89 results about "ASIATIC ACID" patented technology

The invention provides a method for preparing total triterpenoids with a hypoglycemic effect from leaves of Cyclocarya paliurus. The leaves of the Cyclocarya paliurus are taken as a raw material and subjected to extraction with an ethanol-water mixed solvent and liquid-liquid extraction with an organic solvent, polyamide column chromatography based organic solvent elution and macroporous resin column chromatography based ethanol-water elution are performed for separation and purification, and high-purity total triterpenoids can be obtained. Research proves that main components such as arjunolic acid, asiatic acid, cyclocaric acid B and a compound 4 in the total triterpenoids can effectively increase glucose uptake of 3T3-L1 adipose cells and have antidiabetic activity, and the total triterpenoids and the main components of the total triterpenoids can be used for preparing products such as hypoglycemic and antidiabetic drugs, health food and functional food. The method for preparing thetotal triterpenoids from the leaves of Cyclocarya paliurus and an application of the total triterpenoids and the compound 4 to preparation of the antidiabetic drugs are developed, reference is provided for popularization, utilization and deep processing of traditional Chinese medicinal materials, and a new application direction is provided.

The invention relates to the technical field of pharmaceutical preparation, in particular to an asiatic acid sustained-release microsphere used for injection and a preparation method thereof. A biodegradable chitosan is taken as a carrier, an asiatic acid is taken as principal agent, and the asiatic acid sustained-release microsphere used for injection is obtained by the technology of cross-linked emulsion. Due to the obtained medicament carried microspheres, the surfaces are relatively smooth; the particle diameters range from 20mum to 110mum; and the medicament loading rate of the microspheres ranges from 4.8% to 15.6%. The asiatic acid microsphere has the characteristics that the burst effect is modest (the burst size on the first day is smaller than 15%); the release rate is stable; the sustained release time is long (4-10 weeks); and the asiatic acid microsphere is biodegradable. The implantation and the removal by operation before and after the medicament is used are avoided.

The invention discloses a compound with a wrinkle removing function. The compound comprises triterpenoid saponin and triterpene acid, wherein the triterpenoid saponin and the triterpene acid are active ingredients from centella. The triterpenoid saponin comprises one or two of asiaticoside and hydroxy asiaticoside, and the triterpene acid comprises one or two of asiatic acid and madasiatic acid. By compounding any one or two of the triterpenoid saponin with any one or two of the triterpene acid, human skin fibroblast secretes type I collagen, and the like can be remarkably improved, the obvious effect of aging skin regeneration is realized, and the compound can be used for the development of wrinkle removing cosmetics.

The new use of astatic acid in manufacturing drugs is disclosed, particularly the use in the aspect of manufacturing drugs for anti hepatic fibrosis.

The invention relates to the new application of asiatic acid and its derivatives in the preparation of antidepressants. Experiments have proved that asiatic acid and its derivatives, as well as the pharmaceutical composition, are safe, efficient, stable, and cheap drugs for preventing and treating depression, all of which have relatively high activity, especially asiatic acid, centella asiatica Compounds such as sodium oxalate are more active than doxepin.

The invention provides a method for purifying asiatic acid in asiatic pennywort herb. The method comprises the following steps of: adding a biological enzyme into an asiatic pennywort herb medicinal material serving as a raw material for performing natural enzymolysis; extracting a zymolyte with 70-99 percent alcohol solution for 1-3 times; recovering ethanol from an extracting solution under reduced pressure; adding petroleum ether into a concentrated solution for degreasing; dissolving a crude extract and adding macroporous resin for mixing; loading onto a macroporous resin column with a dry method; eluting with ethanol solutions of different concentrations; concentrating and crystalizing; refluxing, dissolving and recrystallizing a crystal with methanol and acetone; and drying to obtain a product. The method has the advantages of easiness for process operation, resin recyclability, and high content, high yield and low cost of the obtained product, and is suitable for industrial production.

