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Glassiness sosoloid contg. 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazol formic-acid and polyvinyl pyrrolidone and its prepn. method

A technology of polyvinylpyrrolidone and isobutoxyphenyl, applied in the field of medicine, can solve problems such as poor dissolution rate, and achieve the effects of overcoming poor dissolution rate, fast absorption in vivo, and high bioavailability

Inactive Publication Date: 2006-06-14
GUANGZHOU LIXIN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The invention solves the problem of micronization when directly using 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid raw material to prepare pharmaceutical preparations, and overcomes the problem of preparing pharmaceutical preparations at the same time poor dissolution rate

Method used

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  • Glassiness sosoloid contg. 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazol formic-acid and polyvinyl pyrrolidone and its prepn. method
  • Glassiness sosoloid contg. 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazol formic-acid and polyvinyl pyrrolidone and its prepn. method
  • Glassiness sosoloid contg. 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazol formic-acid and polyvinyl pyrrolidone and its prepn. method

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Preparation of glassy solid solution of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (TMX-67 for short) and polyvinylpyrrolidone

[0042]Weigh 1 g each of TMX-67 and polyvinylpyrrolidone k-12, add 20 ml of acetone, stir, dissolve, remove the acetone under reduced pressure at 50°C, and dry to constant weight to obtain a transparent glassy solid solution with a yield of 100%.

Embodiment 2

[0044] Preparation of glassy solid solution of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (TMX-67 for short) and polyvinylpyrrolidone k17

[0045] Weigh 1g of TMX-67, 10g of polyvinylpyrrolidone k-17, add 20ml of absolute ethanol, stir, dissolve, remove acetone under reduced pressure at 50°C, and dry to constant weight to obtain a transparent glassy solid solution with a yield of 100% .

Embodiment 3

[0047] Preparation of glassy solid solution of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (TMX-67 for short) and polyvinylpyrrolidone k-30

[0048] Weigh 1g of TMX-67, 20g of polyvinylpyrrolidone k-30, add 20ml of methanol, stir and dissolve, remove acetone under reduced pressure at 50°C, dry to constant weight, and obtain a transparent glassy solid solution with a yield of 100%.

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Abstract

A glass-state sosoloid of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolylformic acid (TMX-67) and polyvinyl pyrrolidone for treating gout is disclosed. Its advantages are high stability and high dissolving speed.

Description

technical field [0001] The invention belongs to the technical field of medicine, and mainly relates to 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (TMX-67 for short) and A glassy solid solution formed by polyvinylpyrrolidone and a preparation method thereof, and a pharmaceutical preparation prepared with the solid solution as a main component and a preparation method thereof. Background technique [0002] 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (TMX-67 for short) is a xanthine oxidase inhibitor synthesized in recent years. Regulates the activity of uric acid biosynthesis, and can be used as a therapeutic agent for hyperuricemia, clinically used for the treatment of gout. [0003] TMX-67 English name: Febuxostat, chemical name: 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid [0004] The structural formula is as follows |: [0005] [0006] The molecular formula of the compound: C 16 h 16 N 2 o 3 S, wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K9/14A61K9/20A61K9/48A61K31/79A61P19/06
Inventor 周世旺周学福韩建平田青松王娜姜瑛吴民义瞿虹杨胜利范喜园赵健
Owner GUANGZHOU LIXIN PHARM CO LTD
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