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Edaravone pharmaceutical co-crystal and preparation method thereof

A technology for Edaravone and drugs, which is applied in the field of preparation of new Edaravone drug co-crystals and the drug co-crystals, and can solve the problems of decreased content of Edaravone raw materials and poor stability of Edaravone, etc.

Active Publication Date: 2013-10-16
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ren Yong et al. (Chinese patent CN101953832) prepared β-cyclodextrin / edaravone inclusion compound (mass ratio 6~50:1) by β-cyclodextrin inclusion edaravone under different pH conditions. The results of light (4500±500LX) and heat (40°C) accelerated stability tests for 10 days showed that the content of non-inclusion Edaravone raw materials decreased significantly (both less than 95%), while the preparation of inclusion complexes under neutral conditions The content of edaravone in the medium is relatively stable (all greater than 96.6%), and the stability of edaravone in the clathrate prepared under acidic conditions (pH4.5) is poor (about 95.2%)

Method used

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  • Edaravone pharmaceutical co-crystal and preparation method thereof
  • Edaravone pharmaceutical co-crystal and preparation method thereof
  • Edaravone pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Accurately weigh 39.9 mg of Edaravone and 260.1 mg of β-cyclodextrin, add 6 ml of a mixed solvent of ethanol and water (volume ratio 1:7), heat to 50-80 °C, and react for 0.5 h under stirring. Stirring was stopped, the temperature was lowered naturally, and after cooling down to room temperature, crystals were precipitated after standing still for 12-24 hours, which was the Edaravone / β-cyclodextrin eutectic.

Embodiment 2

[0058] Accurately weigh 39.9 mg of Edaravone and 260.1 mg of β-cyclodextrin, add 10 ml of a mixed solvent of methanol and water (volume ratio 1:1), heat to 50-65 ° C, and react for 0.5 h under stirring. Stirring was stopped, the temperature was lowered naturally, and after cooling down to room temperature, crystals were precipitated after standing still for 12-24 hours, which was the Edaravone / β-cyclodextrin eutectic.

Embodiment 3

[0060] Accurately weigh 39.9 mg of Edaravone and 260.1 mg of β-cyclodextrin, add 8 ml of a mixed solvent of isopropanol and water (volume ratio 1:5), heat to 50-80 °C, and react for 0.5 h under stirring. Stirring was stopped, the temperature was lowered naturally, and after cooling down to room temperature, crystals were precipitated after standing still for 12-24 hours, which was the Edaravone / β-cyclodextrin eutectic.

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Abstract

The invention belongs to the technical field of organic pharmaceutical co-crystals and particularly relates to a novel edaravone pharmaceutical co-crystal and a preparation method thereof. The edaravone pharmaceutical co-crystal takes edaravone as an active ingredient of the medicine and beta-cyclodextrin as a co-crystal formation; a basic structure unit of the edaravone pharmaceutical co-crystal consists of an edaravone molecule, a beta-cyclodextrin molecule and 10.5 water molecules, wherein a carbonyl oxygen atom and an amido nitrogen atom in the edaravone molecule are taken as a hydrogen bonding acceptor and hydroxyl in the beta-cyclodextrin molecule is taken as a hydrogen bonding donor to form two different intermolecular hydrogen bonds, and the antioxygenation of the edaravone is mainly exerted through clearing free radicals and inhibiting lipid peroxidation so as to inhibit the oxidative damage of brain cells, vascular endothelial cells and nerve cells. The co-crystal prepared by the invention keeps the pharmacological activity of the edaravone, and the solubility, the stability and the bioavailability are all remarkably improved. The result of the solubility test shows that the solubility of the pharmaceutical co-crystal is 6 times that of the edaravone.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to a novel edaravone drug co-crystal and a preparation method of the drug co-crystal. [0002] Background technique [0003] Supramolecular chemistry is a science that studies molecular aggregates that are complex and orderly and have specific structures and functions formed by the association between molecules. Supramolecular chemistry has the following notable features: a. The strong binding force that forms supramolecular compounds is the result of the superposition and synergy of weak interaction forces between different molecules, and is a comprehensive expression of various forces; b. It is formed by the self-assembly of different molecules Supramolecular compounds show new functions that are completely different from the original self-assembled molecules. Its core content is molecular recognition and supramolecular self-assembly through the syne...

Claims

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Application Information

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IPC IPC(8): C07D231/26C08B37/16A61P39/06
Inventor 吴素香沈金胡秀荣
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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