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Butane diacid(5-androstene-17-ketone- 3beta -hydroxyl group ) diester solid dispersoid and method for making same and applications thereof

A technology of solid dispersion and succinic acid, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., to achieve good water solubility, improve water solubility, and significant curative effect

Inactive Publication Date: 2007-12-05
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solvent method technology uses an inert carrier polyethylene glycol (PEG) to mix with the drug. The solvent method is often used to dissolve the drug and then evaporate the organic solvent, so that the drug is highly dispersed in the carrier in an amorphous form. This method requires the use of tetrahydrofuran, pyridine, and chloroform. , dichloromethane and other organic solvents, there are shortcomings of organic solvent residues and wrapped in the carrier

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1 Succinic acid (5-androstene-17-one-3β-hydroxyl) diester solid dispersion preparation

[0021] Succinic acid (5-androstene-17-one-3β-hydroxyl) diester, with a purity of 99.6%, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Life Sciences, Sun Yat-sen University. Polyvinylpyrrolidone PVP-k30 (referred to as PVP), imported sub-packaged, provided by the Guangzhou Chemical Reagent Wholesale Department, succinic acid, analytically pure, provided by the Guangzhou Chemical Reagent Wholesale Department.

[0022] 10 grams of succinic acid (5-androstene-17-one-3β-hydroxyl) diester is mixed with 80 grams of succinic acid, the heated solid is completely melted, added dropwise to 5000ml deionized distilled water, and stirred while adding dropwise, Collect the suspended matter by filtration, redissolve the suspended matter in 5000ml deionized distilled water, resuspend with 5000ml deionized distilled water, filter and collect ...

Embodiment 2

[0023] Example 2 Preparation of succinic acid (5-androstene-17-one-3β-hydroxyl) diester solid dispersion

[0024] Succinic acid (5-androstene-17-one-3β-hydroxyl) diester, with a purity of 99.6%, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Life Sciences, Sun Yat-sen University. Polyvinylpyrrolidone PVP-k30 (referred to as PVP), imported sub-packaged, provided by the Guangzhou Chemical Reagent Wholesale Department, succinic acid, analytically pure, provided by the Guangzhou Chemical Reagent Wholesale Department.

[0025] 80 grams of succinic acid (5-androstene-17-ketone-3β-hydroxyl) diester is mixed with 750 grams of succinic acid, the heated solid is completely melted, added dropwise to 20000ml deionized distilled water, and stirred while adding dropwise, The suspension is collected by filtration, the suspension is re-dissolved in 20000ml deionized distilled water, suspended again with 20000ml deionized water, the suspension is ...

Embodiment 3

[0026] Example 3 Solubilization of Succinic Acid (5-Androstene-17-one-3β-Hydroxy) Diester Homogeneous Dispersion

[0027] Succinic acid (5-androstene-17-one-3β-hydroxyl) diester with a purity of 99.6%, referred to as A1998, provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Life Sciences, Sun Yat-sen University. Polyvinylpyrrolidone PVP-k30 (referred to as PVP), imported and repackaged, provided by Guangzhou Chemical Reagent Wholesale Department.

[0028] Preparation of solid dispersion of A1998 According to the method provided in Example 1, solid dispersions with ratios of A1998:PVP of 1:2, 1:4, 1:6, 1:8, and 1:10 were prepared. A1998 in vitro dissolution test was determined with ZRS28G intelligent dissolution tester (Tianjin University Radio Factory). According to the dissolution method of the second part of the Chinese Pharmacopoeia in 2005, 1000ml of aqueous solution is used as the solvent, the rotation speed is 100 revolutions per m...

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Abstract

The present invention discloses solid dispersoid of bis(5-androstene-17-one-3beta-hydroxy) succinate and its preparation process and application. The solid dispersoid consists of bis(5-androstene-17-one-3beta-hydroxy) succinate and polyvinyl pyrrolidone intelligent weight ratio of 1-20. It is prepared through heating the mixture of succinic acid and bis(5-androstene-17-one-3beta-hydroxy) succinate to form melt and prepare powdered bis(5-androstene-17-one-3beta-hydroxy) succinate, coating bis(5-androstene-17-one-3beta-hydroxy) succinate with polyvinyl pyrrolidone in water solution to obtain the solid dispersoid. The solid dispersoid of bis(5-androstene-17-one-3beta-hydroxy) succinate has over 80 times raised water solubility and obvious curative effect on drug liver injury.

Description

technical field [0001] The present invention relates to succinic acid (5-androstene-17-one-3β-hydroxyl) diester, specifically, relates to a kind of succinic acid (5-androstene-17-one-3β-hydroxyl) diester Ester solid dispersion and its preparation method and application. Background technique [0002] At present, the solubility of most pharmaceutical active ingredients in organisms is very small, and the difficult problem for the pharmaceutical industry is how to improve the solubility and bioavailability of poorly soluble drugs. Solutions include micronization technology, cyclodextrin inclusion technology, self-emulsification technology, and solvent method technology. [0003] Succinic acid (5-androstene-17-one-3β-hydroxy) diester compound, insoluble in water, soluble in organic solvents such as tetrahydrofuran, chloroform, pyridine, dichloromethane, etc., using conventional micronization technology, it is difficult to improve its solubility. Micronization technology is ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/565A61K47/34A61P1/16
CPCA61K31/5685A61K9/1635A61P1/16
Inventor 许东晖梅雪婷许实波
Owner SUN YAT SEN UNIV
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