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目的考察吴茱萸生物碱、芥子碱硫氰酸盐、盐酸小檗碱对阿魏酸的透皮促渗效果,筛选有效的透皮吸收促进剂,提高阿魏酸的透皮速率。方法采用YB-P6型智能透皮试验仪,以小鼠离体腹部皮肤为渗透屏障,采用HPLC法对阿魏酸进行测定,考察3种促进剂对阿魏酸累积渗透量、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。结果吴茱萸总生物碱、芥子碱硫氰酸盐、盐酸小檗碱的渗透速率分别为:9.086 1、26.396 0、8.663 9μg(cm2·h),增渗倍数(ER)分别为:12.79、4.40、4.20,透皮时滞分别:0.03、0.74、1.50 h。结论 3种天然透皮促进剂均能明显促进阿魏酸的透皮吸收,为研究其透皮给药提供参考依据。
Objective To investigate the transdermal permeation enhancement effect of Evodia alkaloids, sinapine thiocyanate and berberine on ferulic acid, and to screen effective transdermal absorption enhancer to improve the transdermal rate of ferulic acid. Methods By using YB-P6 intelligent transdermal test apparatus, the isolated abdominal skin of mice was used as the penetration barrier. The ferulic acid was determined by HPLC. The effects of three accelerators on the cumulative amount of ferulic acid, the transdermal absorption rate , Transdermal delay and other in vitro transdermal absorption kinetic parameters. Results The permeation rates of total alkaloids, sinapine thiocyanate and berberine were as follows: 9.086 1,26.396 0 and 8.663 9μg (cm2 · h) respectively. The permeation rate (ER) were 12.79 and 4.40, 4.20, transdermal delay respectively: 0.03,0.74,1.50 h. Conclusion All three natural transdermal enhancers can significantly promote the transdermal absorption of ferulic acid and provide a reference for the study of transdermal administration.