloses " a kind of anti-inflammatory and analgesic snow lotus gel and preparation method thereof ", is to avenge
Lotus extract mixes with suitable water gelling agent matrix, a kind of exterior-applied formulation sticked for skin.But snow lotus gel moderate snow
Lotus extract is to be dispersed in the form of suspension in matrix, rather than to be dissolved in medicine water-based by increasing the solubility of medicine
In gel substrate, therefore, medicine it is transdermal very limited, and the transdermal of extract need to be realized by adding transdermal enhancer.
Publication No. CN101209274 A disclose " a kind of production method of saussurea involucrata catablasm ", are by Saussurea involucrata extract
Shaping in catablasm base material is dispersed in be prepared, it is transdermal to realize, skin penetration enhancer is also added in molding formula.
Publication No. CN102349939 A disclose " a kind of Saussurea involucrate extractive microemulsion compound ", are to extract saussurea involucrata
Thing is dispersed in aqueous phase and oil phase, is added emulsifying agent and assistant for emulsifying agent and is made, micro emulsion can increase medicine as cutaneous penetration carrier
The solubility of thing.
Publication No. CN102349939 A disclose " a kind of production method of Saussurea involucrata extract carrier ", and saussurea involucrata is carried
Take in the molten ethanol of thing, phosphatide, surfactant and form organic phase；Aqueous phase is phosphate buffer, and organic phase is injected in aqueous phase
Stirring forms transparent system, and carrier is a kind of preferable percutaneous penetration of drugs carrier of transdermal effect.
Herba Saussureae Involueratae injection made of Herba Saussureae Involueratae folk prescription, it is evident in efficacy although drug administration by injection is rapid-action.But snow lotus injection agent
Have serious muscle irritation, exist injection site pain, redness, it is inconvenient for use the shortcomings of, patient compliance is poor.In order that
Saussurea involucrata preferably plays clinical efficacy, and clinically there is an urgent need to a kind of new system safe, easy to use and compliance is good
Agent.
In summary, existing Herba Saussureae Involueratae extract dissolubility is poor, is not easy to be absorbed in the gastrointestinal tract so as to cause to give birth to
Thing availability is low, it is impossible to gives full play to its drug action；Existing Herba Saussureae Involueratae preparation is mostly external preparation and injection, is suffered from
Person takes poor compliance；And Herba Saussureae Involueratae extract dissolubility can be improved, and can improves the Tianshan Mountains snow that patient takes compliance
Lotus extract formulation is up for research and development.
The content of the invention
The invention provides a kind of Herba Saussureae Involueratae extract phosphatide complexes, oral disnitegration tablet and preparation method thereof, overcome
The deficiency of above-mentioned prior art, it is poor that it can effectively solve existing Herba Saussureae Involueratae extract dissolubility, be not easy in the gastrointestinal tract by
Absorb so as to causing bioavilability low, it is impossible to give full play to its drug action and the problem of patient takes poor compliance.
One of technical scheme is realized by following measures：A kind of Herba Saussureae Involueratae extract phosphatide is compound
Thing, obtain as follows：The first step, appropriate Herba Saussureae Involueratae extract and phosphatide is taken to be placed in container, phosphatide and Herba Saussureae Involueratae
The mass ratio of extract is 1:1 to 1:3, then added by 1mg into 30mg Herba Saussureae Involueratae extracts based on 1ml organic solvent As, to
Added in container after organic solvent A mixes and obtain the first mixed liquor；Second step, the first mixed liquor is placed into constant temperature in a water bath and stirred
Mix 0.5 hour to 2 hours, then obtain the second mixed liquor after water-bath vacuum rotary steam removes organic solvent A；3rd step, is pressed
1.5mg adds 1ml organic solvent B meters into 3.75mg Herba Saussureae Involueratae extracts, and organic solvent B is added into the second mixed liquor and is mixed
Filtrate is obtained after even and filtering；4th step, the relative density that filtrate is concentrated into when temperature is 20 DEG C through water-bath vacuum rotary steam are
1.31 to 1.34, then it is less than or equal to 5% through low-temperature vacuum drying to quality single-detector, obtains Herba Saussureae Involueratae extract phosphorus
Fat complexes.
Here is the further optimization and/or improvements to one of foregoing invention technical scheme：
Above-mentioned phosphatide is natural phospholipid or synthetic phospholipid；Or/and organic solvent A is methanol, ethanol, ethyl acetate and just
One or more of hexane；Or/and organic solvent B is one or more of chloroform, dichloromethane, n-hexane or ether；
Or/and Herba Saussureae Involueratae extract is Patent No. ZL 200710203380.9, entitled " Saussurea involucrata extract and its producer
Saussurea involucrata extract in method ".
Above-mentioned natural phospholipid is soybean lecithin；Or/and in second step, bath temperature is 30 DEG C to 40 DEG C, stir speed (S.S.) is
2000 revs/min to 3000 revs/min；Or/and in second step and the 4th step, the temperature of water-bath vacuum rotary steam is 30 DEG C to 40
DEG C, the pressure of water-bath vacuum rotary steam is -0.08MPa；Or/and the 4th in step, the temperature of low-temperature vacuum drying is 30 DEG C to 60
℃。
The two of technical scheme are realized by following measures：A kind of Herba Saussureae Involueratae extract phosphatide is compound
The preparation method of thing, carry out as follows：The first step, appropriate Herba Saussureae Involueratae extract and phosphatide is taken to be placed in container, phosphatide
Mass ratio with Herba Saussureae Involueratae extract is 1:1 to 1:3, it is organic that 1ml is then added into 30mg Herba Saussureae Involueratae extracts by 1mg
Solvent orange 2 A meter, added into container after organic solvent A mixes and obtain the first mixed liquor；Second step, the first mixed liquor is placed on water
Constant temperature stirs 0.5 hour to 2 hours in bath, then obtains the second mixed liquor after water-bath vacuum rotary steam removes organic solvent A；The
Three steps, add based on 1ml organic solvent Bs, added into the second mixed liquor organic into 3.75mg Herba Saussureae Involueratae extracts by 1.5mg
Solvent B is mixed and is obtained filtrate after filtering；4th step, filtrate are concentrated into relative when temperature is 20 DEG C through water-bath vacuum rotary steam
Density is 1.31 to 1.34, is then less than or equal to 5% through low-temperature vacuum drying to quality single-detector, obtains Herba Saussureae Involueratae and carry
Take thing phosphatide complexes.
