CN102755333A - Asiatic acid salt micro-emulsion preparation and preparation method thereof - Google Patents
Asiatic acid salt micro-emulsion preparation and preparation method thereof Download PDFInfo
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- CN102755333A CN102755333A CN2011101130812A CN201110113081A CN102755333A CN 102755333 A CN102755333 A CN 102755333A CN 2011101130812 A CN2011101130812 A CN 2011101130812A CN 201110113081 A CN201110113081 A CN 201110113081A CN 102755333 A CN102755333 A CN 102755333A
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- hydrochlorate
- herba centellae
- microemulsion formulation
- asiatic acid
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Abstract
The invention discloses an asiatic acid salt micro-emulsion preparation and a preparation method thereof. A formula of the asiatic acid salt micro-emulsion preparation comprises 5-30 percent of asiatic acid amino butantriol salt, 10-30 percent of an oil phase, 5-20 percent of a surfactant, 10-30 percent of a cosurfactant and the balance of a water phase, wherein the percentage refers to the mass percentage of each component in the total amount of the raw materials. The preparation method comprises the following steps of: uniformly mixing the asiatic acid amino butantriol salt with the surfactant according to the formula; uniformly mixing with the cosurfactant; uniformly mixing with the oil phase; and uniformly mixing with the water phase. The asiatic acid salt micro-emulsion preparation disclosed by the invention has high bioavailability.
Description
Technical field
The present invention relates to a kind of Herba Centellae hydrochlorate microemulsion formulation 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 microemulsion formulation 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 microemulsion formulation thereof unsatisfactory, and the extremely low defective of bioavailability, and a kind of Herba Centellae hydrochlorate microemulsion formulation with good biological availability and preparation method thereof is provided.
Herba Centellae hydrochlorate microemulsion formulation prescription of the present invention contains 5%～30% asiatic acid tromethane salt, 10%～30% oil phase, 5%～20% surfactant, 10%～30% cosurfactant and supplies the water of surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
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.
In the present invention, the oil phase of the conventionally used in the art of oil phase, preferably is polyethylene glycol-400, ethylene glycol, acetonitrile, acetylated monoglyceride, ethyl acetate, methyl acetate, Isoamyl acetate, amyl acetate, ethyl alcohol, ethanol, denatured alcohol, diluted alcohol, diethyl ether, ethylene glycol distearate, triethylene glycol dilaurate, triethylene glycol monoethyl cinnamate, diethylene glycol monolaurate, diethylene glycol monostearate, triethylene glycol dicaprylate, xylene, dimethyl acetamide, dimethyl formamide, dimethyl sulfoxide, ten dialkyl sulfoxide, diisopropylamine, methylene chloride, carbon disulfide, triethylene glycol, diglycidyl ether, isopropyl myristate, N, N-dimethylformamide, 2,3 - butanedione, 1,3 - butanediol, 1,4 - butanediol, butanone, triglycerol octyl caprate, triglycerol monooleate, triglycerol monostearate, hexaglycerol monostearate fat acid esters, decaglycerol tetraoleate, decaglycerol monooleate eight, ten glycerol monooleate ten, ten ten glycerol monostearate, hexaglycerol distearate, diglycerol mono-2 - hexyl decyl esters, triglycerol monolaurate, trichlorethylene, dichloroethylene, tetrachlorethylene, hexane, Azone, 1 - Ge geranylgeranyl - aza ring hept - one, 1 - farnesyl - heterocyclic hept - ketone, diethyl malonate, propylene glycol, propane, propylene carbonate, butyl acrylate, methyl acrylate, allyl alcohol, acetone, 2 - methyl -2,4 - pentanediol , methyl isobutyl ketone, N-methyl-2 - pyrrolidone, methanol, glycerol acetal, 5 - hydroxy-dioxan-4 - hydroxy-dioxane, glycerol, glycerol diacetate, glycerol triacetate, glycerol mono- acetate, tetrahydrofuran, polyethylene glycol ethers, tetrachlorethylene, carbon tetrachloride, corn oil, n-butanol, isobutanol, petroleum ether, alcohol, isopropyl myristate, isopropyl palmitate, isopropyl alcohol , diisopropyl ether, isooctane, myristyl alcohol, sesame oil, acetic acid, o-dichlorobenzene, diethyl phthalate, dibutyl phthalate, dimethyl phthalate, phthalic acid dioctyl ester, soybean oil, almond oil, peanut oil, benzene, benzaldehyde, cyclohexane, epichlorohydrin, ethyl lactate, butyl lactate, turpentine, terpineol, ethyl oleate, t-amyl alcohol, single amine, diethyl sebacate, isopropyl sebacate, dibutyl sebacate, di-n-octyl sebacate, ethyl decanoate, peach kernel oil, terpene alcohols oils, liquid paraffin, canola oil, nitrogen chloride, chloroform, ethyl succinate, n-butyl stearate, cottonseed oil, decyl seed oil, castor oil, polyethylene glycol, polypropylene glycol, olive oil, acetic acid, L-peppermint oil, hydrogenated castor sulfonated sesame oil and squalane in one or more, more preferably is polyethylene glycol-400, soybean oil, ethyl acetate, ten and eleven glycerol monostearate in one or more of.
