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Eutectic crystal of famotidine and fumaric acid and preparation method thereof

A technology of famotidine and fumaric acid, applied in the fields of medicinal chemistry and crystallization technology, can solve the problem of oral bioavailability of only 40% to 50%, and achieve the effect of improving bioavailability

Active Publication Date: 2020-10-16
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 crystal of famotidine and fumaric acid and preparation method thereof
  • Eutectic crystal of famotidine and fumaric acid and preparation method thereof
  • Eutectic crystal of famotidine and fumaric acid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of co-crystal

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

Embodiment 2

[0034] Weigh 0.3g of famotidine, add it to 100ml of methanol, heat (50-70°C) and stir for 30 minutes, add 0.1g of fumaric 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- Fumaric 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 fumaric acid and continue sonication for 1 hour, leave it at room temperature to precipitate a white precipitate, filter and dry to obtain the famotidine-fumaric acid co-crystal.

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Abstract

The invention discloses a eutectic crystal of famotidine and fumaric acid and a preparation method thereof. The eutectic crystal is a solvate containing one molecule of methanol, and the molar ratio of famotidine to fumaric acid is 2: 1. The invention also discloses a preparation method of the eutectic crystal. The provided eutectic crystal of famotidine and fumaric acid has a characteristic melting point, an infrared spectrum, an X-ray powder diffraction pattern and the like. The solubility of famotidine in water is improved by the eutectic crystal, the stability of famotidine under high-temperature and high-humidity conditions is not changed, and the eutectic crystal has the potential of improving the bioavailability of famotidine. The preparation method of the eutectic crystal of famotidine and fumaric acid is simple in steps, easy to operate and good in reproducibility, and has a 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 fumaric 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 dru...

Claims

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Application Information

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IPC IPC(8): C07D277/42A61K31/426C07C51/43C07C57/15A61P1/04A61P35/00
CPCC07D277/42A61K31/426C07C51/43A61P1/04A61P35/00C07C57/15
Inventor 张燕冷萍周星彤
Owner 青岛市食品药品检验研究院
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