Method for preparing amorphous zafirlukast solid

An amorphous, solid technology, applied in the direction of organic chemistry, can solve the problems of poor yield, complex process, high conditions, achieve good dissolution properties, simplify the production process, and avoid the effects of micronization

Inactive Publication Date: 2011-09-28
北京京卫燕康药物研究所有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] An object of the present invention is to solve the problem that the preparation of amorphous zafirlukast in the above-mentioned prior art needs to be transformed through monohydrate crystals, and high temperature above 100°C is required, the process is complex, the required conditions are high, the yield is poor, and the prepared Amorphous zafirlukast still needs to be improved in terms of dissolution rate, and micronization treatment is required to provide a simple and efficient amorphous zafirlukast product with more obvious advantages in dissolution rate preparation method

Method used

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  • Method for preparing amorphous zafirlukast solid
  • Method for preparing amorphous zafirlukast solid
  • Method for preparing amorphous zafirlukast solid

Examples

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Effect test

Embodiment 1

[0024] Example 1 Preparation of amorphous zafirlukast method 1

[0025] Put 10g of zafirlukast in a 250ml round-bottomed flask, add 50ml of acetone, stir at room temperature until fully dissolved, and then vacuumize to 2.65×10 on a rotary evaporator with a water pump 3 Pa. Soak the flask in a water bath preheated to 40°C, evaporate to complete dryness, and scrape off the product after cooling to obtain amorphous zafirlukast in the form of white powder.

Embodiment 2

[0026] Example 2 Preparation of amorphous zafirlukast method 2

[0027] Put 10g of zafirlukast in a 250ml round-bottomed flask, add 50ml of acetonitrile, stir at room temperature until completely dissolved, and then vacuumize to 2.65×10 on a rotary evaporator with a water pump. 3 Pa, immerse the flask in a water bath preheated to 40°C, evaporate to complete dryness, and scrape off the product after cooling to obtain amorphous zafirlukast in the form of white powder.

Embodiment 3

[0028] Example 3 Preparation of amorphous zafirlukast method 3

[0029] Put 10g of zafirlukast in a 250ml round-bottomed flask, add 50ml of 1,4-dioxane, stir at room temperature until fully dissolved, and then pump vacuum to 2.65×10 on the rotary evaporator 3 Pa, immerse the flask in a water bath preheated to 30°C, evaporate to complete dryness, heat up to 60°C for 1 hour, and use an oil pump to evacuate to 1×10 2 Pa, heated to 80°C for 1 hour. The product was scraped off after cooling to obtain amorphous zafirlukast as a white powder.

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Abstract

The invention relates to amorphous zafirlukast, in particular to a method for preparing amorphous N-[4-[5-(cyclooxycarbonyl)amino-1-methylindole-3-yl-methyl]-3-methoxybenzoyl]-2-methyl benzene sulphonamide, and belongs to the field of medicine preparation. The invention solves the problems that monohydrate crystal conversion and high temperature of over 100DEG are needed, the process is complicated, the requirements are high, the yield is low, the dissolution of the prepared amorphous zafirlukast is needed to be improved, the prepared amorphous zafirlukast is needed to be micronized and the like in the prior art for preparing the amorphous zafirlukast. The invention provides a simple and high-efficiency method for preparing the amorphous zafirlukast with more obvious advantage on the dissolution. The method comprises the following steps of: dissolving zafirlukast in an organic solvent, and removing the organic solvent to obtain the amorphous zafirlukast solid. The preparation method is simple and high-efficiency, and the product has good dissolution and is suitable to be promoted and applied.

Description

technical field [0001] The present invention relates to amorphous zafirlukast, namely amorphous N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-ylmethyl]-3-methoxybenzene The invention discloses a preparation method of formyl]-2-methylbenzenesulfonamide, which belongs to the field of medicine preparation. Background technique [0002] N-[4-[5(cyclopentyloxycarbonyl)amino-1-methylindol-3-ylmethyl]-3-methoxybenzoyl]-2-methylbenzenesulfonamide, common name Zha Lukast, trade name Encore, as a leukotriene receptor antagonist of polypeptide LTC4, LTD4, LTE4 and other hypersensitive slow-response substances, competitively inhibits leukotriene activity and effectively prevents leukotriene Peptide-induced airway edema caused by increased vascular permeability, while inhibiting the infiltration of airway eosinophils produced by leukotriene peptides, reducing tracheal constriction and inflammation, and reducing asthma symptoms. This product is highly selective and only acts on ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/24
Inventor 王德平王宾张严源
Owner 北京京卫燕康药物研究所有限公司
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