目的 将草胡椒素B（PB）制成固体分散体，改善PB的溶解度。方法 分别以聚乙烯吡咯烷酮（PVP）、聚乙二醇4000（PEG 4000）和泊洛沙姆188（F68）为载体，采用溶剂法或溶剂-熔融法制备PB固体分散体，并进行饱和溶解度和体外溶出度试验；利用差热分析（DSC）、电镜扫描（SEM）和红外光谱（IR）研究固体分散体的性质。结果 以PVP为载体制备的PB固体分散体的溶解度和体外溶出度优于PEG 4000和F68，且以PB-PVP质量比1∶6为最佳。结论 以PVP为载体制备固体分散体能显著增加PB的溶解度，且以过饱和的固态溶液或无定型状态均匀分布在载体中。

Objective To prepare peperomin B (PB) solid dispersion and to improve the dissolution of PB. Methods The solid dispersion of PB was prepared by the dissolved or solvent-melting methods with PVP, PEG 4000, and Poloxamer 188 (F68) as carriers, respectively. The equilibrium solubility and dissolution characteristics of the solid dispersion in vitro were measured by HPLC. Properties of the solid dispersion were studied by DSC, SEM, and IR. Results The solid dispersion of PB with PVP as the carrier was better to improve the dissolution and solubility than those with PEG 4000 and F68, and PB-PVP (1∶6) was the best. Conclusion The PB solid dispersion with PVP as the carrier could significantly improve the solubility of PB, and is evenly distributed in the carrier in supersaturated solid solution or amorphous state.

国家自然科学基金资助项目（30901852）；国家“重大新药创制”科技重大专项（2009ZX09301-007）；上海市青年科技启明星计划项目（10QB1404000）