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Crystalline Ilaprazole sodium ethylate and preparation method thereof

A technology of ilaprazole sodium and ethanolate, applied in the field of medicine, achieves the effects of good reproducibility, less impurities and easy control

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

AI Technical Summary

Problems solved by technology

[0006] However, the stability and bioavailability of the drug need to be further improved.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Dissolve solid NaOH in ethanol to form a solution with a pH of about 11. Add the solution to dichloromethane to adjust the alkalinity to about pH 10. The volume ratio of dichloromethane to ethanol is 10:1. 100 mg of ilaprazole sodium was dissolved in the solution to prepare a saturated solution, filtered, and placed in a fume hood to evaporate at room temperature. One day later, 85 mg of light yellow needle-shaped single crystals were obtained, with a yield of 85%.

Embodiment 2

[0034] Dissolve solid NaOH in ethanol to form a solution with a pH of about 11. Add the solution to dichloromethane to adjust the alkalinity to about pH 10. The volume ratio of dichloromethane to ethanol is 10:1. At room temperature, 100 mg of ilaprazole sodium was dissolved in the solution to prepare a saturated solution, filtered, and the solution was drained by a vacuum pump to obtain 90 mg of white powder with a yield of 90%.

Embodiment 3

[0036] In this example, the crystalline ilaprazole sodium ethanolate prepared in Example 1 was measured and characterized, as follows.

[0037] Adopt Bruker D8 Advance diffractometer to measure the powder diffraction pattern of the crystalline ilaprazole sodium ethanolate that obtains in embodiment 1, measurement condition is as follows: Cu K α, 40kV, 40mV is light source, step-size 0.018 °, scanning speed 4 ° / min, scanning range 5-35°, room temperature, in its powder X-ray diffraction pattern, there are diffraction peaks at the following 2θ diffraction angles: 5.914, 7.479, 9.143, 10.89, 10.902, 14.185, 14.97, 14.991, 15.574, 16.174 , 18.674, 18.754, 20.851, 21.88, 22.668, 23.593, 23.602, 23.646, 23.654, 24.478, 24.53, 24.552, 25.024, 25.034, 25.179, 26.01, 26.222, 28.282, 30. figure 1 shown. Expressed in terms of interplanar distance d, Bragg angle (2θ) and percentage I of relative intensity, as follows:

[0038]

[0039]

[0040] The crystal structure of the crysta...

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Abstract

The invention provides a crystalline Ilaprazole sodium ethylate and a preparation method thereof. The X ray powder diffraction spectrum of the crystalline Ilaprazole sodium ethylate provided by the invention includes diffraction peaks represented by the following 2 theta angles: 5.9 degrees + / - 0.1 degree, and 10.8 degrees + / - 0.1 degree. The crystalline Ilaprazole sodium ethylate provided by the invention has high crystal purity. In addition, the method provided in the invention for preparation of the crystalline Ilaprazole sodium ethylate has the advantages of simple operation, mild reaction conditions, easy control, low production cost, definite obtaining of the target product crystal with good repeatability, fewer introduced impurities, and significantly improves the bioavailability of drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a crystalline ilaprazole sodium alcoholate 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...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61P1/04
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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