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Ilaprazole sodium crystal form and preparation method thereof

A technology of ilaprazole sodium and its crystal form, which is applied in the field of ilaprazole sodium new crystal form and its preparation, and can solve the problems of no ilaprazole sodium crystal form, limited clinical application, gastric acid secretion rebound, etc. problems, to achieve the effect of easy preparation, low preparation cost, and less amount of 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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  • Ilaprazole sodium crystal form and preparation method thereof
  • Ilaprazole sodium crystal form and preparation method thereof
  • Ilaprazole sodium crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] at 25°C with CH 2 Cl 2 : a mixed solution of methanol=10:1 (volume ratio), 5.5 mL of which was added dropwise with 1 drop of triethylamine, 300 mg of ilaprazole sodium was added to the solution, stirred to dissolve, filtered, and the filtrate was placed in a fume hood to volatilize. After a few hours, the solvent evaporated completely and dried under vacuum. 282 mg of pale yellow crystalline powder were obtained with a yield of 94%.

Embodiment 2

[0036] at 25°C with CH 2 Cl 2 : methanol=10:1 (volume ratio) mixed solution, 1 mL of which was added dropwise with 1 drop of triethylamine, 60 mg of ilaprazole sodium was added to the solution, stirred and dissolved, filtered, and the filtrate was placed in a fume hood to volatilize, and several After 1 hour, the solvent evaporated completely, and vacuum-dried. 55 mg of pale yellow crystalline powder were obtained, with a yield of 91.7%.

Embodiment 3

[0038] at 27°C with CH 2 Cl 2 : a mixed solution of methanol=10:1 (volume ratio), 5.5 mL of which was added dropwise with 1 drop of triethylamine, 300 mg of ilaprazole sodium was added to the solution, stirred to dissolve, filtered, and the filtrate was placed in a fume hood to volatilize. After a few hours, the solvent evaporated completely and dried under vacuum. 272 mg of pale yellow crystalline powder were obtained with a yield of 91%.

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Abstract

The invention discloses an ilaprazole sodium crystal form 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] Ilaprazole belongs to benzimidazoles and is an irreversible proton pump inhibitor. After oral administration, ilaprazole selectively enters gastric parietal cells and is converted into the active metabolite of sulfenamide, which interacts with H + , K + -Sulfhydryl action on ATPase, forming covalent binding of disulfide bonds, irreversibly inhibiting H + , K + -ATPase, 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 a significant rebound in gastric acid secretion after drug withdrawal. As one of the new generation of proton pump inhibitors (PPI), ilaprazole has overcome some of the defects of the original similar products to varying de...

Claims

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Application Information

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IPC IPC(8): C07D401/14
Inventor 孙朋杰鲁统部侯雪梅陈嘉媚周月广王祥红毛文金李菁
Owner LIVZON PHARM GRP INC
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