A kind of benzbromarone crystal form a and preparation method thereof

A technology of benzbromarone and crystal form, which is applied in the field of chemical pharmaceuticals, can solve the problems of poor industrial applicability of crystallization purification methods, poor stability of drug forms, and inestimable market potential, and achieve low cost, good crystal form stability, and conditions mild effect

Active Publication Date: 2016-06-08
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 forms Poor stability, high content of related substances, poor industrial applicability of crystallization purification method

Method used

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  • A kind of benzbromarone crystal form a and preparation method thereof
  • A kind of benzbromarone crystal form a and preparation method thereof
  • A kind of benzbromarone crystal form a and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Preparation of benzbromarone crystal form A:

[0019] Take 27.5g of benzbromarone raw material and dissolve it in 90ml of acetone solvent under reflux condition at 56°C. After dissolving, the temperature is rapidly lowered, and solid is gradually precipitated. It is left to stand at 5°C for crystallization for 10 hours, filtered, and rinsed with a small amount of cold acetone. , the benzbromarone crystal form A can be obtained.

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

[0021] The infrared absorption spectrum of the obtained benzbromarone crystal form A is as follows image 3 shown.

[0022] The differential scanning calorimetry differential thermal analysis spectrum of the obtained benzbromarone crystal form A is attached Figure 4 shown.

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

[0024] Benz...

Embodiment 2

[0032] Take 27.5g of benzbromarone raw material and dissolve it in 82ml of acetone solvent at 50°C. After dissolving, the temperature is rapidly lowered, and a solid is gradually precipitated. It is left to stand at 0°C for crystallization for 2 hours, filtered, and rinsed with a small amount of cold acetone. The benzbromarone crystal form A can be obtained.

Embodiment 3

[0034] Take 27.5g of benzbromarone raw material and dissolve it in 138ml of acetone solvent at 40°C. After dissolving, the temperature is rapidly lowered, and a solid is gradually precipitated. It is left to stand at 20°C for crystallization for 15 hours, filtered, and rinsed with a small amount of cold acetone. The benzbromarone crystal form A can be obtained.

[0035] Its related substance content of the benzbromarone crystal form A obtained by the preparation method of the present invention is far less than the standard of European Pharmacopoeia 7.0 edition (1465-1466 pages), and the content of related substances is shown in Table 1.

[0036] Table 1 Comparison of benzbromarone raw material and crystal form A sample related substances with European Pharmacopoeia standards

[0037]

[0038] The solid state of benzbromarone crystal form A obtained by this preparation method has the following conditions of color and related substances after 10 days, 20 days and 30 days unde...

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PUM

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Abstract

A benzbromarone crystal form A applied in the field of chemical pharmacy and a preparation method thereof, the benzbromarone crystal form A, in the X-ray powder diffraction pattern represented by 2θ angle, the error range of the 2θ angle ± 0.2; the benzbromarone crystal form A has a basic X-ray powder diffraction pattern; the benzbromarone crystal form A has a maximum endothermic peak when the heating rate is 10°C per minute in the differential scanning calorimetry spectrum , The melting point of benzbromarone crystal form A is 152.23°C; at 25°C, take 1.0g of benzbromarone crystal form A, add 10ml of chloroform, all the solids are dissolved, and the solution is clear; and take 1.25g of benzbromarone crystal form A, Add 25ml of N,N-dimethylformamide, the solid is slightly insoluble, and the solution is not clear; the crystal form A of benzbromarone is obtained by crystallization from a single solvent, acetone. The invention has good crystal form stability, simple preparation method, low cost, simple post-treatment, high purity of the prepared product and less related substances.

Description

technical field [0001] The invention relates to a benzbromarone crystal form A in the field of chemical pharmacy and a preparation method thereof. Background technique [0002] Benzbromarone, also known as Benzbromone, Gout Lixian, Gout Ning, etc. This product is a benzofuran derivative, which has the effect of inhibiting the reabsorption of uric acid by the renal tubules, thereby reducing the concentration of uric acid in the blood. It is easily absorbed by oral administration, 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. Used to treat gout. [0003] Benzbromarone was launched in Germany in 1971, licensed under the trade name Urinorm in August 1978, and sold in tablets from April 1979. Benzbromarone has occupied the first place in the hospital for anti-gout drugs since it entered my country in 2000. Moreover, the market share of benzbromarone is still on the rise, and its mar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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陈静白跃飞
Owner NORTHEAST PHARMA GRP
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