Among the present invention; Described surfactant is the surfactant of the conventional aerosol in this area; Like the hard ester ether of sodium lauryl sulphate, sodium tetradecyl sulfate, sodium cetostearylsulphate, nonokynol-9-10, Hamposyl L, Hamposyl C, Semen Myristicae sarcosine, Hamposyl S, lauric isopropropanolamide, lauric acid diethyl amide, propylene glycol, propylene glycol diacetate, propylene glycol monostearate, Polyoxyethylene Sorbitan Monooleate, glycerol, isopropyl alcohol, lecithin, hydrolecithin, sodium lactate, stearic acid sodium lactate, lactic acid myristyl ester, lactic acid cetyl ester, sodium palmitate, polyvinyl alcohol, polysorbate-20, polysorbate-40, polysorbate-60, polysorbate-65, Polyoxyethylene Sorbitan Monooleate, polysorbate-85, BL-25, polyoxyethylene cetostearyl ether, polyoxyethylene (30EO) sorbitol 4 oleyl ethers, polyoxyethylene (40EO) sorbitol 4 oleyl ethers, polyoxyethylene (60EO) sorbitol 4 oleyl ethers, polyoxyethylene (60EO) sorbitol 4 stearyl ether, Emulsifier LT-60M, polyoxyethylene alkyl ether, emulsifying agent-BY, emulsifying agent-MoA, emulsifying agent-O, polyoxyethylene (10) oleyl ether, polyoxyethylene (8), the hard ester ether of polyoxyethylene (12), the hard ester ether of polyoxyethylene (24), the hard ester ether of polyoxyethylene (100), the hard ester ether of polyoxyethylene (110), the hard ester ether of polyoxyethylene (40), the hard ester ether of polyoxyethylene (50), polyoxyethylene (40) castor oil hydrogenated, polyoxyethylene (10) castor oil hydrogenated, polyoxyethylene (30) castor oil hydrogenated, polyoxyethylene (50) castor oil hydrogenated, polyoxyethylene (60) castor oil hydrogenated, polyoxyethylene (40) Oleum Ricini, polyoxyethylene (10) Oleum Ricini, polyoxyethylene (35) Oleum Ricini, polyoxyethylene (60) Oleum Ricini, polyoxyethylene (80) Oleum Ricini, polyoxyethylene (90) Oleum Ricini, polyoxyethylene (100) Oleum Ricini, the single oleyl ether of polyoxyethylene (300), the single oleyl ether of polyoxyethylene (400), the single oleyl ether of polyoxyethylene (600), sulphur Hua Oleum Ricini, sulfonation castor oil hydrogenated, sodium dioctyl sulfosuccinate, dioctyl sulphosuccinate calcium and dioctyl sulphosuccinate potassium, one or more that preferable is in Polyoxyethylene Sorbitan Monooleate, polyoxyethylene-40 Oleum Ricini, polyoxyethylene-40 castor oil hydrogenated and the lecithin.
