3种促透剂对钩藤体外透皮吸收的影响

Effects of Three Different Penetration Enchancers on Transdermal Absorption of the Extract of Ramulus Uncariae Cum Uncis in Vitro

目的研究氮酮、冰片、薄荷脑3种促透剂对钩藤体外透皮吸收的影响。方法用改良Franz扩散池,选择大鼠背皮为渗透屏障,从接受室取样,用HPLC测定样品中钩藤碱含量,比较3种促透剂对钩藤透皮吸收的影响。结果不同浓度的3种促透剂对钩藤碱的透皮效果皆以5%为最佳,含5%氮酮、5%冰片、5%薄荷脑的钩藤提取液平均透皮速率分别为1.00,0.92,0.87μg·cm-2·h-1,使钩藤碱透皮速率分别提高2.44,2.24,1.95倍。结论 3种促透剂皆可以促进钩藤主要活性成分钩藤碱的透皮吸收,在实验浓度范围内,以5%氮酮促渗透效果最好。

OBJECTIVE To study the effects of three different penetration enchancers on the transdermal absorption of the extract of Ramulus Uncariae cum uncis in vitro. METHODS Using the extracorporeal back skin of rat as the penetration barrier in a improved Franz diffusion cell, the percutaneous rates of rhynchophylline at various concentrations of azone, bornel and methol were compared by determining the content of rhynchophylline by HPLC. RESULTS The average percutaneous rate of rhynchophylline were 1.00, 0.92, 0.87 μg·cm-2·h-1 respectively corresponding to the concentrations of azone, bornel and menthol at 5%, the enhancing rate （ER） were 2.44, 2.24, 1.95, respectively. CONCLUSION Azone, bornel and menthol can enhance transdermal absorption of rhynchophylline （the main active ingredient in Ramulus Uncariae cum uncis）, and in study range of concentrations of azone, bornel and methol, the effect of promoting penetration of 5% azone is the best.