CN102755330A - Asiatate granules and preparation method thereof - Google Patents
Asiatate granules and preparation method thereof Download PDFInfo
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- CN102755330A CN102755330A CN2011101130615A CN201110113061A CN102755330A CN 102755330 A CN102755330 A CN 102755330A CN 2011101130615 A CN2011101130615 A CN 2011101130615A CN 201110113061 A CN201110113061 A CN 201110113061A CN 102755330 A CN102755330 A CN 102755330A
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- asiatic acid
- acid salt
- salt particle
- asiatic
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Abstract
The invention discloses asiatate granules and a preparation method thereof. The asiatate granules comprise 1-40% of trometamol asiatate, 25-60% of filler, 1-10% of binder and 0-40% of disintegrating agent in mass percentages of the total amount of the asiatate granules. The preparation method comprises the following steps: according to a formulation, uniformly mixing the components; granulating; and drying. The asiatate granules have good bioavailability.
Description
Technical field
The present invention relates to a kind of asiatic acid salt particle agent and preparation method thereof.
Background technology
Report asiatic acid and salt thereof can be prevented and treated the fibrotic disease of some internal organs in the prior art, and still, the drug effect of relevant granule is unsatisfactory, and bioavailability is extremely low, effectively utilizes this medicine for maximizing, and this present situation needs to be resolved hurrily.
Summary of the invention
Technical problem to be solved by this invention is that to have overcome the drug effect of existing asiatic acid and salt particle agent thereof unsatisfactory, and the extremely low defective of bioavailability, and a kind of asiatic acid salt particle agent with good biological availability and preparation method thereof is provided.
Asiatic acid salt particle agent prescription of the present invention contains 1%～40% asiatic acid tromethane salt, 25%～60% filler, 1%～10% binding agent and 0%～40% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
Among the present invention, the size of described granule is the conventional used size in this area, and that preferable is 370 μ m～991 μ m.
Among the present invention, described asiatic acid tromethane salt is the conventional described asiatic acid tromethane salt in this area, commercially available get or extract by the asiatic acid raw material according to this area conventional method obtain.
Among the present invention; Described filler is the conventional described filler in this area; Can use diluent for water-soluble diluent, water-insoluble diluent or direct compression; Preferable in trihydroxy aminomethane, sorbitol, sorbitol instant, D-xylose, xylitol, propylene carbonate, calcium glycerophosphate, mannitol, the corn starch of can sterilizing, compressible sugar, crospolyvinylpyrrolidone, inositol, Thomas balsam, maltose alcohol, soda-lime, alpha-lactose, lactose, aluminium hydroxide, medicinal sugar, calcium oxide, zinc oxide, prepared teobroma, pregelatinized Starch, Powderd cellulose, colloidality silicon dioxide, aluminium silicate, Aluminum calcium silicate., starch, sodium chloride, calcium chloride, aluminum chloride, calcium sulfate, glucose, Pulvis Talci, microcrystalline Cellulose, bagasse regrowth, carboxymethylcellulose calcium, polyethylene, polyethylene azoxy ketone, polyvinyl butyral resin, polyethylene acetal diethyl acetate ester, calcium carbonate, magnesium carbonate, magnesium oxide, sucrose, spherical sucrose, compressible sugar, sugar,confectioner's, dextrin, white dextrin, calcium phosphate and the sodium starch phosphate one or more, one or more that better is in mannitol, alpha-lactose, microcrystalline Cellulose and the starch.
