良肤乳膏小鼠皮肤药物动力学的研究

Dermatopharmacokinetic studies of Liangfu cream in rat skin

目的:考察良肤乳膏中丹皮酚、白鲜碱、梣酮及甘草次酸等主要有效成分在小鼠皮肤中滞留量与时间的关系,研究良肤乳膏小鼠皮肤药物动力学特征。方法:采用HPLC测定皮肤生物样品中各成分的浓度,计算不同时间给药,皮肤中丹皮酚、白鲜碱、梣酮、甘草次酸的滞留量,采用DAS软件拟合药物动力学参数。结果:良肤乳膏中丹皮酚、甘草次酸在小鼠皮肤中滞留量的动力学过程符合二室模型,白鲜碱、梣酮符合一室模型,4种成分皮肤给药t1/2Ka分别为0.307,0.112,0.146,0.216 h,Tlag分别为0.006,0.123,0.136,0.109 h,Tmax均0.5 h,Cmax分别为40.163,1.607,6.725,100.553μg.cm-3,t1/2β分别为14.719,1.262,0.838,234.807 h,AUC0-∞分别为116.987,2.713,9.345,697.000μg.cm-3.h-1,MRT0-∞分别为3.662,1.67,1.585,10.897。结论:4种主要有效成分能迅速渗透进入皮肤,并在皮肤局部较长时间蓄积,有利于药物在皮肤局部长时间发挥药理作用。

Objective： To study the relationship between deposition content and time of the active ingredients in rat skin,and investigate the dermatopharmacokinetics of Liangfu Cream.Method： The contents of paeonol,dictamnine,fraxinellone and glycyrrhetinic acid in rat skin were determined by HPLC.The dermatopharmacokinetics parameters were calculated by DAS software.Result： The dermatopharmacokinetics of paeonol and glycyrrhetinic acid were two compartment model,while that of dictamnine and fraxinellone were one compartment model： T1/2Ka of four active ingredients were 0.307,0.112,0.146,0.216 h,respectively;Tlag of them were 0.006,0.123,0.136,0.109 h,respectively;all the Tmax of them was 0.5 h;the Cmax were 40.163,1.607,6.725,100.553 μg·cm-3,respectively;the t1/2β were 14.719,1.262,0.838,234.807 h,respectively;the AUC0-∞ were 16.987,2.713,9.345,697.000 μg·cm-3·h-1,respectively;and the MRT0-∞ were 3.662,1.67,1.585,10.897,respectively.Conclusion： The skin pharmacokinetics characteristic of four ingredients in Liangfu cream is lined with the cataplasm long time.