银杏总黄酮自乳化释药系统的制备及其性质研究  

Preparation and Characteristics of Self-Emulsifying Drug Delivery System of Total Ginkgo Flavonoid

作　　者：廖祥茹[1] 史琼枝[1] 方松[1] 陈鹰[1] 

机构地区：[1]广州军区武汉总医院药剂科,武汉430070

出　　处：《中国药师》2016年第5期850-853,共4页China Pharmacist

基　　金：武汉总医院科研课题(编号:YZ201438)

摘　　要：目的:制备银杏总黄酮自乳化释药系统,并对其体外特性进行评价。方法:通过溶解度试验、处方配伍和伪三元相图中形成微乳区域面积的大小来确定银杏总黄酮自乳化释药系统的处方组成,并考察了该释药系统经水稀释后形成微乳的外观、形态、粒径分布、Zeta电位以及体外药物溶出度。结果:所得银杏总黄酮的自乳化释药系统的处方组成:油酸聚乙二醇甘油酯(油相)、聚山梨酯-80(表面活性剂)、二乙二醇单乙基醚(XCF,助表面活性剂),最佳配比为10∶6∶4,载药量10.0 mg·g^(-1)。经水稀释后形成澄清、透明状溶液,透射电镜观察微乳呈大小均一,球状分布,平均粒径为(87.4±26.7)nm,Zeta电位为(-13.1±1.5)m V。溶出度结果表明,银杏总黄酮的自乳化释药系统在p H1.2的盐酸溶液中45 min内累积溶出度可达(96.1±4.8)%。结论:自乳化释药系统能够显著提高银杏总黄酮的体外溶出速度,有望成为银叶总黄酮的优良口服制剂。Objective：To prepare total ginkgo flavonoid self-emulsifying drug delivery system（TGF-SMDDS） and estimate its characteristics in vitro.Methods：The formula of TGF-SMDDS was optimized based on the solubility tests,formula compatibility and microemulsion area in the pseudo ternary phase diagram.The appearance,morphology,particle size,zeta potential and in vitro dissolution of TGF-SMDDS were investigated.Results：The formula was composed of oleoyl macrogolglycerides as the oil phase,Tween-80 as the surfactant and XCF as the co-surfactant.The ratio of oil phase,surfactant and co-surfactant was 10 ∶ 6 ∶ 4.The drug loading was 10.0 mg·g^-1.After mixed with water,TGF-SMDDS was formed a clear and transparent microemulsion with homogeneous small spheres as seen under a transmission electron microscope.The particle size and zeta potential of TGF-SMDDS was（87.4 ± 26.7） nm and -13.1 ± 1.5）m V,respectively.The accumulative dissolution of TGF-SMDDS in p H1.2 hydrochloric acid solution was（96.1 ± 4.8） % in 45 min.Conclusion：The TGF-SMDDS can significantly enhance the dissolution of TGF in vitro,which may be a potential effective preparation for TGF.

关 键 词：银杏总黄酮 自乳化释药系统 体外溶出 

分 类 号：R944.9[医药卫生—药剂学]