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Dexlansoprazole-isonicotine eutectic and application of eutectic

A technology of dexlansoprazole and isonicotine, applied in the direction of medical preparations containing active ingredients, digestive system, organic active ingredients, etc. Poor stability and other problems, to achieve the effect of high crystal purity, excellent crystal stability and high repeatability

Active Publication Date: 2017-06-13
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, dexlansoprazole has very poor water solubility, and is sensitive to light, heat, and humidity. Therefore, it is looking for its new crystal form, hydrate, solvate, salt or cocrystal to improve these properties of dexlansoprazole. Shortcomings have always been an international research hotspot

Method used

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  • Dexlansoprazole-isonicotine eutectic and application of eutectic

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Example 1 Dissolve 144 mg of dexlansoprazole and about 50 mg of isonicotine (molar ratio 1:1) in 2 to 3 mL of acetonitrile solvent, heat to 40°C, and use an organic nylon head with a filter pore size of about 0.22 μm After filtration, the two solutions were mixed, left to stand at room temperature for 24 hours to evaporate, then filtered, and vacuum-dried at room temperature for 24 hours to obtain 134 mg of a white blocky solid with a yield of about 69%.

Embodiment 2

[0035] Example 2 Dissolve 295 mg of dexlansoprazole and about 50 mg of isonicotine (molar ratio: 2:1) in 2 to 3 mL of acetonitrile solvent, heat to 40°C, and use an organic nickel with a filter pore size of about 0.22 μm. After the faucet was filtered, the two solutions were mixed, left to stand at room temperature for 24 hours to evaporate, then filtered, and vacuum-dried at room temperature for 24 hours to obtain 180 mg of a white blocky solid with a yield of about 52%.

Embodiment 3

[0036] Example 3 Dissolve 142mg of dexlansoprazole and about 98mg of isonicotine (molar ratio: 1:2) in 2-3mL of acetonitrile solvent respectively, heat to 40°C, and use organic nickel with a filter pore diameter of about 0.22μm After the faucet was filtered, the two solutions were mixed, left to evaporate at room temperature for 24 hours, then filtered, and vacuum-dried at room temperature for 24 hours to obtain 159 mg of white blocky solid, with a yield of about 66%.

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Abstract

The invention discloses dexlansoprazole-isonicotine eutectic and application of the eutectic. The eutectic is a crystalline complex combined by dexlansoprazole and isonicotine at a mole ratio of 1:1 in a non-covalent form; an X-ray powder diffraction spectrum of the eutectic comprises diffraction peaks expressed by the following 2 theta angles: 5.3-5.5 degrees, 10.7-10.9 degrees, 12.8-13.0 degrees, 14.9-15.1 degrees, 16.1-16.3 degrees, 18.4-18.6 degrees, 19.1-19.3 degrees, 19.9-20.1 degrees, 22.0-22.2 degrees, 22.6-22.8 degrees, 24.3-24.5 degrees, 25.8-26.0 degrees, 26.2-26.4 degrees, 27.0-27.2 degrees, 27.4-27.6 degrees, 31.4-31.6 degrees and 32.5-32.7 degrees. Compared with the prior art, the dexlansoprazole-isonicotine eutectic is excellent in crystal form stability and high in bioavailability, and has greater maximum apparent solubility in ultrapure water; a preparation method of the dexlansoprazole-isonicotine eutectic is simple, mild in condition and high in repeatability; a product can be conveniently, quickly and stably obtained; the crystal form purity of the product is high; obvious raw material impurities and residual solvents do not exist.

Description

technical field [0001] The invention relates to a co-crystal of dexlansoprazole, in particular to a co-crystal of dex-lansoprazole-isonicotine, its preparation method and application. Background technique [0002] Lansoprazole, chemical name 2-[[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzimidazole, The English name Lansoprazole is the world's second proton pump inhibitor drug developed by Takeda Corporation of Japan in 1991, and it was officially put on the market in early 1992. As a proton pump inhibitor, it acts on the H of gastric parietal cells + -K + -ATPase, which makes H in parietal cells + It cannot be transported to the stomach, so the amount of gastric acid in the gastric juice is greatly reduced. It is clinically used for the treatment of duodenal ulcer, gastric ulcer, reflux esophagitis, and Zoller-Ellison syndrome (gastrinoma). Significantly, it has an inhibitory effect on Helicobacter pylori. On January 30, 2009, the U.S. FDA app...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D213/81A61K31/4439A61P1/04
CPCC07B2200/13C07D213/81C07D401/12
Inventor 张海禄李健慧汪莲艳付雪邓宗武
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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