不同生物碱透皮吸收促进剂对芍药苷透皮吸收的影响

Influences of different alkaloid penetration enhancers on transdermal absorption of paeoniflorin

目的考察吴茱萸总生物碱、芥子碱硫氰酸盐、盐酸小檗碱3种促进剂对芍药苷的体外透皮渗透效果,筛选有效的透皮促渗剂,提高芍药苷的透皮速率。方法以小鼠离体腹部皮肤为渗透屏障,采用HPLC法对芍药苷进行含量测定,考察3种促进剂在12 h内对芍药苷累积渗透量、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0.543 9、0.993 0、3.709 9 g/(cm^2·h),增渗倍数(ER)分别为1.50、2.74、10.22,透皮时滞分别为2.10、1.12、0.34 h。结论 3种天然透皮促进剂均能明显促进芍药苷的透皮吸收,为研究其透皮给药提供参考依据。

Objective alkaloids, sinapine thi To survey the effects of 3 kinds of penetration enhancers, evodia rutaecarpa ocyanate and berberine hydrochloride, on transdermal permeation of paeoniflorin in vitro, screen effective penetration enhancers and improve the transcutaneous permeability of paeoniflorin. Methods The abdomen skin of mice in vitro was taken as permeation barrier. The content of paeoniflorin was determined by using HPLC for studying the influences of 3 kinds of penetration enhancers on kinetic parameters of in vitro transdermal absorption of paeoniflorin including cumulative permeation quantity, transdermal absorption rate and transdermal time-lag within 12 h. Results The transcutaneous permeability of evodia rutaecarpa alkaloids, sinapine thiocyanate and berberine hydrochloride was, respectively, 0. 543 9 g/cm2 · h, 0. 993 0 g/cm2 · h and 3. 709 9 g/cm2 · h, enhancing rate was, respectively, 1.50, 2.74 and 10.22, and transdermal time-lag was, respectively, 2.10 h, 1.12 h and 0.34 h. Conclusion Evodia rutaecarpa alkaloids, sinapine thiocyanate and berberine hydrochloride can significantly improve the transdermal absorption of paeoniflorin.