4.6 Article

Syntheses, structure characterization and dissolution of two novel cocrystals of febuxostat

期刊

JOURNAL OF MOLECULAR STRUCTURE
卷 1130, 期 -, 页码 480-486

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ELSEVIER
DOI: 10.1016/j.molstruc.2016.10.044

关键词

Febuxostat; Cocrystal; Syntheses; Structure; Dissolution

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Febuxostat was investigated due to its significant effect in the treatment of gout. However, its poor water solubility hinder its potential applications. In recent years, cocrystals have increasingly being applied to enhance the drug solubility. To improve the solubility, two cocrystals of Febuxostat were synthesized through the method of cooling crystallization. The prepared cocrystals febuxostat-isonicotinamide(FEB-INA) and febuxostat-arginine(FEB-Arg) were studied by microscopical observation, Powder X-Ray Diffraction(PXRD), Single Crystal X-ray Diffraction, Differential Scanning Calorimetry(DSC), and infrared spectrometry. At the same time, the cocrystals' solubility and dissolution rate were explored. Both the cocrystals showed higher solubility compared to the pure drug. The FEB-Arg cocrystal enhanced about 900 times of solubility compared to the pure drug. The current study proved that cocrystallization can be a better way to enhance the solubility of the poorly water-soluble drug. (C) 2016 Elsevier B.V. All rights reserved.

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