The invention discloses an asiatic acid self-microemulsifying drug delivery system (AA-SMEDDS) and its preparation method. The AA-SMEDDS comprises the following raw materials, by mass, 0.5-5% of AA, 10-50% of an oil phase, 30-75% of an emulsifier, and 0-30% of an emulsification assistant. The preparation method comprises the following steps: weighing a proper amount of the AA, adding formula amounts of the emulsification assistant and the emulsifier, stirring at 25-45DEG C to dissolve the AA, adding the oil phase and other auxiliary materials according to formula amounts, and uniformly stirring. An AA micro-emulsification oral preparation composition provided by the invention self-emulsifies to emulsion droplets with the particle sizes being below 100nm after the composition is orally taken and meets with a body fluid. The AA-SMEDDS has the advantages of simple preparation, good drug stability and high biological utilization degree.

The invention discloses a method for preparing asiatic acid by basic hydrolysis of asiaticoside, which comprises the following steps: 1) adding a raw material of astiaticoside into a water solution of inorganic base in batches, and hydrolyzing the raw material at a temperature of between 45 and 90 DEG C for 1-24 hours; 2) adding acid into the hydrolysate solution, adjusting the pH value to between 2 and 4, depositing the solution, and filtrating the solution to obtain precipitate; and 3) adding the precipitate into organic solvent after drying of the precipitate, dissolving the precipitate and filtering the solvent, adding water into filtrate for crystallization, obtaining a crystal after filtration of the filtrate, and drying the crystal through vacuum so as to obtain asiatic acid products. The asiatic acid products have high yield and purity and can be used for preparing raw materials medicine or astiatic acid derivant; in addition, the method has a simple technical process and low investment, and is easy to realize industrialization.

The invention relates to a centella asiatica fermentation liquor, a preparation method and application of the centella asiatica fermentation liquor, wherein the centella asiatica fermentation liquor can be used for converting high-content madecassoside and producing high-activity asiatic acid and derivatives of the high-activity asiatic acid by utilizing a microbial conversion reaction. After centella asiatica is fermented by thermus thermophilus, the centella asiatica is converted to generate the madecassoside and asiatic acid, the content of madecassoside is increased by 200-8000 times, and the effects of the fermented centella asiatica, such as inflammation resistance, wound repair, oxidation resistance, whitening and skin cell repair capability (light damage repair and scratch repair) are also remarkably improved.

The invention relates to skin external products, in particular to drug-carrying nanofibers and a preparation method and application thereof. The drug-carrying nanofibers contain nanofiber bodies and asiatic acid, wherein the nanofiber bodies are formed by auxiliary components, and asiatic acid is loaded on the nanofiber bodies; and relative to each gram of asiatic acid, the content of the auxiliary components is 5-75 g. The preparation method of the drug-carrying nanofibers includes the steps: a spinning solution containing asiatic acid and the auxiliary components is subjected to electrostatic spinning to obtain the drug carrying nanofibers. The application of the drug-carrying nanofibers for preparing scar-inhibiting skin external products is also disclosed. According to the drug-carrying nanofibers, asiatic acid serves as an active component, the efficacy of the active component is released continuously, therefore, healing is promoted, inflammation is diminished, growth and proliferation behaviors of cells are adjusted, then, growth and development of scars are effectively inhibited, and accordingly the drug-carrying nanofibers can be widely applied to the skin external products, especially to dressings. A blending electrostatic spinning method is adopted to prepare the drug carrying nanofibers, a preparation technology is simple, and the prepared drug-carrying nanofibers are continuous and uniform.

The invention discloses an asiatic acid salt tablet and a preparation method thereof. A formula of the tablet comprises 1-40 percent of asiatic acid amino butantriol salt, 25-60 percent of a filling agent, 1-10 percent of an adhesive, 0.5-40 percent of a disintegrating agent and 0.1-1.5 percent of a lubricant, wherein the percentage refers to the mass percentage of each component in the total amount of the asiatic acid salt tablet. The method comprises the following steps of: in the terms of the formula, uniformly mixing the smashed and sieved asiatic acid amino butantriol salt, filling agent, adhesive and disintegrating agent; mixing with 5-20 percent by mass of an ethanol solution; pelletizing and drying; mixing with the lubricant; and tableting. The asiatic acid salt tablet disclosed by the invention has high bioavailability.

