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Crystal-form ilaprazole sodium and preparation method thereof

A technology of ilaprazole sodium and form, applied in the field of medicine, can solve the problems of no ilaprazole sodium crystal form, limited clinical application, rebound gastric acid secretion, etc., and achieves easy preparation, low preparation cost, solvent small amount of effect

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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  • Crystal-form ilaprazole sodium and preparation method thereof
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  • Crystal-form ilaprazole sodium and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] At 25°C, add 100 mg of ilaprazole sodium into a ball mill jar, add 1 drop of 1,4-dioxane solution, and ball mill for 20 minutes at a frequency of 20 Hz. 90 mg of light yellow crystalline powder was obtained with a yield of 90%.

Embodiment 2

[0034] At 23°C, add 107 mg of ilaprazole sodium into a ball mill jar, add 1 drop of 1,4-dioxane solution, and ball mill for 20 minutes at a frequency of 20 Hz. 95 mg of light yellow crystalline powder was obtained with a yield of 88.8%.

Embodiment 3

[0036] At 27°C, add 100 mg of ilaprazole sodium into a ball mill jar, add 1 drop of 1,4-dioxane solution, and ball mill for 20 minutes at a frequency of 20 Hz. 86mg of light yellow crystalline powder was obtained, yield 86%.

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PUM

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Abstract

The invention discloses a crystal-form ilaprazole sodium and a preparation method thereof. The novel ilaprazole sodium crystal form provided by the invention is easy to prepare, and has advantages of high purity and low 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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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14
Inventor 陈嘉媚侯雪梅鲁统部孙朋杰周月广陈剑罗兰庆李菁
Owner LIVZON PHARM GRP INC
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