Jiang Yong-nan, Mo Hong-ying
Guangdong Food and Drug Vocational College, Guangzhou 510520, China.
Zhong Yao Cai. 2010 May;33(5):767-71.
To study the formulation optimization of epimedium flavonoids self-emulsifying drug delivery system and evaluate its effect in vitro and in vivo.
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.
The experimental results revealed the optimized formulation of the self-emulsifying drug delivery system which consisted 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.
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.
研究淫羊藿黄酮自乳化给药系统的处方优化，并对其体外及体内效果进行评价。
基于乳化程度和乳化时间，通过测定溶解度、采用正交设计以及构建三元相图，对处方进行优化（即筛选合适的油相、非离子表面活性剂和助表面活性剂）。测定自乳化给药系统（SEDDS）的溶出度，并测定其在大鼠体内的药代动力学。
实验结果揭示了自乳化给药系统的优化处方，该处方由油酸作为油相、吐温-80作为非离子表面活性剂、聚乙二醇400作为助表面活性剂，比例为2:4:4。SEDDS在水中25分钟内的溶出度超过85%，而淫羊藿黄酮胶囊在60分钟内的溶出度小于50%。
应用优化后的淫羊藿黄酮自乳化给药系统处方可显著提高淫羊藿黄酮在水中的溶解度并改善其生物利用度。
