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齐墩果酸与三元固体分散体的溶出度改善

Improved dissolution of oleanolic acid with ternary solid dispersions.

作者信息

Liu Longxiao, Wang Xiaocui

机构信息

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.

出版信息

AAPS PharmSciTech. 2007 Dec 21;8(4):E113. doi: 10.1208/pt0804113.

Abstract

The purpose of this study was to enhance the dissolution of oleanolic acid by solid dispersions consisting of the drug, a polymeric carrier, and a surfactant. Binary solid dispersions consisting of oleanolic acid and polyvinylpyrrolidone were prepared for comparison. Polysorbate 80, a nonionic surfactant, was incorporated into binary solid dispersions as the third component to prepare ternary solid dispersions. Solid dispersions were characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, and dissolution tests. The crystallinization of OA was prohibited in solid dispersions. Both the binary and ternary solid dispersions enhanced the dissolution of OA. Moreover, the dissolution of ternary solid dispersion was faster compared with that of binary solid dispersion. Polysorbate 80 played an important positive role in dissolution of the solid dispersion.

摘要

本研究的目的是通过由药物、聚合物载体和表面活性剂组成的固体分散体来提高齐墩果酸的溶出度。制备了由齐墩果酸和聚乙烯吡咯烷酮组成的二元固体分散体用于比较。将非离子表面活性剂聚山梨酯80作为第三组分加入二元固体分散体中制备三元固体分散体。通过差示扫描量热法、傅里叶变换红外光谱法和溶出度试验对固体分散体进行表征。在固体分散体中,齐墩果酸的结晶被抑制。二元和三元固体分散体均提高了齐墩果酸的溶出度。此外,三元固体分散体的溶出速度比二元固体分散体更快。聚山梨酯80在固体分散体的溶出过程中发挥了重要的积极作用。

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