Among the present invention; Described cosurfactant is the conventional described cosurfactant in this area; Like ethylene glycol monostearate, ethylene glycol laurate, ethylene glycol monoleate, glycol monopalmitate, ethylhydroxyethylcellulose, acetylated monoglyceride, diethylene glycol distearate, triethylene glycol laurate, triethylene glycol list cinnamate, triethylene glycol monolaurate, diethylene glycol monostearate, triethylene glycol dicaprylate, N; N-diethyl lauramide, diacetyl monoglyceride, polyvinyl alcohol, polysorbate-20, polysorbate-40, polysorbate-60, polysorbate-65, Polyoxyethylene Sorbitan Monooleate, polysorbate-85, polyoxyethylene (4) laurate, polyoxyethylene (8) laurate, polyoxyethylene (12) laurate, polyoxyethylene (24) laurate, polyoxyethylene (40) laurate, polyoxyethylene (100) laurate, Polyethylene Glycol (200) monolaurate, Polyethylene Glycol (400) monolaurate, gather second two ferment (600) monolaurate, gather second two ferment (1000) monolaurate, gather second two ferment (6000) monolaurate; In short chain alcohol that preferable is, organic amine, the plain acid of alkyl, single two alkyl acid glyceride and the polyoxyethylene fatty acid ester one or more, one or more that better is in propylene glycol, triethylene glycol list cinnamate, Polyethylene Glycol-400 monolaurate and the diethylene glycol monostearate.
Among the present invention, described water is the conventional described water in this area.
What Herba Centellae hydrochlorate microemulsion formulation of the present invention prescription was preferable is made up of 5%～30% asiatic acid tromethane salt, 10%～30% oil phase, 5%～20% surfactant, 10%～30% cosurfactant and the water of supplying surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
The invention still further relates to the Herba Centellae hydrochlorate microemulsion formulation preferred embodiments of filling a prescription and contain 5%～20% asiatic acid tromethane salt, 10%～25% oil phase, 5%～15% surfactant, 10%～30% cosurfactant and supply the water of surplus 100%, percentage ratio accounts for the mass percent of raw material total amount for each composition.
The invention still further relates to the Herba Centellae hydrochlorate microemulsion formulation another preferred embodiments of filling a prescription and be made up of 5%～20% asiatic acid tromethane salt, 10%～25% oil phase, 5%～15% surfactant, 10%～30% cosurfactant and the water of supplying surplus 100%, percentage ratio accounts for the mass percent of raw material total amount for each composition.
Wherein, described oil phase dive, surfactant and cosurfactant all as previously mentioned.
The invention still further relates to the Herba Centellae hydrochlorate microemulsion formulation preferred embodiments of filling a prescription and contain 5%～30% asiatic acid tromethane salt, 10%～30% Polyethylene Glycol-400,5%～15% Polyoxyethylene Sorbitan Monooleate, 10%～30% propylene glycol and supply the water of surplus 100%, percentage ratio accounts for the mass percent of raw material total amount for each composition.
Herba Centellae hydrochlorate microemulsion formulation of the present invention can also contain conventional various other additives that add in this area and other active components, as long as it does not have antagonism or not appreciable impact microemulsion formulation effect of the present invention.
Herba Centellae hydrochlorate microemulsion formulation of the present invention can make by this area conventional method; Preferable method for preparing comprises the steps: by said prescription; With asiatic acid tromethane salt and surfactant uniform mixing, again with the cosurfactant uniform mixing, afterwards with the oil phase uniform mixing; With the water uniform mixing, get final product again.
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: Herba Centellae hydrochlorate microemulsion formulation of the present invention has the good biological availability, and quality stability is good, and extensive market prospects and practical value are arranged.
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: with asiatic acid tromethane salt and surfactant uniform mixing,,, with the water uniform mixing, get final product again afterwards with the oil phase uniform mixing again with the cosurfactant uniform mixing by last table prescription.
Through simultaneously the sample of SD rat vein administration being compared (rat tail vein injection with asiatic acid tromethane salt; The bioavailability of asiatic acid tromethane salt is 20.4% in the gained microemulsion formulation " it is thus clear that Nanfang Medical Univ's journal " 06 phase in 2009).
Embodiment 2
Method for preparing: with asiatic acid tromethane salt and surfactant uniform mixing,,, with the water uniform mixing, get final product again afterwards with the oil phase uniform mixing again with the cosurfactant uniform mixing by last table prescription.
Through simultaneously the sample of SD rat vein administration being compared (rat tail vein injection with asiatic acid tromethane salt; The bioavailability of asiatic acid tromethane salt is 18.1% in the gained microemulsion formulation " it is thus clear that Nanfang Medical Univ's journal " 06 phase in 2009).
