藤黄酸自微乳化释药系统的制备与质量评价

目的构建藤黄酸自微乳化释药系统(GA-SMEDDSs),并对其质量进行评价。方法通过溶解度实验确定GA-SMEDDSs使用的油相、乳化剂和助乳化剂种类,根据伪三元相图法绘制出影响其微乳液形成的辅料用量范围,采用中心复合设计-效应面法优化并确定GA-SMEDDSs的最佳处方组成,在透射电镜下观察GA-SMEDDSs形成微乳的微观结构,用马尔文激光粒度仪测定粒径分布,考察GA-SMEDDSs经模拟人体生理体液稀释后的稳定性,比较GA-SMEDDSs与原料药的体外药物溶出速率。结果通过实验优化得到GA-SMEDDSs的最优处方组成:肉豆蔻酸异丙酯(IPM)质量分数为20.0%,辛酸癸酸聚乙二醇甘油酯(labrasol)质量分数为35.0%,二乙二醇单乙基醚(transcutol P)质量分数为45.0%,GA-SMEDDSs经水分散可形成黄色透明状微乳液,透射电镜下可观察到微乳呈类球状,大小均匀,平均粒径为168.4±5.9 nm;经模拟人体生理体液稀释后微乳物理稳定性良好;GA-SMEDDSs在人工胃液和人工肠液中药物溶出速率均显著提高。结论藤黄酸制备成自微乳化释药系统可提高药物溶出速度,...

Preparation and quality evaluation of gambogic acid self-microemulsifying drug delivery systems

Objective To construct gambogic acid self-microemulsifying drug delivery systems(GA-SMEDDSs)and evaluate its quality.Methods The oil phase,surfactant and co-surfactant used in GA-SMEDDSs were selected on the basis of solubility studies.And mass fraction range capable of influencing the formation of microemulsions was determined according to the pseudo-ternary phase diagram.The central composite design-response surface methodology(CCD-RSM)was adopted to optimize the composition of GA-SMEDDSs.The microstructure of microemulsion formed by GA-SMEDDSs was observed under transmission electron microscope.The particle size distribution was determined by Malvern laser particle size analyzer.The stability of GA-SMEDDSs after dilution with simulating human physiological fluids was investigated.The in vitro drug dissolution rate of GA-SMEDDSs and GA was compared.Results The optimal formulation of GA-SMEDDSs was obtained through experimental optimization:IPM mass fraction was 20.0%,labrasol was 35.0%,and transcutol P was 45.0%.The water-dispersed GA-SMEDDSs can form a yellow transparent microemulsion.Under the transmission electron microscope,the microemulsion could be observed as a spherical shape with uniform size,and the average particle size was 168.4±5.9 nm.Microemulsion had good physical stability after dilution with simulating human physiological fluids.The dissolution rate of GA-SMEDDSs was significantly increased.Conclusion The GA-SMEDDSs could improve the dissolution rate,which is expected to improve the oral bioavailability of gambogic acid.