The invention discloses a method for extracting, separating and purifying chemical components of walnut green seedcases and application of the chemical components. According to the method, 13 compounds are separated from the walnut green seedcases and respectively identified as 3,5-dimethoxy-4-hydroxy-benzoic acid-7-O-beta-D-glucoside (1), myricananin F (2), beta-sitosterol (3), oleanolic acid (4), walnut ketone (5), asiatic acid (6), hederagenin (7), beta-carotene (8), (4R)-4,8-dihydroxy-alpha-tetralone-4-O-beta-D-glucopyranoside (9), 3beta,23-dihydroxy-12-olefin-28-ursolic acid (10), ursolicacid (11), syringic acid (12) and Juglanoside B (13). After screening of anti-tumor activity in vitro, it is found that some compounds have certain growth inhibitory activity against cancer cells andcan be further used for preparing anticancer drugs.

The invention discloses AA-CS-DCA micelles and a preparation method of AA-CS-DCA micelles. According to the AA-CS-DCA micelles provided by the invention, CS-DCA is taken as a carrier, and AA is encapsulated, the particle sizes of obtained micelles are smaller than 100nm, the drug loading amount is 4% to 11% and the encapsulation efficiency is 61% to 81%. The preparation method of the AA-CS-DCA micelles comprises the following steps: firstly, synthesizing CS-DCA, then adding CS-DCA to deionized water to be dissolved, and taking AA to be dissolved in methanol, carrying out ultrasound treatment by a probe after mixing the two solutions, carrying out reduced pressure rotary evaporation to remove organic solvents, taking a supernatant to be freeze-dried after performing centrifugation to obtainthe AA-CS-DCA micelles. The micelles can significantly increase intestinal drug absorption and improve oral bioavailability.

The invention discloses a method for preparing asiaticoside by alkali hydrolysis of centella selected triterpenes, which comprises the following steps: 1) adding centella selected triterpenes raw material into an aqueous solution of inorganic base in batch for hydrolysis at a temperature of between 45 and 90 DEG C for 1 to 24 hours; 2) adding acid into the hydrolysate solution to adjust the pH value to be 2-4, depositing and filtering the hydrolysate solution to obtain deposit; and 3) drying the deposit, adding the deposit into an organic solvent for dissolution, decoloring the solution by active carbon, filtering the solution, adding water into filtrate for crystallization, filtering the filtrate to obtain crystals, and drying the crystals in vacuum to obtain the asiaticoside product. The asiaticoside product has high yield and purity, and can be used as bulk drug or further separated into different asiatic acid products; the asiaticoside product taken as a medicine can be used to treat skin wound, resist depressive illness and Alzheimer's disease, protect liver and veins of heart and brain, induce tumour cell apoptosis and so on; meanwhile, the method has simple technological process, small investment, and easy industrialization.

The invention provides an Asiatic acid derivative compound, or a pharmaceutically acceptable salt or ester thereof, or any optical isomer thereof, or any tautomer thereof represented by a general formula (I). In the formula, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 can be independently same or different, and can be hydrogen, hydroxy, carboxy, C1-6 alkylhydroxyl, C1-6 alkylcarboxyl, C1-6 alkoxy, unsubstituted or mono-substituted or poly-substituted C3-6 cycloalkyl substituted by C1-6 alkyl, halogen, hydroxy or C1-6 alkoxy, or unsubstituted or mono-substituted or poly-substituted C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl substituted by halogen. The invention also provides a preparation method of the above Asiatic acid derivative, and an application of the derivative in the preparation of hypoglycemic drugs. The preparation method is suitable for large-scale productions. The obtained Asiatic acid derivative has an outstanding effect in the application of the preparation of the hypoglycemic drugs.

The invention discloses a method for extracting asiatic acid from centella. The method comprises the following steps: 1) pulverizing centella, extracting with a 60-70 v% ethanol solution under reflux, filtering the extracting solution, recovering the solvent from the filtrate, adding 40-50-DEG C for dissolution, filtering, and dissolving the filter residue in a 50-60 v% ethanol solution to obtain a crude extract; 2) adding a rare-earth salt into the crude extract, and mixing and stirring uniformly to obtain a mixed solution; and 3) passing the mixed solution through an X-5 macroporous resin column, washing with water to a colorless state, eluting with 20-30 v% ethanol, carrying out thin-layer chromatography tracking detection, collecting the ethanol eluate containing the target component, recovering the ethanol, and drying to obtain the asiatic acid. The asiatic acid extracted by the method has the advantages of high purity and high yield.

