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Benzbromarone of crystal form B, and its preparation method

A technology of benzbromarone and crystal form, applied in the field of chemical pharmacy, can solve the problems of poor industrial application of crystallization and purification method, inestimable market potential, poor stability of drug form, etc., and achieves low cost, mild conditions and good stability. Effect

Active Publication Date: 2015-01-28
NORTHEAST PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since Benzbromarone entered my country in 2000, it has occupied the No. 1 position of anti-gout drugs in hospitals. Moreover, the market share of Benzbromarone is still on the rise, and its market potential is hard to estimate
[0004] Through the search of Chinese patents, it is found that most of the existing patents are the protection of the preparation method of benzbromarone synthesis or different dosage forms and uses. After searching the literature and domestic and foreign patents, no reports about the crystal form of benzbromarone have been found, and the existing drug form is stable. Poor performance, high content of related substances, poor industrial applicability of crystallization purification method

Method used

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  • Benzbromarone of crystal form B, and its preparation method
  • Benzbromarone of crystal form B, and its preparation method
  • Benzbromarone of crystal form B, and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation method of benzbromarone crystal form B sample:

[0019] Take 7.2g of benzbromarone raw material and dissolve it completely in 65ml of acetone solvent at a temperature of 22°C, then add 93.6ml of water, gradually solids are precipitated, stand at 5°C for crystallization for 10 hours, filter with suction, and use a small amount of cold water Wash with acetone to obtain a sample of benzbromarone crystal form B.

[0020] The powder X-ray diffraction pattern of gained benzbromarone crystal form B is as attached figure 2 shown.

[0021] The infrared absorption spectrum figure of gained benzbromarone crystal form B is as attached image 3 shown.

[0022] The differential scanning calorimetry differential thermal analysis spectrum of gained benzbromarone crystal form B is as attached Figure 4 shown.

[0023] The detection method and result of differential scanning calorimetry differential thermal analysis spectrum are as follows:

[0024] Benzbromarone (6...

Embodiment 2

[0038] Take 7.2g of benzbromarone raw material and completely dissolve it in 87ml of acetone solvent at a temperature of 30°C, then add 134ml of water, gradually a solid precipitates, stand at 0°C for crystallization for 2 hours, filter with suction, and use a small amount of cold acetone The sample of benzbromarone crystal form B can be obtained by rinsing.

Embodiment 3

[0040] Take 7.2g of benzbromarone raw material and completely dissolve it in 108ml of acetone solvent at a temperature of 20°C, then add 180ml of water, gradually solids are precipitated, stand at 20°C for crystallization for 15 hours, filter with suction, and use a small amount of cold acetone The sample of benzbromarone crystal form B can be obtained by rinsing.

[0041] The content of related substances of the benzbromarone crystal form B obtained by the preparation method of the present invention is far less than the standard of European Pharmacopoeia Version 7.0 (page 1465-1466), and the contents of related substances are shown in Table 1.

[0042] Table 1 Comparison of related substances of benzbromarone raw materials and crystal form B samples with European Pharmacopoeia standards

[0043]

[0044] The benzbromarone crystal form B state solid obtained by this preparation method is subjected to 92.5% humidity, light, and high temperature conditions of 60° C. for 10 da...

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Abstract

The invention relates to benzbromarone of crystal form B applied in the field of chemical pharmacy, and its preparation method. In the X-ray powder diffraction pattern represented by 2theta angles of the benzbromarone of crystal form B, the error range of the 2theta angles is + / -0.2, and the benzbromarone of crystal form B has a basic X-ray powder diffraction pattern; and in the differential scanning calorimetry pattern of the benzbromarone of crystal form B, a maximum endothermic peak exists when the heating speed is 10DEG C / min, and the maximum endothermic peak begins at 150.54DEG C, reaches the top at 151.62DEG C and ends at 153.82DEG C, the melting point is 151.66DEG C; when 10ml of trichloromethane is added to 1.0g of the benzbromarone of crystal form B at 25DEG C, a very small amount of the benzbromarone of crystal form B is not dissolved, and the obtained solution is not clear; and 25ml of N,N-dimethyl formamide is added to the 1.25g of benzbromarone of crystal form B, the benzbromarone of crystal form B is complete dissolved, and the obtained solution is clear. The benzbromarone of crystal form B has good stability, and the preparation method has the advantages of simplicity, low cost, simple post-treatment, high product purity and few relevant substances.

Description

technical field [0001] The invention relates to a benzbromarone crystal form B in the field of chemical pharmacy and a preparation method thereof. Background technique [0002] Benzbromarone, also known as benzobromone, tongfenglixian, tongfengning, etc. This product is a derivative of benzofuran, which can inhibit the reabsorption of uric acid by renal tubules and thus reduce the concentration of uric acid in blood. It is easily absorbed orally, and its metabolites are effective. The uric acid in the blood 24 hours after taking the medicine is 66.5% of that before taking the medicine. For the treatment of gout. [0003] Benzbromarone was launched in Germany in 1971, licensed under the trade name of Urinorm in August 1978, and started selling tablets in April 1979. Since Benzbromarone entered my country in 2000, it has occupied the No. 1 position of anti-gout drugs in hospitals. Moreover, the market share of Benzbromarone is still on the rise, and its market potential is ...

Claims

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Application Information

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IPC IPC(8): C07D307/80
CPCC07B2200/13C07D307/80
Inventor 祝春艳胡铁军李想何艳艳刘素娜阎欢赵会白跃飞
Owner NORTHEAST PHARMA GRP
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