Crystalline Ilaprazole sodium hydrate and preparation method thereof

A technology of ilaprazole sodium and its crystalline form, which is applied in the field of crystalline ilaprazole sodium hydrate and its preparation, achieving the effects of easy control, good storage stability, and high purity of the crystalline form

Active Publication Date: 2013-07-17
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, the stability and bioavailab

Method used

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  • Crystalline Ilaprazole sodium hydrate and preparation method thereof
  • Crystalline Ilaprazole sodium hydrate and preparation method thereof
  • Crystalline Ilaprazole sodium hydrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] First put 33% aqueous sodium hydroxide solution on the lower layer of the test tube, dissolve 100 mg of ilaprazole in isopropanol to prepare a saturated solution, and then carefully add the solution dropwise to the upper layer of the test tube (v / v 1:1) , standing at room temperature for liquid-liquid diffusion for about a week, to obtain 80 mg of pale yellow needle-like crystals, with a yield of 80%.

Embodiment 2

[0038] Dissolve 100 mg of ilaprazole sodium in alkaline isopropanol at 40°C and pH 11 to make a saturated solution, filter, and slowly cool down to 4°C. After 12 hours, 86 mg of light yellow needle-shaped crystals were obtained, with a yield of 86%.

Embodiment 3

[0040] At room temperature, 100 mg of ilaprazole sodium was dissolved in isopropanol to make a saturated solution. At room temperature, the solution was placed in an isopropyl ether atmosphere for gas-liquid diffusion. After 24 hours, 85 mg of light yellow needle-shaped crystals were obtained, producing rate of 85%.

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Abstract

The invention provides a crystalline Ilaprazole sodium hydrate and a preparation method thereof. An X ray powder diffraction spectrum of the crystalline Ilaprazole sodium hydrate provided by the invention includes diffraction peaks represented by the following 2 theta angles: 5.9 degrees +/- 0.1 degree, 25.4 degrees +/- 0.1 degree and 10.7 degrees +/- 0.1degree. The crystalline Ilaprazole sodium hydrate provided in the invention has high crystal purity. In addition, the method provided in the invention for preparation of the crystalline Ilaprazole sodium hydrate has the advantages of simple operation, mild reaction conditions, easy control, low production cost, definite obtaining of a target product crystal with good repeatability, less introduction of impurities, and significantly improves drug bioavailability.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a crystalline ilaprazole sodium hydrate and a preparation method thereof. Background technique [0002] The structure of Ilaprazole (Ilaprazole) belongs to the class of benzoimazoles and is an irreversible proton pump inhibitor. After oral administration, ilaprazole selectively enters the parietal cells of the stomach and is transformed into an active metabolite of sulfenamide, which interacts with the sulfhydryl group on the H+, K+-ATPase to form a covalent combination of disulfide bonds, irreversibly inhibiting 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...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61K31/4439A61P1/04
Inventor 郑赛利陈嘉媚鲁统部侯雪梅毛文金周月广曾创
Owner LIVZON PHARM GRP INC
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