宣痹凝胶帖膏剂有效成分的透皮行为研究

目的:研究宣痹凝胶贴膏剂中有效成分龙胆苦苷、柚皮苷、原苏木素B的透皮吸收特性。方法:采用Franz扩散池法,以大鼠腹皮为体外模型,用HPLC测定接受液、皮中、膏中残留的龙胆苦苷、柚皮苷、原苏木素B 3种指标成分的含量。结果:宣痹凝胶贴膏剂中龙胆苦苷、柚皮苷、原苏木素B的透皮速率分别为3.47,1.59,2.13μg.cm-2.h-1;24 h的累积透过率分别为25.42%,11.73%,17.78%;在皮中的滞留量分别为0.231,0.593,0.568μg.cm-2,滞留率分别为0.027%,0.227%,0.475%;在膏中的残留量分别为2 179,674,278μg,残留率分别为81.36%,81.92%,73.83%。结论:宣痹凝胶贴膏剂中有效成分的体外透皮行为接近零级过程,皮中滞留率相比透过率和膏中残留率来说非常低。

Transdermal behavior of effective constituents in Xuanbi gel plaster

Objective: To study the transdermal absorbability of gentiopicroside,naringin and protosappanin B contained in Xuanbi gel plaster.Method: The Franz diffusing cells method was adopted for the in vitro model of rat belly skins.Three indexes,gentiopicroside,naringin and protosappanin B,residued in the accept liquid,skins and plaster were determined by HPLC.Result: The penetration rates of gentiopicroside,naringin and protosappanin B were respectively 3.47,1.59,2.13 μg·cm-2·h-1.After 24 h,their penetration rates were 25.42%,11.73%,17.78%,respectively.The residual quantities of gentiopicroside,naringin and protosappanin B in skin were 0.231,0.593,0.568 μg·cm-2,with the retention rates of 0.027%,0.227%,0.475%,respectively.The amount of residue of gentiopicroside,naringin and protosappanin B in plaster were 2 179,674,278 μg,with the retention rates of 81.36%,81.92%,73.83%,respectively.Conclusion: The in vitro transdermal behavior of Xuanbi gel plaster is close to a zero-order process.The residual quantity the retention rate in skins is much lower than the penetration rate and the residual rate in plaster.