The invention discloses a culture solution and method for improving the in-vitro maturation quality of porcine oocytes. The culture solution is prepared from the following components: an M199 culturesolution, 10 ng / mL of EGF, 10 [mu]M of asiatic acid, 0.6 mM of L-cysteine, 0.91 mM of sodium pyruvate, 10% follicular fluid, 10 IU / mL of LH, 10 IU / mL of FSH and 100 IU / mL of penicillin. According to the culture solution and method, the asiatic acid is added into the porcine oocyte in-vitro maturation culture solution for the first time, the maturation rate of the oocytes can be effectively increased, the quality of the oocytes can be effectively improved, the development rate of the oocytes can be effectively increased, the quality of the oocytes can be effectively improved, the developmentalrate of parthenogenetic embryos and in-vitro fertilized embryos can be increased, the embryo quality of the parthenogenetic embryos and the in-vitro fertilized embryos can be improved, and the problems of low efficiency and poor quality of in-vitro maturation and in-vitro culture at present are effectively solved.

The invention discloses a crystal form A of asiatic acid tromethamine salt, which has main peaks at angles of diffraction 2theta being equal to 5.98, 6.87, 9.12, 10.38, 12.00, 12.47, 12.93, 13.42, 14.72, 15.10, 17.01 and 18.14 degrees, and which has minor peaks at 2theta being equal to 3.44, 13.87, 15.89, 19.04, 19.64, 20.17, 20.94, 21.75, 22.56, 23.33, 24.18, 26.38, 26.98 and 27.75 degrees. The invention also discloses a crystal form B of asiatic acid tromethamine salt, which has main peaks at angles of diffraction 2theta being equal to 3.54, 7.05, 10.04, 11.88, 13.38, 14.29 and 15.18 degrees; and which has minor peaks at 2theta being equal to 9.28, 9.59, 12.43, 16.68, 17.03, 17.57, 18.16, 18.91, 19.24, 20.07, 20.68, 22.46, 24.84, 25.20, 26.86, 27.73, 28.30, 28.85, 30.43, 30.83 and 33.93 degrees. Further, the invention discloses preparation methods of the crystal forms A and B. The crystal forms A and B of asiatic acid tromethamine salt are brand new crystal forms and have excellent stability. The methods provided by the invention have the advantages of simple operation and ease of implementation.

The invention discloses a process for extracting asiatic acid from herba centellae and belongs to the technical field of preparation of the asiatic acid. The asiatic acid is prepared through the following steps of crushing, carrying out primary de-coloring, crystallizing, carrying out secondary de-coloring, recrystallizing, extracting, separating and purifying, concentrating and crystallizing, drying and the like. According to the method disclosed by the invention, the extraction yield of the asiatic acid is 64.8 percent or more and the purity of the asiatic acid is 98.09 percent or more, the purity is higher than that of the asiatic acid prepared in the prior art and the asiatic acid can be used as a qualitative and quantitative reference substance.

The invention discloses a method for preparing asiatic acid by asiaticoside acid hydrolysis. The method comprises the following steps: 1) adding the asiaticoside raw material into a mixed solution of an organic solvent I, water and inorganic acid to be hydrolyzed at a temperature of between 45 and 90 DEG C for 1 to 24 hours; 2) concentrating under reduced pressure hydrolyzate to remove the organic solvent I, filtering the precipitated solvent to obtain a precipitate; and 3) adding an organic solvent II into the dried precipitate to be dissolved and filtered, adding water crystal into filtrate, filtering the mixed solvent to obtain crystal, and drying the crystal in vacuum to obtain the asiatic acid product. The asiatic acid product has high yield and purity, can be used for preparation of a bulk drug or asiatic acid derivates; meanwhile, the method has a simple technological process and small investment, and can realize industrialization easily.

The invention discloses an asiatic acid salt hard capsule and a preparation method thereof. An asiatic acid salt hard capsule formula comprises 5-40 percent of an asiatic acid amino butantriol salt, 50-95 percent of a filling agent, 0-10 percent of a lubricating agent and 0-2.0 percent of an adhesive, wherein the percentage refers to the mass percentage of each component in the total amount of asiatic acid salt hard capsule contents. The method comprises the following steps of: uniformly mixing the raw materials according to a formula; and filling into the conventional hard capsule shell. The asiatic acid salt hard capsule disclosed by the invention has high bioavailability.

