目的筛选3种促透剂组方对盐酸川芎嗪的透皮吸收的理论最佳促透配比。方法用两室扩散池体外透皮实验装置,以盐酸川芎嗪为对象,采用均匀设计处理考察加入不同剂量配比的冰片、薄荷醇、氮酮后,盐酸川芎嗪在BALB/c裸小鼠皮肤上的渗透系数,并对组方中各促透剂所占比例进行筛选。结果促透剂组方中冰片、薄荷醇、氮酮的最佳配比是1.5%∶1.5%∶1.5%(15mg/mL∶15mg/mL∶15mg/mL),实际渗透系数为69.575μg/(h.cm²),理论最佳渗透系数为69.749μg/(h.cm²)。结论均匀设计法筛选促透剂组方的理论最佳促透配比对于盐酸川芎嗪的透皮吸收研究是可行的。

Objective To optimize the proportion of three transdermal penetration enhancers on transdermal absorption of ligustrazine hydrochloride.Methods Permeation tests in vitro through BALB/c nude mouse skin in two compartment diffusion cells were performed to study the effect of synthetic borneol,menthol,and Azone on trandermal absorption of ligustrazine hydrochloride by changing their concentrations,and uniform design method was used to determine the penetration coefficient of ligustrazine hydrochloride and optimize the proportion of three transdermal penetration enhancers.Results The optimal proportion and contents of synthetic borneol,menthol,and Azone were 1.5%∶1.5%∶1.5%(15 mg/mL∶15 mg/mL∶15 mg/mL),the real penetration coefficient of ligustrazine hydrochloride was 69.575 μg/(h·cm²),while the theoretical penetration coefficient was 69.749 μg/(h·cm²).Conclusion Uniform design method is an effective way to optimize the proportion of three transdermal penetration enhancers on trandermal absorption of ligustrazine hydrochloride.

广东省卫生厅资助课题(2000490)；广东省自然科学基金重点项目(06105114)