Here is two further optimization and/or improvements to foregoing invention technical scheme：
Above-mentioned phosphatide is natural phospholipid or synthetic phospholipid；Or/and organic solvent A is methanol, ethanol, ethyl acetate and just
One or more of hexane；Or/and organic solvent B is one or more of chloroform, dichloromethane, n-hexane or ether；
Or/and Herba Saussureae Involueratae extract is Patent No. ZL 200710203380.9, entitled " Saussurea involucrata extract and its producer
Saussurea involucrata extract in method ".
Above-mentioned natural phospholipid is soybean lecithin；Or/and in second step, bath temperature is 30 DEG C to 40 DEG C, stir speed (S.S.) is
2000 revs/min to 3000 revs/min；Or/and in second step and the 4th step, the temperature of water-bath vacuum rotary steam is 30 DEG C to 40
DEG C, the pressure of water-bath vacuum rotary steam is -0.08MPa；Or/and the 4th in step, the temperature of low-temperature vacuum drying is 30 DEG C to 60
℃。
The three of technical scheme are realized by following measures：A kind of oral disnitegration tablet, raw material is by weight
Number include 20 parts to 30 parts of Herba Saussureae Involueratae extract phosphatide complexes, 6 parts to 16 parts of disintegrant, 35 parts to 60 parts of filler,
1 part to 3 parts of 1 part to 5 parts of adhesive, 0.5 part to 1 part of lubricant and flavouring；The Herba Saussureae Involueratae extract phosphatide complexes mouth
Cavity disintegrating tablet obtains as follows：By the desired amount of Herba Saussureae Involueratae extract phosphatide complexes, filler and disintegrant gross weight
The 1/2 of amount obtains mixture after mixing, and adds after the desired amount of adhesive mixes and is pelletized in the mixture, through dry after granulation
Whole grain after dry, the 1/2 of the desired amount of lubricant, flavouring and disintegrant gross weight is added after whole grain and is well mixed, tabletting
After obtain Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet.
Here is three further optimization and/or improvements to foregoing invention technical scheme：
Above-mentioned disintegrant is low-substituted hydroxypropyl cellulose, PVPP, sodium carboxymethyl starch, crosslinking carboxylic
One or more of sodium carboxymethylcellulose pyce, super sodium carboxymethyl starch；Or/and filler is microcrystalline cellulose, lactose, sweet dew
One or more of alcohol, soluble starch；Or/and lubricant is magnesium stearate, superfine silica gel powder, talcum powder and hard fumaric acid
One or more of sodium；Flavouring is one or more of Aspartame, honey element and stevioside；Adhesive is percent by volume
One or more of ethanol water and polyvinylpyrrolidone alcohol mixeding liquid for 90% to 95%, wherein：Polyvinyl pyrrole
Alkanone alcohol mixeding liquid obtains as follows：Count in parts by weight, by 1 part to 5 parts of polyvinylpyrrolidone and 97 parts extremely
The ethanol water that 99 parts of percents by volume are 95% obtains polyvinylpyrrolidone alcohol mixeding liquid after mixing；Or/
With particle diameter after granulation is 0.5 millimeter to 1 millimeter；Or/and drying temperature be 45 DEG C to 55 DEG C, drying time be 0.5h extremely
2h。
The four of technical scheme are realized by following measures：A kind of preparation method of oral disnitegration tablet,
Raw materials by weight portion includes 20 parts to 30 parts of Herba Saussureae Involueratae extract phosphatide complexes, 6 parts to 16 parts of disintegrant, filler 35
Part to 1 part to 3 parts of 60 parts, 1 part to 5 parts of adhesive, 0.5 part to 1 part of lubricant and flavouring；The Herba Saussureae Involueratae extract phosphatide
The preparation method of compound oral disnitegration tablet is carried out as follows：By the desired amount of Herba Saussureae Involueratae extract phosphatide complexes,
Mixture is obtained after 1/2 mixing of filler and disintegrant gross weight, after adding the desired amount of adhesive mixing in the mixture
Pelletized, whole grain after drying after granulation, add the desired amount of lubricant, flavouring and disintegrant gross weight after whole grain
1/2 and it is well mixed, Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet is obtained after tabletting.
