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二氟尼柳与聚乙烯吡咯烷酮K30共沉淀物的溶解动力学

Dissolution kinetics for coprecipitates of diflunisal with PVP K30.

作者信息

Rodríguez-Espinosa C, Martínez-Ohárriz M C, Martín C, Goñi M M, Vélaz I, Sánchez M

机构信息

Dpto. de Química Sección de Química-Física, Facultad de Ciencias, Universidad de Navarra, Pamplona, Spain.

出版信息

Eur J Drug Metab Pharmacokinet. 1998 Apr-Jun;23(2):109-12. doi: 10.1007/BF03189324.

Abstract

Diflunisal is a nonsteroidal anti-inflammatory drug that is poorly soluble in water. The present study describes the formulation of solid dispersions of the drug designed to increase its solubility. X-ray diffraction and DSC were used to examine the physico-chemical characteristics of solid dispersions of diflunisal and polyvinylpyrrolidone (PVP) prepared by the solvent method, using percentage proportional compositions ranging from 20:80 to 50:50. X-ray diffraction analysis detected that diflunisal is present in solid dispersions in crystalline or amorphous state depending on the PVP content. The thermal behavior of diflunisal observed in the DSC curves of solid dispersion systems, was attributed to a solid-state interaction. The increased release of the PVP-drug dispersion as compared to the PVP-drug physical mixture was attributed to the formation of a complex resulting from the interaction of the drug and the polymer.

摘要

双氟尼酸是一种难溶于水的非甾体抗炎药。本研究描述了旨在提高其溶解度的该药物固体分散体的制剂。采用溶剂法,使用比例范围从20:80至50:50的组成,通过X射线衍射和差示扫描量热法(DSC)研究双氟尼酸与聚乙烯吡咯烷酮(PVP)固体分散体的物理化学特性。X射线衍射分析检测到,根据PVP含量,双氟尼酸在固体分散体中以结晶态或无定形态存在。在固体分散体系的DSC曲线中观察到的双氟尼酸的热行为归因于固态相互作用。与PVP - 药物物理混合物相比,PVP - 药物分散体释放增加归因于药物与聚合物相互作用形成的复合物。

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