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目的:筛选淫羊藿黄酮自乳化释药系统(SEDDS)的最佳处方,体内体外评价其效果。方法:通过溶解度实验、伪相图绘制,以形成乳剂的乳化程度和乳化时间长短为指标,对淫羊藿黄酮处方中的油相、非离子表面活性剂、助表面活性剂进行筛选,确定最佳处方,通过体外溶出度测定和大鼠体内动力学的研究评价自乳化的效果和效能。结果:自乳化处方中油相为油酸,非离子表面活性剂为Tween-80,助表面活性剂为PEG400,最佳比例为2∶4∶4。SEDDS在水中25min的溶出度可达85%以上,而淫羊藿黄酮胶囊60min的溶出度不足50%;大鼠体内生物利用度提高1倍以上。结论:按优化处方制得的淫羊藿自乳化释药系统能有效提高淫羊藿黄酮在水中的溶出,并能有效提高大鼠体内的生物利用度。
Objective: To screen the best prescription of epimedium flavonoid self-emulsifying drug delivery system (SEDDS) and evaluate its effect in vitro and in vivo. Methods: Through the solubility experiments and pseudo-phase diagrams, the emulsifying degree and the emulsifying time of the emulsifier were used as indexes to screen the oil phase, non-ionic surfactant and co-surfactant in the formula of Epimedium flavonoids and determine the most. The best prescription was to evaluate the effectiveness and efficacy of self-emulsification by in vitro dissolution assay and rat in vivo kinetic studies. Results: In the self-emulsifying formulation, the oil phase was oleic acid, the non-ionic surfactant was Tween-80, the co-surfactant was PEG400, and the optimal ratio was 2:4:4. The dissolution of SEDDS in water at 25 min can reach 85% or more, while the dissolution rate of Epimedium flavonoid capsules is less than 50% in 60 minutes; the bioavailability in rats is increased by more than 1 time. Conclusion: Epimedium self-emulsifying drug release system prepared by optimized prescription can effectively improve the dissolution of epimedium flavonoids in water, and can effectively improve the bioavailability in rats.