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2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazolyl formic acid of delta-crystal form, as well as preparation method and medicine composite thereof

A technology of thiazole carboxylic acid and phenyl group, applied to the delta-crystal form of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazole carboxylic acid, its preparation and medicine field of composition, capable of addressing issues such as limitations

Inactive Publication Date: 2010-08-18
成都威克药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be inferred from the experimental operation described therein that it is an alcoholate, and the form of the alcoholate has brought great limitations to its pharmaceutical application

Method used

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  • 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazolyl formic acid of delta-crystal form, as well as preparation method and medicine composite thereof
  • 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazolyl formic acid of delta-crystal form, as well as preparation method and medicine composite thereof
  • 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazolyl formic acid of delta-crystal form, as well as preparation method and medicine composite thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Preparation of δ-crystalline form of Febuxostat

[0019] 20 grams of febuxostat obtained according to the method described in the International Patent Specification WO92 / 0927920 was added to 200ml of absolute ethanol, heated to reflux, while stirring, until completely dissolved. The resulting clear solution was refluxed for another hour, then cooled and filtered. The obtained solid was placed in an oven at 80°C and dried under a vacuum of 2 mmHg for 2 hours. According to XRD, δ-crystalline form was formed.

Embodiment 2

[0020] Example 2: Pharmaceutical composition

[0021] A formula for preparing 1,000 tablets each containing 120 mg of febuxostat:

[0022] Example 1 compound 120g

[0023] Pregelatinized starch 110g

[0024] PVP 11.5g

[0025] Magnesium stearate 0.8g

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Abstract

The invention discloses 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazolyl formic acid of a new delta-crystal form and a preparation method thereof. The method comprises the steps of: heating a mixture of Febuxostat and absolute ethanol till completely dissolving, and then filtering to obtain an alcoholate; putting the alcoholate in a 80 DEG C baking oven for baking for 2 hours under 2mmHg vacuum decompression to obtain crystals of the delta-crystal form, which has excellent temperature and humidity stability, no any organic solvents or water and is suitable for preparation process and long-term storage. A medicine composite which takes the compound of the crystal form can be used for reducing uric acid in blood and treating all clinical hyperlithic situations, such as uarthritis.

Description

Technical field [0001] The present invention relates to the delta-crystal form of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid, its preparation method and pharmaceutical composition using the compound as an active ingredient . Background technique [0002] 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid, commonly known as Febuxostat (Febuxostat), structural formula (I) is: [0003] [0004] Febuxostat has extremely valuable pharmacological and therapeutic properties, especially inhibiting the activity of xanthine oxidase, so that the compound can be used to treat diseases with excessive uric acid, such as gout, and to lower blood uric acid. [0005] The preparation and therapeutic use of febuxostat has been described in the International Patent Specification WO92 / 09279. But there is no mention of the compound crystal form phenomenon, so the crystal form of the compound is unclear. It can be inferred from the experimental operation described the...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426A61P19/06
Inventor 王德祥吴松福李主全
Owner 成都威克药业有限责任公司
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