New crystal form of febuxostat and preparation method thereof

A technology of febuxostat and crystal form, applied in the new crystal form K of febuxostat and its preparation field, can solve problems such as unfavorable industrial production, high environmental protection pressure, large crystal form static electricity, etc., and achieves less solvent usage , low cost, low hygroscopicity

Active Publication Date: 2010-03-17
HEFEI IND PHARMA INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the process of studying the crystal form of febuxostat, the inventor found that although the microcrystalline dissolution rate mentioned in CN101085761A was ideal, the crystal form had relatively high static electricity, required more auxiliary materials in the preparation process, and the operation was extremely cumbersome, and The amount of solvent is large, and the pressure on environmental protection is high, which is not conducive to industrial production

Method used

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  • New crystal form of febuxostat and preparation method thereof
  • New crystal form of febuxostat and preparation method thereof
  • New crystal form of febuxostat and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Add 5g of febuxostat crude product and 40ml of tetrahydrofuran into a three-neck flask, raise the temperature to 40°C, stir to completely dissolve, filter, concentrate the filtrate until crystals are precipitated, let it cool to crystallize, filter, and dry in vacuum at 60°C to obtain the crystal form K sample 4.1g.

Embodiment 2

[0057] Tablet preparation

[0058] The new crystal form 40g that embodiment 1 prepares

[0059] Microcrystalline Cellulose 40g

[0060] Starch 30g

[0061] Crospovidone 10g

[0062] Magnesium Stearate 1g

[0063] Made into 1000 pieces

[0064] Preparation process: weigh components other than magnesium stearate and mix them evenly, use water as a binder to make a soft material, granulate with a 16-mesh sieve, dry at 80°C for about 2 hours, add magnesium stearate to the whole granule, mix evenly, and press into tablets. have to.

Embodiment 3

[0066] Preparation of capsules

[0067] The new crystal form 40g that embodiment 1 prepares

[0068] Low-substituted hypromellose 40g

[0069] Lactose 20g

[0070] Carboxymethyl Starch Sodium 10g

[0071] Magnesium Stearate 1g

[0072] Make 1000 capsules

[0073] Preparation process: Weigh and mix the components other than magnesium stearate evenly, use water as the binder to make a soft material, granulate with a 16-mesh sieve, dry at 80°C for about 2 hours, add magnesium stearate to the whole granule, mix evenly, fill in 4 No. capsules, you can.

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Abstract

The invention discloses a new crystal form of febuxostat and a preparation method thereof. The preparation method of the crystal form adopts tetrahydrofuran as a solvent, the crystal form is small instatic electricity and has good dissolution rate, other processing manners such as micronization or preparation of solid dispersion and the like are not required during the process of preparing the pharmaceutical preparation, and the preparation with good dissolution rate can be obtained according to the conventional preparation process.

Description

technical field [0001] The invention relates to a new crystal form K of febuxostat and a preparation method thereof. The crystal form has low static electricity and good dissolution rate, and is suitable for preparing solid preparations with excellent dissolution rate with conventional pharmaceutical auxiliary materials. Background technique [0002] Febuxostat (Febuxostat) chemical name: 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid, is a new type of non-purine XOR inhibitor, its It is highly selective to XOR, and has significant inhibitory effect on both oxidized and reduced XOR, and is clinically used to treat hyperuricemia. [0003] There are many crystal forms of febuxostat. Chinese patent CN1275126 records A, B, C, D, G crystal forms and amorphous forms and their preparation methods invented by Teijin Corporation of Japan. Among them, A, C, and G crystal forms are relatively stable. , from the consideration of industrial superiority, crystal form A ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/56A61K31/426A61P19/06
Inventor 何广卫李丰吴强刘为中
Owner HEFEI IND PHARMA INST CO LTD
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