Here is four further optimization and/or improvements to foregoing invention technical scheme：
Above-mentioned disintegrant is low-substituted hydroxypropyl cellulose, PVPP, sodium carboxymethyl starch, crosslinking carboxylic
One or more of sodium carboxymethylcellulose pyce, super sodium carboxymethyl starch；Or/and filler is microcrystalline cellulose, lactose, sweet dew
One or more of alcohol, soluble starch；Or/and lubricant is magnesium stearate, superfine silica gel powder, talcum powder and hard fumaric acid
One or more of sodium；Flavouring is one or more of Aspartame, honey element and stevioside；Adhesive is percent by volume
One or more of ethanol water and polyvinylpyrrolidone alcohol mixeding liquid for 90% to 95%, wherein：Polyvinyl pyrrole
Alkanone alcohol mixeding liquid obtains as follows：Count in parts by weight, by 1 part to 5 parts of polyvinylpyrrolidone and 97 parts extremely
The ethanol water that 99 parts of percents by volume are 95% obtains polyvinylpyrrolidone alcohol mixeding liquid after mixing；Or/
With particle diameter after granulation is 0.5 millimeter to 1 millimeter；Or/and drying temperature be 45 DEG C to 55 DEG C, drying time be 0.5h extremely
2h。
Organic solvent-free remains in Herba Saussureae Involueratae extract phosphatide complexes, bioavilability height, physical property and chemistry
Property is relatively stable；The Herba Saussureae Involueratae extract phosphatide complexes of the present invention obtained by Herba Saussureae Involueratae extract phosphatide complexes
Oral disnitegration tablet is convenient to take, action is rapid, while improves the compliance of patient, and Herba Saussureae Involueratae extract phosphatide of the present invention is answered
Compound oral disnitegration tablet has good anti-inflammatory, analgesic activity, is used to treat rheumatism for it and rheumatoid arthritis provides
Pharmacology foundation.
Embodiment
The present invention is not limited by following embodiments, can technique according to the invention scheme and actual conditions it is specific to determine
Embodiment.
Embodiment 1, the Herba Saussureae Involueratae extract phosphatide complexes, is obtained by following preparation methods：The first step, take appropriate day
Mountain Saussurea involucrata extract and phosphatide are placed in container, and the mass ratio of phosphatide and Herba Saussureae Involueratae extract is 1:1 to 1:3, then by 1mg
1ml organic solvent A meters are added into 30mg Herba Saussureae Involueratae extracts, is added into container after organic solvent A mixes and obtains first
Mixed liquor；Second step, the first mixed liquor is placed into constant temperature in a water bath and stirred 0.5 hour to 2 hours, then depressurizes and revolves through water-bath
Boil off and obtain the second mixed liquor after removing organic solvent A；3rd step, 1ml is added into 3.75mg Herba Saussureae Involueratae extracts by 1.5mg
Organic solvent B meter, into the second mixed liquor, addition organic solvent B mixes and obtains filtrate after filtering；4th step, filtrate is through water-bath
The relative density that vacuum rotary steam is concentrated into when temperature is 20 DEG C is 1.31 to 1.34, then through low-temperature vacuum drying to quality hundred
Divide water content to be less than or equal to 5%, obtain Herba Saussureae Involueratae extract phosphatide complexes.Container can be ground round-bottomed flask.
Embodiment 2, the Herba Saussureae Involueratae extract phosphatide complexes, is obtained by following preparation methods：The first step, take appropriate day
Mountain Saussurea involucrata extract and phosphatide are placed in container, and the mass ratio of phosphatide and Herba Saussureae Involueratae extract is 1:1 or 1:3, then by 1mg
Or 1ml organic solvent A meters are added in 30mg Herba Saussureae Involueratae extracts, added into container after organic solvent A mixes and obtain first
Mixed liquor；Second step, the first mixed liquor is placed into constant temperature in a water bath and stirred 0.5 hour or 2 hours, then depressurizes and revolves through water-bath
Boil off and obtain the second mixed liquor after removing organic solvent A；3rd step, by adding 1ml in 1.5mg or 3.75mg Herba Saussureae Involueratae extracts
Organic solvent B meter, into the second mixed liquor, addition organic solvent B mixes and obtains filtrate after filtering；4th step, filtrate is through water-bath
The relative density that vacuum rotary steam is concentrated into when temperature is 20 DEG C is 1.31 or 1.34, then through low-temperature vacuum drying to quality hundred
Divide water content to be less than or equal to 5%, obtain Herba Saussureae Involueratae extract phosphatide complexes.Container can be ground round-bottomed flask.
Embodiment 3, as the optimization of above-described embodiment, phosphatide is natural phospholipid or synthetic phospholipid in embodiment 3；Or/and
Organic solvent A is one or more of methanol, ethanol, ethyl acetate and n-hexane；Or/and organic solvent B be chloroform,
One or more of dichloromethane, n-hexane or ether；Or/and Herba Saussureae Involueratae extract is Patent No. ZL
200710203380.9, the Saussurea involucrata extract in entitled " Saussurea involucrata extract and its production method ".
Embodiment 4, as the optimization of above-described embodiment, natural phospholipid is soybean lecithin in embodiment 4；Or/and second step
In, bath temperature is 30 DEG C to 40 DEG C, and stir speed (S.S.) is 2000 revs/min to 3000 revs/min；Or/and second step and the 4th
In step, the temperature of water-bath vacuum rotary steam is 30 DEG C to 40 DEG C, and the pressure of water-bath vacuum rotary steam is -0.08MPa；Or/and the 4th step
In, the temperature of low-temperature vacuum drying is 30 DEG C to 60 DEG C.
Embodiment 5, the Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet, raw materials by weight portion are avenged including Tianshan Mountains
20 parts to 30 parts of lotus extract phosphatide complexes, 6 parts to 16 parts of disintegrant, 35 parts to 60 parts of filler, 1 part to 5 parts of adhesive,
1 part to 3 parts of 0.5 part to 1 part of lubricant and flavouring；The Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet presses following systems
Preparation Method obtains：After the 1/2 of the desired amount of Herba Saussureae Involueratae extract phosphatide complexes, filler and disintegrant gross weight is mixed
Mixture is obtained, adds after the desired amount of adhesive mixes and is pelletized in the mixture, whole grain after drying after granulation, whole grain
The 1/2 of the desired amount of lubricant, flavouring and disintegrant gross weight is added afterwards and is well mixed, and Herba Saussureae Involueratae is obtained after tabletting
Extract phosphatide complexes oral disnitegration tablet.Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention is complete in 40s
Full disintegration, 2 min dissolution rates are up to more than 85%, 10min dissolutions up to 90%；Herba Saussureae Involueratae extract phosphatide complexes of the present invention
Oral disnitegration tablet drug content can be 50mg/ pieces to 75mg/ pieces.
