Solid pharmaceutical composition containing 2-(3-cyano-4- isobutoxy phenyl)-4-methyl-5-thiazole methanoic acid

A technology of isobutoxyphenyl and thiazole carboxylic acid, which is applied in the field of solid pharmaceutical compositions, can solve the problems that the drug dissolution curve cannot be obtained without deviation

Inactive Publication Date: 2008-04-02
BEIJING D VENTUREPHARM TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN 1642546 believes that 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid has multiple crystal forms, even if it is used in the physical stability test during the preparation of th

Method used

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  • Solid pharmaceutical composition containing 2-(3-cyano-4- isobutoxy phenyl)-4-methyl-5-thiazole methanoic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] (1) Evenly mix Febuxostat and polyethylene glycol, and dissolve in an aqueous solution containing 50% (v / v) ethanol;

[0034] (2) by (1) step gained solution, spray drying;

[0035] (3) Add the powder obtained in step (2), add microcrystalline cellulose PH101, lactose, crospovidone xl, and mix evenly; take an appropriate amount of 10% starch slurry, granulate, dry, and granulate, and the dry granules are added to hard Magnesium fatty acid, blended, compressed.

Embodiment 2

[0038] (1) Evenly mix Febuxostat and polyethylene glycol, and dissolve in an aqueous solution containing 50% (v / v) ethanol;

[0039] (2) by (1) step gained solution, spray drying;

[0040] (3) Add microcrystalline cellulose PH101, lactose, crospovidone xl to the powder obtained in step (2), and mix well. An appropriate amount of 10% starch slurry is granulated, dried, granulated, and the dry granules are added with magnesium stearate, mixed together, and compressed into tablets.

Embodiment 3

[0043] (1) Evenly mix Febuxostat and polyethylene glycol, and dissolve in an aqueous solution containing 50% (v / v) ethanol;

[0044] (2) by (1) step gained solution, spray drying;

[0045] (3) Add microcrystalline cellulose PH101, lactose, crospovidone xl to the powder obtained in step (2), and mix well. An appropriate amount of 10% starch slurry is granulated, dried, granulated, and the dry granules are added with magnesium stearate, mixed together, and compressed into tablets.

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Abstract

The present invention provides a solid medicine combination, which comprises 2 - (3 - cyano -4 - butyl rubber oxygen phenyl) -4 - methyl -5 - thiazole formic acid as active ingredients; and polyethylene glycol. In addition, the present invention is combined with one or a plurality of medicine excipients. The present is used for the curing of gout and hyperuricemia and reducing the outbreak of acute gout.

Description

technical field [0001] The present invention relates to a solid pharmaceutical composition, which contains 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid or a pharmaceutically acceptable form thereof in a pharmaceutically acceptable form. Accepted salt. Background technique [0002] 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (Febuxostat), the structural formula is: [0003] [0004] Febuxostat is a novel non-purine selective inhibitor of xanthine oxidase that reduces uric acid production. Febuxostat is effective for the vast majority of acid patients suffering from gout and hyperuricemia, and can reduce and stabilize blood uric acid levels below 6.0 mg / dl, reducing acute gout attacks. [0005] WO 9209279 discloses the Febuxostat compound, its chemical preparation and its use in the treatment of gout and hyperuricemia, which is incorporated herein by reference in its entirety. [0006] CN 1642546 thinks that 2-(3-cyano-4-isobutoxy...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/426A61P19/06
Inventor 莫良侃
Owner BEIJING D VENTUREPHARM TECH DEV
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