The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analog, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

The invention discloses an asiatic acid lipid nanoparticle capable of stimulating oral absorption and a preparation method thereof. The asiatic acid lipid nanoparticle is prepared by taking a lipid material as a carrier and asiatic acid as a main drug through a solvent diffusion method. The particle size of the obtained lipid nanoparticle is smaller than 700nm, the entrapment rate is 40-90% and the drug-loading rate is 7-11%. By utilizing the nanoparticle, the intestinal drug absorption can be increased, and the oral bioavailability is improved.

The invention discloses a method for preparing asiatic acid by hydrolyzing asiaticoside. The method comprises the following steps: 1) mixing asiaticoside, lauryl sodium sulfate and NaOH, adding water for dissolution, and hydrolyzing at normal temperature for 10-15 minutes; 2) regulating the pH value of the hydrolysate to 2-5, standing, filtering, and collecting the precipitate; and 3) dissolving the precipitate in ethanol, filtering, adding water to the filtrate, crystallizing, filtering to obtain the crystal, and drying to obtain the finished product. The method can quickly cut off glycosidic bonds under the conditions of normal temperature and pressure, has the advantages of mild hydrolytic process and thorough hydrolysis, and can not generate configurative changes of asiatic acid.

The invention discloses a hydroxyl asiatic acid choline salt, a preparation method and an application thereof, a hydroxyl asiatic acid glucosamine salt, a preparation method and an application thereof, and a hydroxyl asiatic acid trometamol salt, a preparation method and an application thereof. A hydroxyl asiatic acid salt solution is high in purity, is wide in concentration range, is abundant in selectable drug delivery approaches, and can be used for preparing medicines and cosmetics for preventing or treating fibrosis and resisting aging. Compared with free hydroxyl asiatic acid or other forms of the hydroxyl asiatic acid salt, the hydroxyl asiatic acid salt is greatly enhanced in water solubility and is easy to prepare into an injection or various solution agents. Through the proper preparation method, the bioavailability of the medicine is effectively improved so that the effect of the medicine is greatly improved. The medicine can be used for treating various fibrosis diseases and preventing or treating scar hyperplasia and also has an anti-aging function.

The invention discloses an asiatic acid lipid nanoparticle capable of stimulating oral absorption and a preparation method thereof. The asiatic acid lipid nanoparticle is prepared by taking a lipid material as a carrier and asiatic acid as a main drug through a solvent diffusion method. The particle size of the obtained lipid nanoparticle is smaller than 700nm, the entrapment rate is 40-90% and the drug-loading rate is 7-11%. By utilizing the nanoparticle, the intestinal drug absorption can be increased, and the oral bioavailability is improved.

The present invention discloses a medicinal composition for treating bladder cancer and a preparation method thereof. The raw material drug, which is prepared by proportioning, can be made into various dosage forms according to the conventional preparation process, and has a remarkable curative effect on bladder cancer.

The invention relates to L-tryptophan asiatic acid amide (X4) and applications thereof in preparation of antidepressant medicines, and also provide a pharmaceutical composition comprising the L-tryptophan asiatic acid amide. Experiments show that: the L-tryptophan asiatic acid amide and the pharmaceutical composition thereof are safe, efficient, stable and cheap medicines for preventing and treating depression, have high activity, are superior to asiatic acid and fluoxetine, and have high development value.

The invention discloses application of asiatic acid in preparation of a medicine for preventing hepatitis virus. The chemical structure of the asiatic acid is as shown in formula I. Through in vitro building a hepatitis c virus (HCV cc) model derived from cell culture, and using an HCV susceptible cell human liver cancer Huh7 cell line, an in-vitro experiment on the anti-HCV activity of the asiatic acid is performed. The result shows that the asiatic acid has obvious anti-HCV activity, particularly is capable of inhibiting the HCV invading the target cell and can be used for preparing the anti-hepatitis c virus medicine. A novel path for the asiatic acid is provided and a novel source for finding the anti-hepatitis c virus medicine is also provided.