马钱子巴布剂体外透皮实验及促透剂的筛选

目的:考察不同促透剂对马钱子巴布剂中马钱子碱、士的宁的体外透皮吸收的影响,筛选合适的促透剂。方法:采用改良Franz扩散池对离体大鼠皮肤进行体外透皮实验,RP-HPLC法测定含不同促透剂的马钱子巴布剂中活性成分的累积渗透量(Q_n)和透过率(T)。结果:马钱子巴布剂体外透皮吸收符合零级动力学方程,不同的促透剂对透皮吸收影响的顺序为:DMF>月桂氮芯卓酮(氮酮)>丙二醇>薄荷醇。在给定的范围内(≤5%),氮酮和薄荷醇的促透性能均是随着浓度增大而先升后降,二甲基甲酰胺和丙二醇的促透效果都是随着浓度增大而增强。结论:不同浓度的促透剂均能一定程度促进马钱子巴布剂活性成分的透皮吸收,其中以5%DMF的促渗效果最好。

Transdermal experiment of nux vomica cataplasm in vitro and the selection of penetration enhancers

OBJECTIVE To investigate the effect of different penetration enhancers on the transdermal absorption of brucine and strychnine in cataplasm in vitro,and screen the appropriate enhancer.METHODS Transdermal test in vitro of isolated rat skin was carried out with improved Franz diffusion cell,and RP-HPLC method was used to determine the cumulative permeation (Q_n) and transmittance (T) of the active components in the nux vomica cataplasm which contained different penetration enhancers.RESULTS The transdermal absorption of nux vomica cataplasm in vitro was in accordance with the zero-order kinetics equation.The orders of effect of different penetration enhancers on transdermal absorption were DMF > azone > propylene glycol > menthol.Within the given range (≤ 5%),the penetration performance of azone and menthol were increased first and then decreased with increasing concentrations,and DMF and propylene glycol were enhanced with the increase of concentration.CONCLUSION Different concentrations of penetration enhancers can promote the transdermal absorption of the active ingredients of nux vomica cataplasm,and the effect of 5% DMF is the best.