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Ursolic acid solid dispersion and preparation method thereof

A technology of solid dispersion and ursolic acid, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problems of low bioavailability, complicated preparation process, and water solubility of ursolic acid. It can solve problems such as poor properties, and achieve the effects of broad market prospects, high solubility and good in vitro dissolution.

Active Publication Date: 2013-01-16
CHINA GATEWAY PHARMA DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by this invention is to overcome the poor water solubility and low bioavailability of ursolic acid in the prior art and its different pharmaceutical preparations, which cannot meet actual needs, and the conventional preparation of solid dispersion preparations needs to involve There are many kinds of excipients, and the defects such as relatively complicated preparation process provide a kind of good solubility, ursolic acid solid dispersion with higher bioavailability and preparation method thereof

Method used

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  • Ursolic acid solid dispersion and preparation method thereof
  • Ursolic acid solid dispersion and preparation method thereof
  • Ursolic acid solid dispersion and preparation method thereof

Examples

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Effect test

Embodiment 1

[0036] Take 10g of ursolic acid and 150g of polyethylene glycol 6000, put them in a 10L bottle, add 4L of ethanol to ultrasonically dissolve, and use Gene Vac vacuum centrifugation to remove the organic solvent. The temperature control range is 30°C, and the concentration time is 2h. Place it in a vacuum oven at ℃ for 12 hours to remove the residual organic solvent, take it out, grind it through a 10-200-mesh sieve, and obtain it.

Embodiment 2

[0038] Take 10g of ursolic acid and 150g of povidone k29 / 33, put them in a 10L bottle, add 4L of ethanol to ultrasonically dissolve, and use Gene Vac vacuum centrifugation to remove the organic solvent. The temperature control range is 40°C, and the concentration time is 3h. Take out, Put it in a vacuum oven at 30°C for 14 hours to remove the residual organic solvent, take it out, grind it through a 10-200-mesh sieve, and obtain it.

Embodiment 3

[0040] Take 10g of ursolic acid and 150g of hypromellose E5, put them in a 10L bottle, add 4L of ethanol to ultrasonically dissolve, use Gene Vac vacuum centrifugation to remove the organic solvent, the temperature control range is 50°C, the concentration time is 12h, take out, Put it in a vacuum oven at 50°C for 16 hours to remove the residual organic solvent, take it out, grind it through a 10-200-mesh sieve, and obtain it.

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Abstract

The invention discloses an ursolic acid solid dispersion and a preparation method thereof. The formula of the ursolic acid solid dispersion comprises ursolic acid and a carrier material; the mass ratio of the ursolic acid to the carrier material is 1:2 to 1:20; and the carrier material is one or more of PEG6000 (polyethylene glycol 6000), povidone k29 / 33, hypromellose E5, polyving alcohol, poloxamer 68, GELUCIRE 50 / 13, polyacrylic resin EPO, polyacrylic resin L 100-55, povidone-vinyl alcohol, hypromellose AS-HG, hypromellose AS-LG, hypromellose AS-MG, low substituted hypromellose, hypromellose phthalate, cellulose acetate phthalate, glucan, polyoxyethylene, polyoxyethylene stearates and polyvinyl acetate phthalate. The preparation method comprises the following steps: dissolving the ursolic acid and the carrier material into an organic solvent according to the formula; removing the organic solvent; and grinding. The ursolic acid solid dispersion has good solubility and has high bioavailability.

Description

technical field [0001] The invention relates to a solid dispersion of ursolic acid and a preparation method thereof. Background technique [0002] Ursolic acid (ursolic acid, UA), also known as ursolic acid and ursolic acid, belongs to pentacyclic triterpene carboxylic acids. It is widely found in various plants such as apple, raspberry, berry, elderberry, pepper, lavender, mint, thyme, hawthorn, plum tree, etc. Ursolic acid has a wide range of pharmacological activities, such as anti-cancer, anti-ulcer, anti-inflammatory, antibacterial, anti-virus, liver protection, anti-hyperlipidemia, anti-oxidation and sedative effects and other biological effects, these physiological effects make it It has a wide range of applications in cancer, especially liver cancer, fatty liver, heart disease treatment, and even in the cosmetics market. [0003] The molecular weight of ursolic acid is 456.7, which is a small molecular compound. It shows rod-shaped crystals under the microscope, an...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/56A61K47/38A61K47/36A61K47/34A61K47/32A61P35/00A61P31/04A61P31/12A61P29/00A61P39/06A61P25/20A61P9/00A61P3/06A61P1/04A61P1/16
Inventor 施斌宋英
Owner CHINA GATEWAY PHARMA DEV CO LTD
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