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Famotidine-malic acid eutectic crystal and preparation method thereof

A technology of famotidine and malic acid, which is applied in the field of co-crystal of famotidine and malic acid and its preparation, can solve the problem of only 40% to 50%, and achieve the effect of improving bioavailability

Active Publication Date: 2020-08-28
青岛市食品药品检验研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Famotidine is almost insoluble in water, and its oral bioavailability is only 40% to 50% due to low water solubility, high polarity and degradation in gastric acid

Method used

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  • Famotidine-malic acid eutectic crystal and preparation method thereof
  • Famotidine-malic acid eutectic crystal and preparation method thereof
  • Famotidine-malic acid eutectic crystal and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of eutectic

[0032] Weigh 0.3g of famotidine and add it into 100ml of methanol and sonicate (power 200W) for 30 minutes, add 0.1g of malic acid and continue to sonicate for 1 hour, leave at room temperature to precipitate a white precipitate, filter and dry to obtain famotidine-malic acid cocrystal.

Embodiment 2

[0034] Weigh 0.3g of famotidine and add it to 100ml of methanol, heat (50-70°C) and stir for 30 minutes, add 0.1g of malic acid and continue heating and stirring for 1 hour, leave it at room temperature to precipitate a white precipitate, filter and dry to obtain famotidine-apple Acid eutectic.

Embodiment 3

[0036] Weigh 0.1 g of famotidine and add it to 100 ml of acetonitrile for 30 minutes of sonication, add 0.04 g of malic acid and continue sonication for 1 hour, leave at room temperature to precipitate a white precipitate, filter and dry to obtain famotidine-malic acid cocrystal.

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Abstract

The invention discloses a famotidine-malic acid eutectic crystal and a preparation method thereof. The molar ratio of famotidine to malic acid in the eutectic crystal is 2:1. The invention also discloses the preparation method of the eutectic crystal. The famotidine-malic acid eutectic crystal provided by the invention has a characteristic melting point, an infrared spectrum, an X-ray powder diffraction pattern and the like. The eutectic crystal improves the solubility of famotidine in water, does not change the stability of famotidine under the conditions of artificial gastric juice, high temperature and high humidity, and has the potential of improving the bioavailability of famotidine. The preparation method of the famotidine-malic acid eutectic crystal is simple in step, easy to operate and good in reproducibility, and has great commercial application value.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry and crystallization technology, and in particular relates to a co-crystal of famotidine and malic acid and a preparation method thereof. Background technique [0002] Famotidine is an H2 receptor antagonist drug, which was developed in 1979. The compound patent was published in 1981, and the original researcher was VALEANT. It is clinically used for gastric and duodenal ulcers, stress ulcers, acute gastric mucosal bleeding, gastrinoma, reflux esophagitis, and Zoller-Ellison syndrome. The chemical name of famotidine is [1-amino-3-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]propylene]sulfamide, chemical structure as follows: [0003] [0004] Drug solubility is a key factor for bioavailability, so improving drug solubility is currently a major challenge for the pharmaceutical industry. Famotidine is almost insoluble in water, and its oral bioavailability is only 40% to 5...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/42C07C59/245C07C51/43A61K31/426A61K47/12A61P1/04A61P1/00A61P35/00
CPCA61K47/12A61P1/00A61P1/04A61P35/00C07B2200/13C07C51/43C07C59/245C07D277/42
Inventor 张燕周星彤蒋万枫冷萍
Owner 青岛市食品药品检验研究院
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