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Crystallization-type ilaprazole sodium and preparation method thereof

A technology of ilaprazole sodium and crystal form, applied in the field of new crystal form of ilaprazole sodium and its preparation, can solve the problem that there is no crystal form of ilaprazole sodium, limited clinical application, rebound of gastric acid secretion, etc. problem, to achieve the effect of easy preparation, low preparation cost and less solvent

Active Publication Date: 2012-10-24
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The first-generation PPIs have limited clinical application because they can cause delayed gastric emptying, parietal cell swelling, and significant gastric acid secretion rebound after drug withdrawal
There is no report on the crystal form of ilaprazole sodium

Method used

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  • Crystallization-type ilaprazole sodium and preparation method thereof
  • Crystallization-type ilaprazole sodium and preparation method thereof
  • Crystallization-type ilaprazole sodium and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] At 25°C, take 49mg of ilaprazole sodium in a beaker, add 0.18mL of n-propanol and stir to dissolve. After 1 hour, the solvent evaporates completely, and then vacuum-dry. 48 mg of off-white crystalline powder was obtained, with a yield of 98%.

Embodiment 2

[0035] At 25°C, take 49mg of ilaprazole sodium in a beaker, add 0.18mL of n-propanol and stir to dissolve. After 1 hour, the solvent evaporates completely, and then vacuum-dry. 46.2 mg of off-white crystalline powder was obtained, with a yield of 96%.

Embodiment 3

[0037] At 30°C, take 115 mg of ilaprazole sodium in a test tube, add 0.3 mL of n-propanol to prepare a supersaturated solution, sonicate for 1 hour, filter, and vacuum dry. 71 mg of off-white crystalline powder was obtained, with a yield of 61.7%.

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PUM

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Abstract

The invention discloses a crystallization-type Ilaprazole sodium and a preparation method thereof. The Ilaprazole sodium with a novel crystalline form provided by the invention is easy to prepare, high in purity and low in impurity content. The preparation method provided by the invention needs low solvent amount, has advantages of low production cost, simple operation and mild reaction condition, is easy to control, and can produce the target product crystalline form doubtlessly and well-repeatedly.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new crystal form of ilaprazole sodium and a preparation method thereof. Background technique [0002] The structure of Ilaprazole (Ilaprazole) belongs to the benzimidazole class and is an irreversible proton pump inhibitor. After oral administration, ilaprazole selectively enters the gastric parietal cells and converts into the active metabolite of sulfenamide, which interacts with H + 、K + -The sulfhydryl group on the ATPase acts to form a disulfide bond and irreversibly inhibits H + 、K + -ATPase, which produces the effect of inhibiting gastric acid secretion. [0003] First-generation PPIs have limited clinical application because they can cause delayed gastric emptying, parietal cell swelling, and apparent rebound of gastric acid secretion after drug withdrawal. Ilaprazole, as one of the new generation of proton pump inhibitors (PPI), has overcome some of the defects of the origin...

Claims

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Application Information

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IPC IPC(8): C07D401/14
Inventor 周月广孙朋杰鲁统部陈嘉媚侯雪梅曾创叶剑轩李菁
Owner LIVZON PHARM GRP INC
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