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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 a solid dispersion of abscisiclacein B (PB) to improve the solubility of PB. Methods Polyvinylpyrrolidone (PVP), polyethylene glycol 4000 (PEG 4000) and poloxamer 188 (F68) were used as carriers to prepare PB solid dispersions by solvent method or solvent-melting method, respectively. Dissolution test; the properties of the solid dispersions were investigated by differential scanning calorimetry (DSC), electron microscopy (SEM) and infrared spectroscopy (IR). Results The solubility and in vitro dissolution of PB solid dispersions prepared with PVP as carrier were better than that of PEG 4000 and F68, and the mass ratio of PB-PVP was 1: 6. Conclusion The preparation of solid dispersions with PVP as a carrier significantly increases the solubility of PB and is uniformly distributed in the carrier either in a supersaturated solid solution or in an amorphous state.