Crystal form of azilsartan and preparation method thereof

A crystal form and X-ray technology, applied in the field of azilsartan's crystal form and its preparation, can solve the problems of poor purity, poor solubility, poor stability, etc., and achieve high yield, high purity and good stability Effect

Active Publication Date: 2012-12-19
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, azilsartan has poor solubility in ethyl acetate, and the crystal form obtained by this method has low yie

Method used

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  • Crystal form of azilsartan and preparation method thereof
  • Crystal form of azilsartan and preparation method thereof
  • Crystal form of azilsartan and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0015] 2-ethoxy-1-([2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl) -Methyl benzimidazole-7-carboxylate (10g) was dissolved in methanol (727.3ml), and 62ml of 2N LiOH aqueous solution was added, then heated to reflux for 3 hours, the pH value of the solution was adjusted to 3 with 2N hydrochloric acid, and evaporated to dryness solvent. The obtained residue was distributed between water (1.2L) and chloroform (3L), then the organic layer was washed with water and dried, and the solvent was evaporated to dryness. After completely dissolving, cool to room temperature and stir to crystallize to obtain 8 g of off-white solid.

[0016] combine figure 2 , image 3 The white solid was identified as azilsartan.

[0017] combine figure 1 The crystal form X-ray diffraction diagram of the present invention is compared with the crystal form spectrum of the prior art, and it can be found that the crystal form of the present invention is a new crystal form.

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PUM

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Abstract

The invention relates to a crystal form of azilsartan shown in formula (I) and a preparation method thereof, a pharmaceutical composition containing the crystal form, and an application of the crystal form or the pharmaceutical composition in preparing anti-hypertension medicaments.

Description

technical field [0001] The invention relates to a crystal form of azilsartan and a preparation method thereof, a pharmaceutical composition containing the crystal form, and an application of the crystal form or the pharmaceutical composition thereof in preparing antihypertensive drugs. Background technique [0002] Azilsartan (English name Azilsartan) is an angiotensin II receptor antagonist drug under development for the treatment of hypertension, which selectively blocks the binding of angiotensin II to the AT1 receptor of vascular smooth muscle Blocking the vasoconstrictive effect of angiotensin II is mostly used to treat hypertension, and it is also the only angiotensin II receptor antagonist (sartan) drug currently in the late clinical stage. [0003] A preparation method of azilsartan is disclosed on page 60 of the patent CN1040755C description, which involves the precipitation method of its crystal form, that is, after the product is distributed in water and chlorofor...

Claims

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Application Information

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IPC IPC(8): C07D413/10A61K31/4245A61P9/12
Inventor 潘必高杨宝海黄龙彬吕爱锋
Owner JIANGSU HANSOH PHARMA CO LTD
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