Embodiment 6, the Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet, raw materials by weight portion are avenged including Tianshan Mountains
20 parts or 30 parts of lotus extract phosphatide complexes, 6 parts or 16 parts of disintegrant, 35 parts or 60 parts of filler, 1 part or 5 parts of adhesive,
0.5 part or 1 part of lubricant, 1 part or 3 parts of flavouring；The Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet presses following systems
Preparation Method obtains：After the 1/2 of the desired amount of Herba Saussureae Involueratae extract phosphatide complexes, filler and disintegrant gross weight is mixed
Mixture is obtained, adds after the desired amount of adhesive mixes and is pelletized in the mixture, whole grain after drying after granulation, whole grain
The 1/2 of the desired amount of lubricant, flavouring and disintegrant gross weight is added afterwards and is well mixed, and Herba Saussureae Involueratae is obtained after tabletting
Extract phosphatide complexes oral disnitegration tablet.Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention is complete in 40s
Full disintegration, 2 min dissolution rates are up to more than 85%, 10min dissolutions up to 90%；Herba Saussureae Involueratae extract phosphatide complexes of the present invention
Oral disnitegration tablet drug content can be 50mg/ pieces to 75mg/ pieces.
Embodiment 7, as the optimization of above-described embodiment, disintegrant is low-substituted hydroxypropyl cellulose, crosslinking in embodiment 7
One or more of polyvinylpyrrolidone, sodium carboxymethyl starch, Ac-Di-Sol, super sodium carboxymethyl starch；
Or/and filler is one or more of microcrystalline cellulose, lactose, mannitol, soluble starch；Or/and lubricant is hard
One or more of fatty acid magnesium, superfine silica gel powder, talcum powder and hard fumaric acid sodium；Flavouring is Aspartame, honey element and sweet tea
One or more of synanthrin；Adhesive is the ethanol water that percent by volume is 90% to 95% and polyvinylpyrrolidone ethanol
One or more of mixed liquor, wherein：Polyvinylpyrrolidone alcohol mixeding liquid obtains as follows：Count in parts by weight,
After the ethanol water that 1 part to 5 parts of polyvinylpyrrolidone and 97 parts to 99 parts percents by volume are 95% is mixed
Obtain polyvinylpyrrolidone alcohol mixeding liquid；Or/and the particle diameter after granulation is 0.5 millimeter to 1 millimeter；Or/and dry temperature
Spend for 45 DEG C to 55 DEG C, drying time is 0.5h to 2h.
Early stage pilot study of the organic solvent to medicine in the above embodiment of the present invention
Influence of 1.1 organic solvents to pharmaceutical chemistry property is investigated
In previous research work, it is to solubility of the Saussurea involucrata extract in nonpolar low boiling point organic solvent
General examination for students from various schools is examined, according to the method for approximate solubility in the pharmacopeia note on the use：Take Saussurea involucrata extract fine powder appropriate, be placed in 25 DEG C ± 2 DEG C necessarily
In the solvent of capacity, every strength shaking in 5 minutes 30 seconds；The dissolving situation in 30 minutes is observed, such as invisible particles of solute
Or during drop, that is, it is considered as and is completely dissolved；As a result show Saussurea involucrata extract be easily soluble in methanol, 75% ethanol, acetone, n-octyl alcohol, 1,
In 4-dioxane, ethyl acetate, insoluble in n-hexane and chloroform.Meanwhile using chlorogenic acid, rutin as index, use
HPLC determines Saussurea involucrata extract in water, methanol, 75% ethanol, acetone, n-octyl alcohol, 1, the dissolving of 4-dioxane, ethyl acetate
Degree, specific method are as follows：Take excessive Saussurea involucrata extract be separately added into the water equipped with 10mL, methanol, 75% ethanol, acetone, 1,4-
In 7 25 mL conical flasks of dioxane, n-octyl alcohol and ethyl acetate, and ultrasound is divided untill Saussurea involucrata extract no longer dissolves
37 are put into after not sealed with sealed membrane（± 2）In DEG C thermostatic control oscillator vibration, 48 h are shaken, taper is kept in whole process
Bottle is with the presence of solid drugs, and suspension is in 6000 rmin-1Under the conditions of centrifuge 15min, supernatant crosses 0. 45 μm of micropores filters
Film, chlorogenic acid, rutin content are determined with HPLC after the certain multiple of subsequent filtrate methanol dilution, calculate Saussurea involucrata extract in each Jie
Equilbrium solubility in matter.As a result show Saussurea involucrata extract water, methanol, 75% ethanol, acetone, 1, it is 4-dioxane, just pungent
Alcohol, the solubility of ethyl acetate reduce successively.
1.2 investigation using methanol as double solvents
Using methanol as solvent, drug quality concentration is set as 10mg/ml, the score that feeds intake of soybean lecithin and Saussurea involucrata extract
Wei 1:1、1:2、1:2.5、1:3（w/w）.Herba Saussureae Involueratae extract and soybean lecithin are placed in ground round-bottomed flask, added
Methanol obtains mixed liquor after mixing, constant temperature water bath stirring, be evaporated under reduced pressure and remove organic solvent, obtain Herba Saussureae Involueratae extract phosphatide
Compound semi-finished product, add n-hexane, Herba Saussureae Involueratae extract phosphatide complexes semi-finished product is fully dissolved, miillpore filter mistake
Filter, filtrate decompression are distilled to recover n-hexane, low-temperature vacuum drying, produce Herba Saussureae Involueratae extract phosphatide complexes of the present invention.With
The evaluation index of chlorogenic acid and rutin recombination rate as I phosphatide complexes preparation technology.
