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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 a self-emulsifying drug delivery system of ginkgo flavonoids and to evaluate its in vitro characteristics. Methods: The prescriptions of self-emulsifying drug delivery system of ginkgo flavonoids were determined by solubility test, prescription compatibility and the size of microemulsion area formed in the pseudo-ternary phase diagram. The effect of the drug release system on the formation of microemulsion Appearance, morphology, particle size distribution, Zeta potential and in vitro drug dissolution. Results: The formulation of self-emulsifying drug delivery system of ginkgo flavonoids was composed of oleic acid polyethylene glycol glyceryl ester (oil phase), polysorbate-80 (surfactant), diethylene glycol monoethyl ether (XCF , Co-surfactant), the best ratio of 10:6:4, drug loading 10.0 mg · g -1. After dilution with water, a clear and transparent solution was formed. The size of the microemulsion was uniform and spherical with transmission electron microscopy. The mean particle size was (87.4 ± 26.7) nm and the zeta potential was (-13.1 ± 1.5) mV. Dissolution results showed that the cumulative dissolution of self-emulsifying drug delivery system of ginkgo flavonoids reached 96.1 ± 4.8% within 45 min of p H1.2 hydrochloric acid solution. Conclusion: Self-emulsifying drug delivery system can significantly improve the in vitro dissolution rate of total flavonoids of Ginkgo biloba and is expected to be an excellent oral preparation of total flavonoids from silver leaf.