固体分散体技术改善吴茱萸次碱溶出特性的研究

Dissolution Improvement of Rutaecarpine by Solid Dispersion Technology

目的:制备吴茱萸次碱(Rut)固体分散体,提高.Rut体外溶出度。方法:分别以聚乙烯吡咯烷酮(PVP)为载体,采用溶剂-共沉淀法,制备含不同辅助载体的Rut固体分散体;采用差示热分析和X-射线衍射分析对固体分散体进行物相鉴别,并进行体外溶出度试验;考察载体用量、载体中表面活性剂的加入和不同溶出介质对药物溶出特性的影响。结果:Rut以微晶形式存在于固体分散体中;其中,以微粉硅胶和乳糖为辅助载体制备的Rut-PVP-微粉硅胶(1:2:1)和Rut-PVP-乳糖(1:2:2)固体分散体,其累积溶出度较其物理混合物提高了约6倍。结论:Rut-PVP-微粉硅胶(1:2:1)和Rut-PVP-乳糖(1:2:2)固体分散体可显著提高药物的溶出速度和程度。

Objective：To prepare rutaecarpine（Rut） solid dispersion（SD） in order to improve the dissolution of rutaecarpine in vitro.Method：Rut-SD was prepared with PVP and other carriers by solvent-melting method.Differential thermal analysis and X-ray diffraction were used to determine the status of Rut in the carriers.The effects of the carrier ratio,surfactant and dissolution media on the dissolution characteristics in vitro were studied.Result：Differential thermal analysis and X-ray diffraction both showed that Rut existed in the solid dispersion in the form of microcrystal.The accumulated dissolution rates of Rut-PVP-micron silica gel（1：2：1） and Rut-PVP-lactose（1：2：2） were nearly 6 times higher than that of their physical mixtures.Conclusion：Among all the solid dispersions of Rut,Rut-PVP- micron silica gel（1：2：1） is the best one to improve the dissolution of Rut in vitro.