The purpose of the present invention, it is the suitable complex solvent system of selection, improves the compound of Herba Saussureae Involueratae extract and phosphatide
Efficiency and quality stability.Selected solvent system can meet following condition simultaneously：1）Phosphatide and Herba Saussureae Involueratae extract are all
The solution to form clear can be dissolved；2）Moisture-free in system, polarity is small, is advantageous to phosphatide and Herba Saussureae Involueratae extract
It is intermolecular compound；3）Solvent system evaporation efficiency is high, easily waves and removes, organic solvent-free residual；4）Preparation process central Tianshan saussurea involucrata
Extract property is stable.
Recombination rate is determined according to following method
Recombination rate（Envelop rate）：Using Herba Saussureae Involueratae extract phosphatide complexes of the present invention in n-hexane it is readily soluble, and swim
From feature of the Herba Saussureae Involueratae extract insoluble in n-hexane, recombination rate measure is carried out.
A certain amount of Herba Saussureae Involueratae extract and soybean lecithin are weighed, is placed in by a certain percentage in 100mL ground round-bottomed flasks,
It is appropriate to add methanol, puts in 40 DEG C of water-baths and fully dissolves, after stirring 2h under constant temperature, is evaporated under reduced pressure except dereaction is molten
Agent.Appropriate anti-solvent n-hexane is added after residue vacuum drying to be completely dissolved, is filtered with 0.45 μm of miillpore filter, and it is heavy to collect
Form sediment.（It is precipitated as the i.e. unreacted Herba Saussureae Involueratae extract of n-hexane insoluble matter and impurity）.Filtrate decompression is distilled, 40 DEG C of temperature,
Under constant temperature, vacuum drying, weigh and produce phosphatide complexes.The initial dosage of Herba Saussureae Involueratae extract（M1）With precipitation
Amount（M2）Difference be Herba Saussureae Involueratae extract phosphatide complexes amount, it is compound so as to calculate chlorogenic acid recombination rate and rutin
Rate, calculation formula are as follows：
Recombination rate is calculated as follows：Recombination rate %=(M1-M2)/M1×100%
Chlorogenic acid, Assaying of Rutin method
The preparation of reference substance solution：Take chlorogenic acid appropriate with control substance of Rutin, it is accurately weighed, put in 10ml brown measuring bottles,
It is the μ gmL of chlorogenic acid 454.5 to add methanol to be configured to mass concentration-1, the μ gmL of rutin 629.9-1Mixing storing solution, precision inhale
Take storing solution 5mL to put in 50mL brown measuring bottles, add methanol dilution to produce the μ gmL of chlorogenic acid 45.45 to scale-1, rutin 62.99
μg·mL-1Mixed reference substance solution, shake up, filtered through 0.45 μm of filter membrane, it is standby.
The preparation of need testing solution：Precision weighs Herba Saussureae Involueratae extract 10mg, is placed in 10mL measuring bottles, adds methanol dilution
To scale, shake up, filter, produce through 0.45 μm of filter membrane.
Chromatographic condition：According to《Chinese Pharmacopoeia》Versions in 2010 and the assay side of bibliography Content of Chlorogenic Acid and rutin
Method, experiment sieving simultaneously determine chromatographic condition：Chromatographic column is Kromasil C18 posts（250 mm × 4.6 mm, 0.5 μm）, mobile phase
For the phosphoric acid solution (B) of acetonitrile (A) -0.4% [0-13min 12% (A), 13-16min 12% (A) -15% (A), 16-50min 15%
(A)] gradient elution, Detection wavelength 353nm, column temperature are 35 DEG C, and flow velocity is 1 mLmin-1, sample size is 10 μ L；By above-mentioned
Chromatographic condition is measured, and the retention time of chlorogenic acid is 9.1min, and the retention time of rutin is 26.1min.
Linear relationship is investigated：With the mixed reference substance solution configured, precision draws 0.5,1.0,2.0,5.0,8.0,
10mL is to 10mL brown measuring bottles, and with methanol dilution constant volume, it is 2.273~45.45 μ gmL to shake up obtained chlorogenic acid concentration-1, reed
Fourth concentration is 3.15~62.99 μ gmL-1Serial solution, draw 10 μ L sample introductions.With reference substance concentration X (μ gmL-1) it is horizontal stroke
Coordinate, peak area Y are ordinate, draw chlorogenic acid and the standard curve of rutin, carry out linear regression, obtain the recurrence side of chlorogenic acid
Journey is Y=16942x+5077.5, r=0.9996；The regression equation of rutin is Y=25029x+7246.6, r=0.9998.Knot
Fruit shows that chlorogenic acid is in 2.273~45.45 μ gmL-1In the range of be in good linear relation, rutin is in 3.15~62.99 μ g
mL-1In the range of be in good linear relation.Determination sample Content of Chlorogenic Acid and the peak area of rutin as stated above, substitute into linear side
Journey, calculate the content of compound Content of Chlorogenic Acid and rutin.
The medicine assay combined in compound with phosphatide：
Precision weighs Herba Saussureae Involueratae extract phosphatide complexes 10mg of the present invention, is settled to after fully being dissolved with methanol
50ml, need testing solution is obtained, determine chlorogenic acid and the peak area of rutin as stated above, substitute into linear equation, calculated compound
Thing Content of Chlorogenic Acid and the content of rutin.
Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention obtained by above-mentioned implementation column is subjected to pharmacodynamics
Experiment, its result and process are as follows：
Test row 1：Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet Dichlorodiphenyl Acetate of the present invention causes mouse writhing reaction
Influence
Kunming mouse 50 is taken, male and female half and half, 20 ± 2g of body weight, is randomly divided into model group, beater wheel mill group, this hair
Tomorrow mountain Saussurea involucrata extract phosphatide complexes oral disnitegration tablet low dose group, Herba Saussureae Involueratae extract phosphatide complexes mouth of the present invention
Cavity disintegrating tablet middle dose group and Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet high dose group of the present invention；Each administration group is pressed
Setting dosage ig is administered, model group ig equivalent distilled water, 1 time a day, for three days on end.The 2h after last dose, per mouse ip 0.6%
Acetic acid NS solution 0.2ml/ is only.Writhing number in mouse 15min is observed and recorded, mean t is examined between carrying out group, and calculates suppression
Rate.Statistical result shows, beater wheel mill and Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet low dose group of the present invention,
Middle dose group and high dose can obviously reduce acetic acid and cause mouse writhing reaction times；Herba Saussureae Involueratae extract phosphatide of the present invention is answered
Compound oral disnitegration tablet Dichlorodiphenyl Acetate causes the influence of mouse writhing reaction to be shown in Table 1.
Test row 2：Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet Carrageenan of the present invention causes rat paw
The influence of swelling
Wistar rats 50 are taken, male and female half and half, body weight 120g to 150g, model group, wind are randomly divided into according to body weight sex
Wet safe and sound group, Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet low dose group of the present invention, Herba Saussureae Involueratae of the present invention carry
Take thing phosphatide complexes oral disnitegration tablet middle dose group and Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention high
Dosage group；Each administration group is administered by setting dosage ig, and model group gives equivalent DW, 1 time a day, continuous 5 days.Not secondary administration 1h
Afterwards, it is scorching to 1% carrageenan sterile solution 50ul causes are injected under the left back vola pedis aponeurosis (aponeuroses) of rat.After measure causes scorching preceding and cause scorching respectively
The left back vola pedis thickness of 1h, 2h, 4h, 6h, 8h, so that the difference of vola pedis thickness is as swelling before and after inflammation.Calculate each group rat paw
Swelling average and inhibiting rate, mean t is examined between carrying out group, and statistical result shows, Herba Saussureae Involueratae extract phosphatide complexes mouth
Cavity disintegrating tablet can suppress carrageenan to some extent and cause rat paw edema；Herba Saussureae Involueratae extract phosphatide complexes of the present invention
Oral disnitegration tablet Carrageenan causes the influence of rat paw edema to be shown in Table 2, Herba Saussureae Involueratae extract phosphatide complexes of the present invention
Oral disnitegration tablet Carrageenan causes the inhibiting rate table 3 of rat paw edema.
Inhibiting rate=×100%
Test row 3：Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention causes small to 1-CHLORO-2,4-DINITROBENZENE
The influence of mouse skin of pinna delayed allergy
NIH mouse 50 are taken, male and female half and half, 25 ± 1g of body weight, are randomly divided into model group, beater wheel mill group, the present invention
Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet low dose group, Herba Saussureae Involueratae extract phosphatide complexes oral cavity of the present invention
Disintegrated tablet middle dose group and Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet high dose group of the present invention；Each administration group is by setting
Determine dosage ig to be administered, model group ig equivalent distilled water, 1 time a day, continuous 9 days.The left ear of the 10th day each group mouse applies after administration
0.25% DNFB acetone solution 0.02ml/ is smeared, the acetone solution that offside auricle smears same volume compares, 24h
After put to death mouse, mouse ear is cut at the basal part of the ear, equal area auricle is cut in left and right ear with card punch, weighed respectively, is calculated left
The difference of auris dextra sheet weight is as swelling, and mean t is examined between carrying out group, and calculates inhibiting rate, and statistical result shows, rheumatism
In safe and sound and Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet, heavy dose of it can substantially suppress 2,4- dinitro-chlorines
Benzene is to Mice Auricle delayed allergy；Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention is to 2,4- dinitros
The influence of base chlorobenzene to Mice Auricle skin turgor degree is shown in Table 4.
From table 1 to table 4 as can be seen that Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention is safe and sound compared with rheumatism
Piece Carrageenan causes rat paw edema and swollen hyperplasia of rat granuloma to have good inhibiting effect, can reduce acetic acid and cause mouse
Writhing response number；Illustrate that Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention has good anti-inflammatory, analgesia
Effect, is used to treat rheumatism and rheumatoid arthritis provides pharmacology foundation for it.
Advantages of the present invention：（1）The organic solvent that the present invention selects can ensure the compound of Herba Saussureae Involueratae extract and phosphatide
Solution is clarified, and its polarity can ensure that the stable composition of Herba Saussureae Involueratae extract and matrix material, and does not influence Herba Saussureae Involueratae and carry
The steady quality of thing is taken, and lower boiling non-polar organic solvent is easily evaporated off, organic solvent-free is residual in obtained compound
Stay, recombination rate prepares more than 95% and storage process drug content is without significant change.
2）Medicine/phosphatide dosage is reasonable：The mass ratio of breakthrough based on double solvents, Herba Saussureae Involueratae extract and phosphatide
For 1:1~1:3, you can obtain compound complete compound, phosphatide dosage matches with theoretical guess value.
3）Herba Saussureae Involueratae extract phosphatide complexes significantly improve the dissolubility of Herba Saussureae Involueratae extract, can be preferable
Raising medicine dissolution rate, improve the dissolubility of Herba Saussureae Involueratae extract in the gastrointestinal tract, so as to improve its biology
Availability, and then drug action is preferably played, and stability is good, physical property and chemical property are relatively stable.
