大豆苷元固体自乳化制剂的处方优化和制备

Preparation and Formulation Optimization of Daidzein Solid Self-emulsifying Preparation

目的:优化大豆苷元固体自乳化制剂的处方。方法:通过处方配伍试验和伪三元相图的绘制,以乳化程度和乳化时间为指标,确定乳化剂、油相和助乳化剂种类;采用星点设计-效应面法,以平均粒径与Zeta电位为指标,优选最佳自乳化处方;以β-环糊精为吸附材料,制备大豆苷元固体自乳化制剂,并采用差示扫描量热(DSC)分析和X-射线衍射鉴别药物在载体中的存在状态。结果:优化后的处方为大豆苷元:吐温80:二乙二醇单乙基醚:油酸乙酯:β-环糊精=9.4:54.2:20.1:25.7:437.6。DSC和X-射线分析结果显示,药物在载体中以无定形或分子形式存在。大豆苷元固体自乳化制剂45min溶出度达85%以上。结论:固体自乳化释药系统能够提高大豆苷元的体外溶出度。

OBJECTIVE：To optimize the formulation of Daidzein solid self-emulsifying preparation.METHODS：The emulsifier,various oils and surfactants were screened by compatibility tests and pseudo-ternary phase diagrams with the degree of emulsification and emulsifying time as index.The formulation of Daidzein solid self-emulsifying preparation was optimized using central composite design response surface methodology with particle size and Zeta potential as dependent variables.Daidzein solid self-emulsifying preparation was prepared with β-CD as adsorbing material.The state of daidzein in carriers was identified by DSC scan and X-diffraction.RESULTS：The best formulation of Daidzein solid self-emulsifying preparation was made up of daidzein：tween 80：transcutol P：ethyl oleate：β-CD=9.4：54.2：20.1：25.7：437.6.The results of DSC scan and X-diffraction indicated that the drug was in the amorphous and molecule state.The dissolution rate of Daidzein solid self-emulsifying preparation was more than 85% in 45 min.CONCLUSION：The dissolution of daidzein could be enhanced by S-SEDDS.