Among the present invention; Described binding agent is the conventional described binding agent in this area, preferable is ethylmethylcellulose, ethyl cellulose, ethyl cellulose aqueous suspension, butadiene-styrene rubber, natural rubber, acrylic acid, butylacrylate, acrylic acid methyl ester., acrylic resin I number, acrylic resin II number, acrylic resin III number, acrylic resin IV number, Eudragit E
30, chitin, chitose, methyl methacrylate, EMA, butyl methacrylate, EUDRAGIT S100, Eudragit E, acrylic resin L, acrylic resin S, acrylic resin RL, acrylic resin RS, metering system-2-ethoxy, methacrylic acid-2-hydroxypropyl acrylate, methylcellulose, glycerol three rosin esters, zein, compressible sugar, sesbania gum, tara gum, Ficus elastica, carbomer, Petropols, Furcellaran, tragacanth, arabic gum, Resina persicae, maltose alcohol, carrageenin, tamarind gum, high fructose syrup, Nulomoline, fructose, Colophonium, loose glue, POLY-karaya, modified starch, poloxamer, medicinal sugar, alginic acid, sodium alginate, potassium alginate, ammonium alginate, calcium alginate, pregelatinized Starch, Powderd cellulose, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, xanthan gum, aluminium-magnesium silicate, terpene resin, liquid glucose, starch, sodium starch glycol, potassium metaphosphate, scleroglucan, glucose, glucosan, Pullulan, acetyl group Pullulan, microbial alginate, microcrystalline Cellulose, bagasse regrowth, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, Mel, guaiac gum, polyethylene, polyethylene azoxy ketone, polyvinyl butyral resin, polyethylene acetal diethyl acetate ester, polybutene, polybutadiene, polymethyl methacrylate, gather methyl 2-methylmethacrylate copolymer, gather methyl and gather L-methyl methacrylate, sodium polyacrylate, polyacrylic acid, polyisobutylene, Parleam, polystyrene-maleic anhydride, polyvinyl-maleic anhydride, gather in 2-ethoxy formyl acrylic ester, polyvidone, polyvinyl acetate, sucrose, spherical sucrose, compressible sugar, sugar,confectioner's, sucrose fatty acid ester, sucrose monolaurate, sucrose palmitic acid ester, locust bean gum, dextrin, white dextrin, cellulose acetate, a cellulose acetate, cellulose diacetate, Triafol T, cellulose acetate dibutylamino-hydrox-ypropyl ether and the sodium starch phosphate one or more, one or more that better is in hydroxypropyl emthylcellulose, dextrin, modified starch and the tragacanth.
Among the present invention; Described disintegrating agent is the conventional described disintegrating agent in this area; One or more that preferable is in silicon dioxide, sodium lauryl sulphate, Stepanol MG, natrium carbonicum calcinatum, fumaric acid, methylcellulose, glycine, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula crystallite aluminum spray drying thing, crospolyvinylpyrrolidone, POLY-karaya, polacrilin potassium, modified starch, malic acid, citric acid, alginic acid, sodium alginate, tartaric acid, pregelatinized Starch, Powderd cellulose, silica sol, hydroxyethylmethyl-cellulose, aluminium-magnesium silicate, starch, sodium starch glycol, microbial alginate, microcrystalline Cellulose, bagasse regrowth, microwax, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, polyethylene azoxy ketone, Polyoxyethylene Sorbitan Monooleate, polyoxyethylene, sodium bicarbonate, potassium bicarbonate, potassium carbonate, sucrose fatty acid ester, sucrose monolaurate, sucrose palmitic acid ester, sodium dioctyl sulfosuccinate, dioctyl sulphosuccinate calcium, dioctyl sulphosuccinate potassium, sodium dihydrogen phosphate and the potassium dihydrogen phosphate, one or more that better is in crospolyvinylpyrrolidone, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose and the citric acid.
Asiatic acid salt particle agent prescription of the present invention is preferable contains 1%～40% asiatic acid tromethane salt, 25%～60% filler, 1%～10% binding agent and 0.5%～40% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
Further preferable being made up of 1%～40% asiatic acid tromethane salt, 25%～60% filler, 1%～10% binding agent and 0.5%～40% disintegrating agent of asiatic acid salt particle agent prescription of the present invention, percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
Asiatic acid salt particle agent prescription of the present invention is also preferable contains 16.22%～38.46% asiatic acid tromethane salt, 38.46%～54.05% filler, 4%～23.08% binding agent and 0%～24.49% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
Wherein, described filler, binding agent and disintegrating agent are all as previously mentioned.
