龙血竭总黄酮固体分散体的制备和性能表征

Preparation and Characterization of Solid Dispersion of Total Flavonols from Resina Draconis

为制备龙血竭总黄酮(RDF)固体分散体,提高其溶出度,并对固体分散体进行表征,以聚乙烯比咯烷酮K30(PVP K30)和泊洛沙姆188(F68)为辅料,采用溶剂法制备了三相固体分散体,以体外溶出试验考察了固体分散体制备工艺,并以X射线衍射(XRD)、红外光谱(IR)、差示扫描量热法(DSC)及扫描电子显微镜法(SEM)等手段对固体分散体进行了性能表征.结果表明:以TFDB,PVP K30,F68质量比为181时制得固体分散体的溶出效果较好,药物和辅料间无相互作用力,药物溶出的改善主要归结于固体分散体中药物的粒径减小和F68的润湿与增溶作用.故采用三相固体分散体技术能显著提高龙血竭总黄酮的体外溶出度,为改善中药难溶性成分的溶出奠定了理论基础.

In order to prepare the solid dispersion of total flavonols from Resina Draconis,the dissolution was improved and the solid dispersion was characterized.Three?phase solid dispersions were prepared by using polyvinylpyrrolidone K30(PVP K30)and poloxamer 188(F68)as the excipients.Then the solid dispersion was prepared by in vitro dissolution test and the performance of the solid dispersion was characterized by XRD,IR,DSC and SEM.The results showed that the formulation of the solid dispersion was seleted as TFDB/PVP K30/F68 with a mass ratio of 1︰8︰1.No interaction occurred between the drug and the carrier materials,and the improvement of the drug dissolution was mainly attributed to the decreasing size of the drug in solid dispersion and the madefaction and solubilization of F68.So the ternary solid dispersion technique can significantly increase in vitro dissolution of TFDB,which pay a theoretical foundation for improving the dissolution of the insoluble ingredients of traditional Chinese medicine.