难水溶性药物非布司他的固体分散体系:制备、表征和优化

Q4 Pharmacology, Toxicology and Pharmaceutics
Mangirish N. Deshpande, Shruti S. Dessai, Pearl Dighe
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引用次数: 0

摘要

非布司他是一种低溶性药物,用于治疗高尿酸血症和痛风。本研究旨在采用溶剂蒸发法,利用固体分散技术,在不同聚合物(β -环糊精、Soluplus®、HPMC E5和Kolliphor®p407)的辅助下,提高非布司他在不同药物载体比中的溶解度。对固体分散体的物理外观、收率、药物含量、饱和溶解度和溶解性进行了评价。该研究的饱和溶解度数据表明,与纯药物相比,固体分散体的溶解度有所增加。体外释放谱显示,药物与Kolliphor®p407比例为1:9的制剂SD20溶出率最高。粉末的x射线衍射研究和扫描电子显微镜(SEM)显示了固体弥散的结晶到非晶转变。研究表明,固体分散体是提高非布司他溶解度和生物利用度的有效技术。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
SOLID DISPERSION SYSTEMS OF POORLY WATER SOLUBLE DRUG FEBUXOSTAT: PREPARATION, CHARACTERIZATION AND OPTIMIZATION
Febuxostat is a poor soluble drug used in the management of hyperuricemia and gout. The present study aims at increasing the solubility of febuxostat by solid dispersion technique with the aid of various polymers (Beta cyclodextrin, Soluplus®, HPMC E5, and Kolliphor® P 407) in various drug: carrier ratios employing the solvent evaporation method. Solid dispersions were evaluated for physical appearance, percentage yield, drug content, saturation solubility and dissolution properties. Saturation solubility data of the study depict an increased solubility of the solid dispersion compared to the pure drug. In in vitro release profiles revealed that formulation SD20, having drug: Kolliphor® P 407 in 1:9 ratio exhibited highest dissolution rate. The powder X-ray diffraction study and scanning electron microscopy (SEM) exhibited a crystalline to an amorphous transformation in the solid dispersion. The study demonstrated that solid dispersions are a highly effective technique to increase solubility and bioavailability of febuxostat.
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来源期刊
INDIAN DRUGS
INDIAN DRUGS Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.30
自引率
0.00%
发文量
98
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