Embodiment 3
Method for preparing: with asiatic acid tromethane salt and surfactant uniform mixing,,, with the water uniform mixing, get final product again afterwards with the oil phase uniform mixing again with the cosurfactant uniform mixing by last table prescription.
Through simultaneously the sample of SD rat vein administration being compared (rat tail vein injection with asiatic acid tromethane salt; The bioavailability of asiatic acid tromethane salt is 13.4% in the gained microemulsion formulation " it is thus clear that Nanfang Medical Univ's journal " 06 phase in 2009).
Embodiment 4
Method for preparing: with asiatic acid tromethane salt and surfactant uniform mixing,,, with the water uniform mixing, get final product again afterwards with the oil phase uniform mixing again with the cosurfactant uniform mixing by last table prescription.
Through simultaneously the sample of SD rat vein administration being compared (rat tail vein injection with asiatic acid tromethane salt; The bioavailability of asiatic acid tromethane salt is 14.40% in the gained microemulsion formulation " it is thus clear that Nanfang Medical Univ's journal " 06 phase in 2009).
Claims (9)
1. Herba Centellae hydrochlorate microemulsion formulation; It is characterized in that: its prescription contains 5%～30% asiatic acid tromethane salt, 10%～30% oil phase, 5%～20% surfactant, 10%～30% cosurfactant and supplies the water of surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
2. Herba Centellae hydrochlorate microemulsion formulation as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate microemulsion formulation prescription is made up of 5%～30% asiatic acid tromethane salt, 10%～30% oil phase, 5%～20% surfactant, 10%～30% cosurfactant and the water of supplying surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
3. Herba Centellae hydrochlorate microemulsion formulation as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate microemulsion formulation prescription contains 5%～20% asiatic acid tromethane salt, 10%～25% oil phase, 5%～15% surfactant, 10%～30% cosurfactant and supplies the water of surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
4. Herba Centellae hydrochlorate microemulsion formulation as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate microemulsion formulation prescription is made up of 5%～20% asiatic acid tromethane salt, 10%～25% oil phase, 5%～15% surfactant, 10%～30% cosurfactant and the water of supplying surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
5. like each described Herba Centellae hydrochlorate microemulsion formulation of claim 1～4, it is characterized in that: described oil phase is one or more in Polyethylene Glycol-400, Oleum Glycines, ethyl acetate and ten glycerol, ten stearates.
6. like each described Herba Centellae hydrochlorate microemulsion formulation of claim 1～4, it is characterized in that: described surfactant is one or more in Polyoxyethylene Sorbitan Monooleate, polyoxyethylene-40 Oleum Ricini, polyoxyethylene-40 castor oil hydrogenated and the lecithin.
7. like each described Herba Centellae hydrochlorate microemulsion formulation of claim 1～4, it is characterized in that: described cosurfactant is one or more in propylene glycol, triethylene glycol list cinnamate, Polyethylene Glycol-400 monolaurate and the diethylene glycol monostearate.
8. Herba Centellae hydrochlorate microemulsion formulation as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate microemulsion formulation prescription contains 5%～30% asiatic acid tromethane salt, 10%～30% Polyethylene Glycol-400,5%～15% Polyoxyethylene Sorbitan Monooleate, 10%～30% propylene glycol and supplies the water of surplus 100%, and percentage ratio accounts for the mass percent of raw material total amount for each composition.
9. like the method for preparing of each described Herba Centellae hydrochlorate microemulsion formulation of claim 1～8; It is characterized in that: it comprises the steps: by said prescription; With asiatic acid tromethane salt and surfactant uniform mixing, again with the cosurfactant uniform mixing, afterwards with the oil phase uniform mixing; With the water uniform mixing, get final product again.
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| CN201110113081.2A CN102755333B (en) | 2011-04-29 | 2011-04-29 | Asiatic acid salt micro-emulsion preparation and preparation method thereof |
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| CN201110113081.2A CN102755333B (en) | 2011-04-29 | 2011-04-29 | Asiatic acid salt micro-emulsion preparation and preparation method thereof |
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| CN102755333B CN102755333B (en) | 2015-07-29 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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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| 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 |
Non-Patent Citations (1)
| Title |
|---|
| 史同瑞等: "微乳及微乳制剂的研究", 《上海畜牧兽医通讯》 * |
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