刺山柑果凝胶膏剂的体外透皮研究

目的研究不同促透剂对刺山柑果凝胶膏中有效成分体外透皮吸收的影响,筛选有效的促透剂。方法选择不同质量分数的氮酮、丙二醇以及氮酮与丙二醇的不同质量比例组合物为促透剂,采用改良的Franz扩散池,以离体小鼠皮肤为透皮屏障,用HPLC测定接收液中有效成分芦丁的含量,考察不同促透剂对刺山柑果凝胶膏中芦丁的单位面积累积透过量和透皮速率常数的影响。结果 20mg.g-1氮酮促渗效果较好,其促渗倍数为1.26倍,芦丁的透皮速率常数为5.45μg.cm-2.h-1。结论不同促透剂对刺山柑果凝胶膏中有效成分的透皮吸收的影响有差异,其中20mg.g-1氮酮能够有效促进凝胶膏中芦丁的体外透皮吸收,可作为刺山柑果凝胶膏的促透剂。

Effects of penetration enhancers on percutaneous absorption in Vitro of rutin in Capparis spinosa Gel Cream

Objective To study the effects of different penetration enhancers on the percutaneous absorption in vitro of active ingredients in Capparis spinosa Gel Cream and to screen out the effective penetration enhancers.Method Using improved Franz-type diffusion cell and excised small mouse skin in vitro as transdermal barrier,the kinetics parameters of active ingredients such as cumulative permeation quantity,permeation rate were determined by HPLC.The enhancement ability of different enhancers such as azone,propylene glycol,and different proportions of the composition of azone and propylene glycol was investigated.Result 20 mg·g-1 azone enhanced the cumulative permeation quantity better than other penetration enhancers,it’s enhancer ratio was 1.26(P<0.05),and the permeation rate of rutin was 5.45 μg·cm-2·h-1.Conclusion The effects of penetration enhancers on the percutaneous absorption in vitro of active ingredients in Capparis spinosa Gel Cream are different.20 mg·g-1 azone which can enhance the cumulative permeation quantity is the most suitable penetration enhancer for Capparis spinosa Gel Cream.