青藤碱微乳的制备及其体外经皮渗透研究

Preparation of Sinomenine microemulsion and its transdermal absorption

目的:筛选最佳处方制备青藤碱微乳,考察青藤碱微乳对离体大鼠皮肤的经皮渗透特征。方法:以油酸-聚山梨酯80-无水乙醇-水作为微乳的组成进行伪三元相图研究,采用改进的Franz扩散池研究青藤碱微乳的透皮行为,筛选最佳处方组成,并与青藤碱凝胶作透皮比较。结果:青藤碱微乳的透皮稳态流量大于青藤碱凝胶(P<0.01),青藤碱微乳平均透皮速率为116.44μg.cm-2.h-1,透皮吸收符合零级模式(r>0.99)。结论:青藤碱微乳有较强的透皮能力,有望成为青藤碱的新型透皮给药制剂。

Objective：To screen the optimum formulation and prepare O/W sinomenine microemulsion and investigate its in vitro transdermal delivery ability. Method：The microemulsions were prepared with the formulation containing oleic acid-tween 80-dehydrated alcohol-water by the pseudo-ternary phase diagram. The permeation flux of sinomenine was determined in vitro by Franz diffusion cell fitted with rat skin. The sinomenine was determined by HPLC. The transdermal characteristics of sinomenine microemulsion were compared with that of sinomenine gels. Result： The steady state flux of sinomenine mieroemulsion was significantly higher than that of sinomenine gels. The average permeation rate of sinomenine microemulsion was 116. 44 μg · cm^-2 · h^-1 in vitro. Conclusion： These results indicated that the studied microemulsion system with high permeation rate may be a potential vehicle for the transdermal delivery of sinomenine.