The invention still further relates to asiatic acid salt particle agent prescription one preferred embodiments and comprise 14%～40% asiatic acid tromethane salt, 30%～60% mannitol, 2%～10% hydroxypropyl emthylcellulose and 5%～30% crospolyvinylpyrrolidone, percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
Asiatic acid salt particle of the present invention agent can also contain conventional various other additives that add and other active component in the conventional granulates agent of this area, as long as it does not have antagonism or not appreciable impact granule effect of the present invention.
Asiatic acid salt particle of the present invention agent can make by this area conventional method, and preferable method for preparing comprises the steps: by said prescription, behind each raw material uniform mixing, granulate, and dry getting final product.
Wherein, the grain diameter of described granulation size is the conventional used size in this area, and that preferable is 370 μ m～991 μ m.
Wherein, the preparation of described asiatic acid salt particle agent uses equipment to be this area conventional equipment.
Agents useful for same of the present invention and raw material are all commercially available to be got.
On the basis that meets this area general knowledge, each above-mentioned among the present invention technical characterictic optimum condition can combination in any obtain preferred embodiments.
Positive progressive effect of the present invention is: asiatic acid salt particle of the present invention agent has the good biological availability, and quality stability is good, and the disintegrate index is stable, and facile hydrolysis does not have extensive market prospects and practical value.
The specific embodiment
Mode through embodiment further specifies the present invention below, but does not therefore limit the present invention among the described scope of embodiments.
Embodiment 1
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through being mixed with preparation posterior vein administration (the rat tail vein injection that is fit to intravenously administrable with normal saline with asiatic acid tromethane salt; It is thus clear that " Nanfang Medical Univ's journal " 06 phase in 2009) simultaneously by measuring behind this prescription single-dose SD rat, the bioavailability of asiatic acid tromethane salt is 23.6% in the gained granule.
Embodiment 2
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through measuring behind the single-dose SD rat simultaneously with asiatic acid tromethane salt intravenously administrable, the bioavailability of asiatic acid tromethane salt is 20.8% in the gained granule.
Embodiment 3
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through measuring behind the single-dose SD rat simultaneously with asiatic acid tromethane salt intravenously administrable, the bioavailability of asiatic acid tromethane salt is 17.4% in the gained granule.
Embodiment 4
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through measuring behind the single-dose SD rat simultaneously with asiatic acid tromethane salt intravenously administrable, the bioavailability of asiatic acid tromethane salt is 15.0% in the gained granule.
Embodiment 5
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through measuring behind the single-dose SD rat simultaneously with asiatic acid tromethane salt intravenously administrable, the bioavailability of asiatic acid tromethane salt is 22.1% in the gained granule.
Comparative Examples 1
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through also measuring behind the parallel while single-dose SD rat with asiatic acid potassium salt intravenously administrable (rat tail vein injection, visible " Nanfang Medical Univ's journal " 06 phase in 2009), the bioavailability of asiatic acid potassium salt is 15.1% in the gained granule.
Comparative Examples 2
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through measure (rat tail vein injection, visible " Nanfang Medical Univ's journal " 06 phase in 2009) simultaneously behind the single-dose SD rat with asiatic acid potassium salt intravenously administrable, the bioavailability of asiatic acid potassium salt is 15.1% in the gained granule.
Comparative Examples 3
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through with asiatic acid arginine salt intravenously administrable (rat tail vein injection; It is thus clear that " Nanfang Medical Univ's journal " 06 phase in 2009) and behind the parallel while single-dose SD rat measure, the bioavailability of asiatic acid arginine salt is 0.9% in the gained granule.
Comparative Examples 4
Method for preparing: behind each raw material uniform mixing, granulate, and dry getting final product.
Through with asiatic acid arginine salt intravenously administrable (rat tail vein injection; It is thus clear that " Nanfang Medical Univ's journal " 06 phase in 2009) and behind the parallel while single-dose SD rat measure, the bioavailability of asiatic acid arginine salt is 0.9% in the gained granule.
