不同透皮促进剂对高乌甲素凝胶体外透皮吸收的影响

Effects of different penetration enhancers on percutaneous absorption of lappaconitine gel in vitro

目的:研究不同透皮促进剂对高乌甲素凝胶体外经皮渗透的影响,筛选有效的复合透皮吸收促进剂,提高高乌甲素的透皮吸收速率。方法:采用改良的Franz扩散池,以离体大鼠皮肤为透皮屏障,用高效液相色谱法测定不同透皮吸收促进剂对高乌甲素凝胶的累积渗透量、透皮吸收速率、透皮时滞等体外透皮吸收动力学参数的影响。对氮酮(Azone)、丙二醇(PG)、油酸(OA)、月桂醇(LA)4种透皮吸收促进剂单独应用和任意2种合用的促渗效果进行考察。结果:以Azone+PG,LA+PG,OA+PG为复合促进剂时释药速率显著提高,其中以OA+PG促渗作用最强。结论:通过考察促进剂对高乌甲素凝胶的影响,为研究其透皮给药提供了参考依据。

Objective: To study the effects of different penetration enhancers on the transcutaneous permeability of lappaconitine gel in vitro and therefore to screen out the effective accelerator to enhance the permeation rate of lappaconitine. Method: Using improved Franz-type diffusion cell and excised big mouse skin in vitro as transdermal barrier, the kinetics parameters such as cumulative permeation quantity,permeation rate and permeation lagged time were determined by HPLC. The enhancement ability of four different enhancers such as azone(Azone), propylene glycol(PG),oleic acid(OA) and lauryl alcohol(LA),was investigated when used either uniquely or combinatively each other at random. Result: When used combinatively, Azone+PG,LA+PG,OA+PG can enhance the cumulative permeation quantity, OA+PG was the best one among them. Conclusion: The selection of the best penetration enhancers provided reference for lappaconitine transdermal delivery.