4）The Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet of the present invention is that one kind has good taste and disintegration
Rapid novel form, have the characteristics that convenient to take, action is rapid, can not only meet that the medication of the patient of dysphagia is asked
Topic, simultaneously for the patient of anhydrous medication also disclosure satisfy that the demand of its medication, and also overcoming other tablets, flavoring is not brought
Insufferable bitterness problem, improve the compliance of patient.
In summary, organic solvent-free remains in Herba Saussureae Involueratae extract phosphatide complexes, and bioavilability is high, physical
Matter and chemical property are relatively stable；The Herba Saussureae Involueratae extract phosphorus of the present invention obtained by Herba Saussureae Involueratae extract phosphatide complexes
Fat complexes oral disnitegration tablet is convenient to take, it is rapid to work, while improves the compliance of patient, Herba Saussureae Involueratae extraction of the present invention
Thing phosphatide complexes oral disnitegration tablet has good anti-inflammatory, analgesic activity, is used to treat rheumatism and rheumatoid joint for it
Inflammation provides pharmacology foundation.
Above technical characteristic constitutes embodiments of the invention, and it has stronger adaptability and implementation result, can basis
The non-essential technical characteristic of increase and decrease is actually needed, to meet the needs of different situations.
Claims (10)
1. a kind of Herba Saussureae Involueratae extract phosphatide complexes, it is characterised in that obtain as follows：The first step, take appropriate Tianshan Mountains
Saussurea involucrata extract and phosphatide are placed in container, and the mass ratio of phosphatide and Herba Saussureae Involueratae extract is 1:1 to 1:3, then by 1mg extremely
1ml organic solvent A meters are added in 30mg Herba Saussureae Involueratae extracts, it is mixed to obtain first after mixing for addition organic solvent A into container
Close liquid；Second step, the first mixed liquor is placed into constant temperature in a water bath and stirred 0.5 hour to 2 hours, then through water-bath vacuum rotary steam
The second mixed liquor is obtained after removing organic solvent A；3rd step, adding 1ml into 3.75mg Herba Saussureae Involueratae extracts by 1.5mg has
Solvent B is counted, and organic solvent B is added into the second mixed liquor and mixes and obtains filtrate after filtering；4th step, filtrate subtract through water-bath
It is 1.31 to 1.34 to press concentrated by rotary evaporation to the relative density when temperature is 20 DEG C, then through low-temperature vacuum drying to quality percentage
Water content is less than or equal to 5%, obtains Herba Saussureae Involueratae extract phosphatide complexes；Wherein：Organic solvent A is methanol, ethanol, acetic acid
One or more of ethyl ester and n-hexane；Organic solvent B be in chloroform, dichloromethane, n-hexane or ether it is a kind of with
On.
2. Herba Saussureae Involueratae extract phosphatide complexes according to claim 1, it is characterised in that phosphatide be natural phospholipid or
Synthetic phospholipid.
3. Herba Saussureae Involueratae extract phosphatide complexes according to claim 1 or 2, it is characterised in that natural phospholipid is soybean
Phosphatide；Or/and in second step, bath temperature is 30 DEG C to 40 DEG C, stir speed (S.S.) is 2000 revs/min to 3000 revs/min；
Or/and in second step and the 4th step, the temperature of water-bath vacuum rotary steam is 30 DEG C to 40 DEG C, the pressure of water-bath vacuum rotary steam for-
0.08MPa；Or/and the 4th in step, the temperature of low-temperature vacuum drying is 30 DEG C to 60 DEG C.
4. a kind of preparation method of Herba Saussureae Involueratae extract phosphatide complexes according to claim 1 or 2 or 3, its feature
It is to carry out as follows：The first step, appropriate Herba Saussureae Involueratae extract and phosphatide is taken to be placed in container, phosphatide and Herba Saussureae Involueratae
The mass ratio of extract is 1:1 to 1:3, then added by 1mg into 30mg Herba Saussureae Involueratae extracts based on 1ml organic solvent As, to
Added in container after organic solvent A mixes and obtain the first mixed liquor；Second step, the first mixed liquor is placed into constant temperature in a water bath and stirred
Mix 0.5 hour to 2 hours, then obtain the second mixed liquor after water-bath vacuum rotary steam removes organic solvent A；3rd step, is pressed
1.5mg adds 1ml organic solvent B meters into 3.75mg Herba Saussureae Involueratae extracts, and organic solvent B is added into the second mixed liquor and is mixed
Filtrate is obtained after even and filtering；4th step, the relative density that filtrate is concentrated into when temperature is 20 DEG C through water-bath vacuum rotary steam are
1.31 to 1.34, then it is less than or equal to 5% through low-temperature vacuum drying to quality single-detector, obtains Herba Saussureae Involueratae extract phosphorus
Fat complexes；Wherein：Organic solvent A is one or more of methanol, ethanol, ethyl acetate and n-hexane；Organic solvent B is three
One or more of chloromethanes, dichloromethane, n-hexane or ether.
5. the preparation method of Herba Saussureae Involueratae extract phosphatide complexes according to claim 4, it is characterised in that phosphatide is
Natural phospholipid or synthetic phospholipid.
6. the preparation method of the Herba Saussureae Involueratae extract phosphatide complexes according to claim 4 or 5, it is characterised in that natural
Phosphatide is soybean lecithin；Or/and in second step, bath temperature be 30 DEG C to 40 DEG C, stir speed (S.S.) be 2000 revs/min extremely
3000 revs/min；Or/and in second step and the 4th step, the temperature of water-bath vacuum rotary steam is 30 DEG C to 40 DEG C, water-bath decompression rotation
The pressure of steaming is -0.08MPa；Or/and the 4th in step, the temperature of low-temperature vacuum drying is 30 DEG C to 60 DEG C.