Claims (10)
1. asiatic acid salt particle agent; It is characterized in that: its prescription contains 1%～40% asiatic acid tromethane salt, 25%～60% filler, 1%～10% binding agent and 0%～40% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
2. asiatic acid salt particle as claimed in claim 1 agent; It is characterized in that: described asiatic acid salt particle agent prescription contains 1%～40% asiatic acid tromethane salt, 25%～60% filler, 1%～10% binding agent and 0.5%～40% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
3. asiatic acid salt particle as claimed in claim 1 agent; It is characterized in that: described asiatic acid salt particle agent prescription is made up of 1%～40% asiatic acid tromethane salt, 25%～60% filler, 1%～10% binding agent and 0.5%～40% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
4. asiatic acid salt particle as claimed in claim 1 agent; It is characterized in that: described asiatic acid salt particle agent prescription contains 16.22%～38.46% asiatic acid tromethane salt, 38.46%～54.05% filler, 4%～23.08% binding agent and 0%～24.49% disintegrating agent, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
5. asiatic acid salt particle as claimed in claim 1 agent is characterized in that: the size of described asiatic acid salt particle agent is 370 μ m～991 μ m.
6. like each described asiatic acid salt particle agent of claim 1～5, it is characterized in that: among the present invention, described filler is one or more in mannitol, alpha-lactose, microcrystalline Cellulose and the starch.
7. like each described asiatic acid salt particle agent of claim 1～5, it is characterized in that: described binding agent is one or more in hydroxypropyl emthylcellulose, dextrin, modified starch and the tragacanth.
8. like each described asiatic acid salt particle agent of claim 1～5, it is characterized in that: described disintegrating agent is one or more in crospolyvinylpyrrolidone, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose and the citric acid.
9. asiatic acid salt particle as claimed in claim 1 agent; It is characterized in that: described asiatic acid salt particle agent prescription contains 14%～40% asiatic acid tromethane salt, 30%～60% mannitol, 2%～10% hydroxypropyl emthylcellulose and 5%～30% crospolyvinylpyrrolidone, and percentage ratio accounts for the mass percent of asiatic acid salt particle agent total amount for each composition.
10. like the method for preparing of the described asiatic acid salt particle of claim 1～9 agent, it is characterized in that: it comprises the steps: by said prescription, behind each composition uniform mixing, granulate, and dry getting final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110113061.5A CN102755330B (en) | 2011-04-29 | 2011-04-29 | Asiatate granules and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110113061.5A CN102755330B (en) | 2011-04-29 | 2011-04-29 | Asiatate granules and preparation method thereof |
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| Publication Number | Publication Date |
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| CN102755330A true CN102755330A (en) | 2012-10-31 |
| CN102755330B CN102755330B (en) | 2015-06-24 |
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| CN201110113061.5A Expired - Fee Related CN102755330B (en) | 2011-04-29 | 2011-04-29 | Asiatate granules and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101176731A (en) * | 2006-11-08 | 2008-05-14 | 上海医药工业研究院 | Application of asiatic acid in the aspect of resisting pulmonary fibrosis |
| CN101969942A (en) * | 2008-01-11 | 2011-02-09 | 上海医药工业研究院 | Therapeutic formulations based on asiatic acid and selected salts thereof |
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2011
- 2011-04-29 CN CN201110113061.5A patent/CN102755330B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101176731A (en) * | 2006-11-08 | 2008-05-14 | 上海医药工业研究院 | Application of asiatic acid in the aspect of resisting pulmonary fibrosis |
| CN101969942A (en) * | 2008-01-11 | 2011-02-09 | 上海医药工业研究院 | Therapeutic formulations based on asiatic acid and selected salts thereof |
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| CN102755330B (en) | 2015-06-24 |
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Effective date of registration: 20150507 Address after: 200040 Beijing West Road, Shanghai, No. 1320 Applicant after: Shanghai Institute of pharmaceutical industry Address before: 200040 Beijing West Road, Shanghai, No. 1320 Applicant before: Shanghai Institute of pharmaceutical industry Applicant before: Heilongjiang Hongdoushan Pharmaceutical Co., Ltd. |
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