Esomeprazole magnesium trihydrate and preparation method thereof

A technology of esomeprazole magnesium trihydrate and esomeprazole sodium, applied in the field of esomeprazole magnesium trihydrate, can solve the problem of undisclosed esomeprazole magnesium quality data and unstable quality , the rapid growth of impurities and other problems, to achieve the effect of stable properties, high chemical and optical purity, and high yield

Active Publication Date: 2014-01-15
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This application does not disclose the quality data of the final product esomeprazole magnesium, and the esomeprazole magnesium in amorphous form prepared by the present inventor with reference to its embodiment 3 ~ 5 disclosed method, after tes

Method used

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  • Esomeprazole magnesium trihydrate and preparation method thereof
  • Esomeprazole magnesium trihydrate and preparation method thereof
  • Esomeprazole magnesium trihydrate and preparation method thereof

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Embodiment 1

[0059] The preparation of embodiment 1 esomeprazole sodium

[0060] Raw materials: esomeprazole is commercially available, chemical purity 97%, optical purity 98%

[0061] Dissolve 2.6kg (7.54mol) of esomeprazole in 1.2L of ethyl acetate, then add 3.6L of acetone, then add 212.0g (5.28mol) of sodium hydroxide solid, stir and crystallize to obtain esomeprazole Sodium solid 1.564kg, yield 56.5%, chemical purity 99.83%, optical purity 99.91%.

Embodiment 2

[0062] The preparation of embodiment 2 esomeprazole sodium

[0063] Raw materials: esomeprazole is commercially available, chemical purity 97%, optical purity 98%

[0064] Dissolve 2.6kg (7.54mol) of esomeprazole in 1.05L of ethyl acetate, then add 2.6L of acetonitrile, then add 302g (7.54mol) of solid sodium hydroxide, stir and crystallize to obtain esomeprazole sodium The solid is 1.785kg, the yield is 64.5%, the chemical purity is 99.88%, and the optical purity is 99.94%.

Embodiment 3

[0065] The preparation of embodiment 3 esomeprazole sodium

[0066] Raw materials: esomeprazole is commercially available, chemical purity 97%, optical purity 98%

[0067] Dissolve 5.0kg (14.5mol) of esomeprazole in 2.5L of methyl isobutyl ketone, then add 11.0L of acetonitrile, then add 522g (13.05mol) of sodium hydroxide solid, stir and crystallize to obtain esomeprazole Sodium azole solid 4.05kg, yield 74.5%, chemical purity 99.90%, optical purity 99.92%.

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Abstract

The invention relates to amorphous esomeprazole magnesium trihydrate, pharmaceutical compositions containing the amorphous esomeprazole magnesium trihydrate, and a preparation method of the amorphous esomeprazole magnesium trihydrate. The amorphous esomeprazole magnesium trihydrate is alpha-radiated by CuK, wherein X-ray powder diffraction pattern has broad peaks at parts that 2theta is 7+-1 degree and 18+-1 degree; according to peak intensity of broad peaks at parts that 2theta is 18+-1 degree being 100%, peak intensity ratios of the broad peaks at parts that 2theta is 7+-1 degree is larger than 50% and smaller than 100%. The esomeprazole magnesium trihydrate has advantages of high chemical and optical purity, stable properties, simple and controllable preparation method, and high yield, and is suitable for large scale production.

Description

technical field [0001] The invention relates to an amorphous form of esomeprazole magnesium trihydrate, a pharmaceutical composition containing it, and a preparation method thereof. Background technique [0002] Esomeprazole magnesium belongs to the class of proton pump inhibitors (proton pump inhibitors, PPIs) drugs, developed by AstraZeneca, the chemical name is bis-S-5-methoxy-2-[(4-methoxy -3,5-Dimethyl-2-pyridyl)methyl]sulfinyl-1H-benzimidazole magnesium, the listed product is its trihydrate, as shown in its structural formula 1: [0003] [0004] 1 . [0005] Proton pump inhibitors are used in the treatment of acid-related diseases, and they are widely used clinically and have the best curative effect in the past decade. PPIs are H + / K + -ATPase inhibitors, which mainly act on the final stage of gastric acid secretion, block intracellular H driven by proton pumps in gastric parietal cells + K + exchange. Compared with the gastric acid-suppressing drug-H2 rec...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61P1/04
CPCC07D401/12
Inventor 史颖周付刚刘洋张雅然马玉秀雷亚丽赵继全
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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