Drug chemical compound for gout

A technology of pharmaceutical compounds, compounds, applied in the field of medicine

Active Publication Date: 2013-12-25
HANGZHOU ZHUYANGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been found that during the long-term storage of febuxostat raw materials or its preparations, a certain specific impurity tends to increase with the prolongation of sample retention time. is very disadvantageous

Method used

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  • Drug chemical compound for gout
  • Drug chemical compound for gout
  • Drug chemical compound for gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0145] Embodiment 1: preparation febuxostat bulk drug

[0146] Step (1): Prepare according to the method described in paragraphs [0022] to [0042] of the specification of Chinese Patent Application No. 200910170029.3 (CN102002016A, Medicom), to obtain the refined febuxostat product. As determined by 【High Performance Liquid Chromatography A】, RRT3.55 content = 0.31%, RRT0.65 content = 0.23%. The chromatographic purity of the product recorded in CN102002016A is greater than 99.5% and less than 0.1% of simple impurities, which is calculated by the "normalization method" different from the method of the present invention, and its detection conditions such as detection wavelength may be different from the present invention, so it is not comparable property; but the RRT3.55 content and the RRT0.65 content of the product of this step (1) are measured by the same assay method as the following product, so their results are comparable.

[0147] Step (2): Refining: Add 1000ml of ethan...

Embodiment 2

[0151] Embodiment 2: preparation febuxostat bulk drug

[0152] Add 1000ml of ethanol-acetonitrile-formic acid (100:20:5) mixture to the refining tank in advance, start stirring and add 100g of the product obtained in step (1) of Example 1 of the present invention (solvent: solute = 10 (v / w)) , heating at a temperature 10°C lower than the reflux temperature until all the solids are dissolved, then stop heating, cool down to 20-25°C, continue stirring for 10-12 hours, cool down to 0-10°C, keep stirring for 1-2 hours, Centrifuge to obtain a product that can be used as febuxostat bulk drug (the yield of such refining once is 93.3%). As determined by 【High Performance Liquid Chromatography A】, RRT3.55 content = 0.08%, RRT0.65 content = 0.06%.

Embodiment 3

[0153] Embodiment 3: preparation febuxostat bulk drug

[0154] Add 1000ml of ethanol-acetonitrile-formic acid (100:40:2) mixture to the refining tank in advance, start stirring and add 130g of the product obtained in step (1) of Example 1 of the present invention (solvent: solute = 7.7 (v / w)) , heated at reflux temperature until all the solids were dissolved, then stopped heating, cooled to 20-25°C, continued to stir for 10-12 hours, cooled to 0-5°C, kept stirring for 1-2 hours, and centrifuged to obtain non- The product of Buxostat bulk drug (94.1% of the yield of such refining once). As determined by 【High Performance Liquid Chromatography A】, RRT3.55 content = 0.11%, RRT0.65 content = 0.08%.

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Abstract

The invention relates to a drug chemical compound for gout. The drug chemical compound has the structure as shown in the following formula I. The invention further relates to a method for preparing the drug chemical compound of the formula I. The method comprises the step of using an organic solvent for refining the chemical compound of the formula I. The drug chemical compound for gout has good pharmaceutical properties.

Description

technical field [0001] The present invention relates to the technical field of medicine, relates to a xanthine oxidase inhibitor febuxostat, in particular to a pharmaceutical compound for gout, in particular to a stable febuxostat, and to The prepared pharmaceutical composition, and the preparation method of the febuxostat. The febuxostat provided by the invention has excellent pharmaceutical properties. Background technique [0002] Hyperuricemia is caused by increased uric acid production and / or decreased renal uric acid secretion, and is the most risky factor for inducing gout. The use of drugs to reduce blood uric acid concentration is one of the common methods to prevent gout, such drugs include uricosuric drugs and xanthine oxidase / xanthine dehydrogenase inhibitors that can block the absorption of uric acid by the lumen of the renal tubules . However, uricosuric drugs are contraindicated in patients with renal dysfunction, and the use of such drugs in patients with ...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426A61P19/06
Inventor 沈如杰李阅东唐建飞何海珍刘玉艳姚成娥赵福斌刘秋敏马雯霞
Owner HANGZHOU ZHUYANGXIN PHARMA
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