淫羊藿黄酮自乳化软胶囊制备及大鼠体内动力学  

Preparation of Self-emulsifying Soft Capsule and Its Pharmacokinetic In Rats for Epimedium Flavonoids

作　　者：江永南[1] 莫红缨[2] 

机构地区：[1]广东食品药品职业学院,广东广州510520 [2]广州医学院第一附属医院,广东广州510120

出　　处：《中药材》2010年第5期767-771,共5页Journal of Chinese Medicinal Materials

摘　　要：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 study the formulation optimization of epimedium flavonoids self-emulsifying drug delivery system and evaluate its effect in vitro and in vivo.Methods：Based on the degree of emulsification and emulsifying time,the formulation optimization（i.e.,screening of suitable oil phases,nonionic surfactants and co-surfactants）was made by the use of determination of the solubility,orthogonal design and construction of tertiary phase diagram.The dissolution of SEDDS was measured and its pharmacokinetic in rats was measured.Results：The experimental results revealed the optimized formulation of the self-emulsifying drug delivery system which consistsed of oleic acid as oil phase,Tween-80 as nonionic surfactant,and PEG400 as co-surfactant in the proportion of 2∶4∶4.The dissolution of SEDDS in water was more than 85% in 25 minutes,while that of the epimedium flavonoids capsule was less than 50% in 60 minutes.Conclusion：Application of the optimized formulation of epimedium flavonoids self-emulsifying drug delivery system could significantly increase the solubility of epimedium flavonoids in water and improve its bioavailability.

关 键 词：淫羊藿黄酮 自乳化 动力学 

分 类 号：R285.5[医药卫生—中药学]