Febuxostat crystal form and preparation method thereof

A febuxostat and crystal form technology, applied in the field of febuxostat crystal form and its preparation, can solve problems such as research without crystal form

Active Publication Date: 2010-02-17
CSPC OUYI PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The patent EP513379 reports the synthesis method of febuxostat, using the method of ethanol recrystallization to obtain febuxostat, but did not study its crystal form

Method used

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  • Febuxostat crystal form and preparation method thereof
  • Febuxostat crystal form and preparation method thereof
  • Febuxostat crystal form and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Put 60g of febuxostat and 480ml of acetone in a round-bottomed flask, heat in a water bath at a temperature of 55°C, and electromagnetically stir to dissolve all the solids. Stop heating after reflux for 1 hour, and electromagnetically stir at room temperature until crystals are precipitated. Suction filtration, normal pressure Dry at 60° C. for 3 hours to obtain 56 g of crystals, ie febuxostat Q crystal form, with a yield of 93.3%.

Embodiment 2

[0022] Put 80g of febuxostat and 640ml of acetone in a round-bottomed flask, heat in a water bath at a temperature of 65°C, and electromagnetically stir to dissolve all the solids. Stop heating after reflux for 2 hours, and electromagnetically stir at room temperature until crystals are precipitated. Suction filtration, normal pressure Dry at 70° C. for 5 hours to obtain 74 g of crystals, ie febuxostat Q crystal form, with a yield of 92.5%.

Embodiment 3

[0024] Put 70g of febuxostat and 560ml of acetone in a round-bottomed flask, heat in a water bath at a temperature of 60°C, and electromagnetically stir to dissolve all the solids. Stop heating after reflux for 1.5 hours, and electromagnetically stir at room temperature until crystals are precipitated. Suction filtration, normal pressure Dry at 65° C. for 4 hours to obtain 66 g of crystals, ie febuxostat crystal form Q, with a yield of 94.3%.

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Abstract

The invention relates to a Febuxostat crystal form. The x-ray powder diffraction has characteristic peaks when a refraction angle 2 theta is at 6.80+ / - 0.2 degree, 11.04+ / - 0.2 degree, 13.56+ / - 0.2 degree, 15.74+ / -0.2 degree, 17.56+ / -0.2 degree, 20.36+ / -0.2 degree, 22.10+ / -0.2 degree, 24.72+ / - 0.2 degree, 25.38+ / - 0.2 degree, 28.80+ / -0.2 degree and 29.10 degrees+ / - 0.2 degree. The invention also provides a preparation method of the Febuxostat crystal form. The crystal form has better stability and is suitable for technically applying preparations and being stored in a long period.

Description

technical field [0001] The invention relates to a febuxostat crystal form and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Febuxostat is a new generation of xanthine oxidase inhibitors, clinically used for the treatment of gout (hyperuric acid). The usual means of treatment for gout is to promote uric acid excretion and inhibit uric acid production, and take appropriate measures to improve related symptoms. The generation of uric acid in the body is related to purine metabolism. In the final step of purine metabolism, hypoxanthine generates xanthine under the action of xanthine oxidoreductase (XOR), and then further generates uric acid. Inhibiting the activity of XOR can effectively reduce the production of uric acid. generate. [0003] Febuxostat is a new type of non-purine XOR enzyme inhibitor, which is highly selective for XOR, and has significant inhibitory effect on both oxidized and reduced XOR. Clinical s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/56A61P19/06
Inventor 张典鹏颜文革李瑞建董鹏胡艳茹
Owner CSPC OUYI PHARM CO LTD
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