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Eutectic of famotidine and adipic acid and preparation method thereof

A technology of famotidine and adipic acid, which is applied in the field of co-crystal of famotidine and adipic acid and its preparation, can solve the problems of oral bioavailability of only 40% to 50%, and improve the bioavailability degree of effect

Active Publication Date: 2021-08-10
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%~50% due to low water solubility, high polarity and degradation in gastric acid

Method used

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  • Eutectic of famotidine and adipic acid and preparation method thereof
  • Eutectic of famotidine and adipic acid and preparation method thereof
  • Eutectic of famotidine and adipic acid and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0028] Embodiment 1: Preparation of eutectic

[0029] Weigh 0.3g of famotidine and add it to 100ml of methanol and sonicate (power 200W) for 30 minutes, add 0.1g of adipic acid and continue to sonicate for 1 hour, leave it at room temperature to precipitate a white precipitate, filter and dry to obtain famotidine-adipic acid co- crystal.

Embodiment 2

[0031] Weigh 0.3g of famotidine and add it into 100ml of methanol, heat (50-70°C) and stir for 30 minutes, add 0.1g of adipic 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- Adipic acid eutectic.

Embodiment 3

[0033] Weigh 0.1 g of famotidine and add it to 100 ml of acetonitrile for 30 minutes of sonication, add 0.04 g of adipic acid and continue sonication for 1 hour, leave at room temperature to precipitate a white precipitate, filter and dry to obtain famotidine-adipic acid co-crystal.

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Abstract

The invention discloses a famotidine and adipic acid eutectic crystal and a preparation method thereof. The eutectic crystal is a hydrate containing one molecule of water, and the molar ratio of famotidine to adipic acid is 2: 1. The invention also discloses a preparation method of the eutectic crystal. The famotidine-adipic acid eutectic crystal provided by the invention has a characteristic melting point, an X-ray powder diffraction pattern and the like. According to the eutectic crystal, the solubility of famotidine in water is improved, the stability of famotidine under high-temperature and high-humidity conditions is improved, and the eutectic crystal has the potential of improving the bioavailability of famotidine. The preparation method of the famotidine-adipic 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 adipic acid and a preparation method thereof. Background technique [0002] Famotidine is an H2 receptor antagonist drug, clinically used for gastric and duodenal ulcers, stress ulcers, acute gastric mucosal bleeding, gastrinoma, reflux esophagitis and Zoller-Ellison syndrome, etc. . The chemical name of famotidine is [1-amino-3-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]propylene]sulfamide. [0003] 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%-50% due to its low water solubility, high polarity and degradation in gastric acid. The main advantage of drug co-crystal as an important means to improve drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/42C07C55/14C07C51/43A61K31/426A61P1/04A61P35/00
CPCC07D277/42C07C55/14C07C51/43A61P1/04A61P35/00C07B2200/13
Inventor 不公告发明人
Owner 青岛市食品药品检验研究院
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