7. a kind of made oral disnitegration tablet of Herba Saussureae Involueratae extract phosphatide complexes according to claim 1 or 2 or 3,
It is characterized in that raw materials by weight portion includes 20 parts to 30 parts of Herba Saussureae Involueratae extract phosphatide complexes, 6 parts to 16 of disintegrant
1 part to 3 parts of part, 35 parts to 60 parts of filler, 1 part to 5 parts of adhesive, 0.5 part to 1 part of lubricant and flavouring；Avenge in the Tianshan Mountains
Lotus extract phosphatide complexes oral disnitegration tablet obtains as follows：The desired amount of Herba Saussureae Involueratae extract phosphatide is compound
Mixture is obtained after 1/2 mixing of thing, filler and disintegrant gross weight, the desired amount of adhesive is added in the mixture and mixes
After pelletized, whole grain after drying after granulation, add the desired amount of lubricant, flavouring and disintegrant gross weight after whole grain
1/2 and be well mixed, Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet is obtained after tabletting.
8. oral disnitegration tablet according to claim 7, it is characterised in that disintegrant is low-substituted hydroxypropyl cellulose, crosslinking
One or more of polyvinylpyrrolidone, sodium carboxymethyl starch, Ac-Di-Sol, super sodium carboxymethyl starch；
Or/and filler is one or more of microcrystalline cellulose, lactose, mannitol, soluble starch；Or/and lubricant is hard
One or more of fatty acid magnesium, superfine silica gel powder, talcum powder and hard fumaric acid sodium；Flavouring is Aspartame, honey element and sweet tea
One or more of synanthrin；Adhesive is the ethanol water that percent by volume is 90% to 95% and polyvinylpyrrolidone ethanol
One or more of mixed liquor, wherein：Polyvinylpyrrolidone alcohol mixeding liquid obtains as follows：Count in parts by weight,
After the ethanol water that 1 part to 5 parts of polyvinylpyrrolidone and 97 parts to 99 parts percents by volume are 95% is mixed
Obtain polyvinylpyrrolidone alcohol mixeding liquid；Or/and the particle diameter after granulation is 0.5 millimeter to 1 millimeter；Or/and dry temperature
Spend for 45 DEG C to 55 DEG C, drying time is 0.5h to 2h.
A kind of 9. preparation method according to the oral disnitegration tablet of claim 7 or 8, it is characterised in that raw materials by weight portion bag
Include 20 parts to 30 parts of Herba Saussureae Involueratae extract phosphatide complexes, 6 parts to 16 parts of disintegrant, 35 parts to 60 parts of filler, adhesive 1
Part to 1 part to 3 parts of 5 parts, 0.5 part to 1 part of lubricant and flavouring；The Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet
Preparation method carry out as follows：The desired amount of Herba Saussureae Involueratae extract phosphatide complexes, filler and disintegrant is total
The 1/2 of weight obtains mixture after mixing, and adds after the desired amount of adhesive mixes and is pelletized in the mixture, is passed through after granulation
Whole grain after drying, the 1/2 of the desired amount of lubricant, flavouring and disintegrant gross weight is added after whole grain and is well mixed, press
Herba Saussureae Involueratae extract phosphatide complexes oral disnitegration tablet is obtained after piece.
10. the preparation method of oral disnitegration tablet according to claim 9, it is characterised in that disintegrant is low substituted hydroxy-propyl
In cellulose, PVPP, sodium carboxymethyl starch, Ac-Di-Sol, super sodium carboxymethyl starch
More than one；Or/and filler is one or more of microcrystalline cellulose, lactose, mannitol, soluble starch；Or/and
Lubricant is one or more of magnesium stearate, superfine silica gel powder, talcum powder and hard fumaric acid sodium；Flavouring be Aspartame,
One or more of honey element and stevioside；Adhesive is the ethanol water that percent by volume is 90% to 95% and polyethylene pyrrole
One or more of pyrrolidone alcohol mixeding liquid, wherein：Polyvinylpyrrolidone alcohol mixeding liquid obtains as follows：By weight
Number meter is measured, 1 part to 5 parts of polyvinylpyrrolidone is mixed with 97 parts to 99 parts percents by volume for 95% ethanol water
Polyvinylpyrrolidone alcohol mixeding liquid is obtained after being combined；Or/and the particle diameter after granulation is 0.5 millimeter to 1 millimeter；Or/
It it is 45 DEG C to 55 DEG C with, drying temperature, drying time is 0.5h to 2h.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1359682A (en) * | 2001-12-25 | 2002-07-24 | 沈阳药科大学 | Breviscapine-phosphotide compound and its preparing process |
| CN101209274A (en) * | 2007-12-25 | 2008-07-02 | 新疆维吾尔自治区药物研究所 | Saussurea involucrata extract and saussurea involucrata catablasm and producing method thereof |
| CN101926791A (en) * | 2008-12-25 | 2010-12-29 | 天津康鸿医药科技发展有限公司 | Phospholipid complex of silybin dihemisuccinate disodium and preparation method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1359682A (en) * | 2001-12-25 | 2002-07-24 | 沈阳药科大学 | Breviscapine-phosphotide compound and its preparing process |
| CN101209274A (en) * | 2007-12-25 | 2008-07-02 | 新疆维吾尔自治区药物研究所 | Saussurea involucrata extract and saussurea involucrata catablasm and producing method thereof |
| CN101926791A (en) * | 2008-12-25 | 2010-12-29 | 天津康鸿医药科技发展有限公司 | Phospholipid complex of silybin dihemisuccinate disodium and preparation method and application thereof |
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