靛玉红自乳化释药系统的体外评价

In vitro evaluation of indirubin self-emulsifying drug delivery system

目的:制备靛玉红自乳化释药系统,并对其进行体外评价。方法:利用三角相图法探讨自乳化的形成条件,并优化靛玉红自乳化释药系统处方。通过测定自乳化时间、乳化后乳液粒径的大小及药物的体外溶出行为对自乳化释药系统进行体外评价。结果:最佳处方组成为Labrasol-Peceol-Transcutol P(85∶10∶5),优选出的自乳化处方5 min内已基本乳化完全,乳化后乳液粒子大小在100 nm左右;同靛玉红混悬液相比,靛玉红自乳化释药系统的体外溶出明显提高。结论:自乳化释药系统可以提高难溶性药物的体外溶出。

AIM： To prepare indirubin self-emulsifying drug delivery system（SEDDS） and evaluate it in vitro. METHODS： The criteria of SEDDS formation was studied and indirubin SEDDS preparation optimized with triangle phase diagram. In order to investigate self-emulsifying ability, the time of self-emulsifying, particle size of emulsion and the dissolution of indirubin in vitro were determined. RESULTS ： The best formulation of SEDDS was made up of labrasol-peceol-transcutol P （85：10：5 ）, which served as oil phase, emulsifier and assistant emulsifier,respectively. The selected formulation could completely emulsify in 5 min and the particle size was about 100 nm. As compared with indirubin suspension, SEDDS could improve drug dissolution significantly. CONCLUSION： SEDDS can give rise to the dissolution increase of slightly soluble drug in water in vitro.