不同透皮吸收促进剂对延胡索乙素透皮吸收的影响

The effect of different penetration enhancers on transdermal absorption of tetrahydropalmatine

【目的】考察不同透皮吸收促进剂对延胡索乙素透皮吸收的影响,为促透剂的选择提供依据。【方法】采用Franz体外释药装置,紫外分光光度法检测接受液中延胡索乙素的浓度,通过计算药物的累积透皮百分率研究延胡索乙素经离体鼠皮的透皮规律。考察了不同种类及浓度促透剂对延胡索乙素体外透皮特性的影响。【结果】延胡索乙素透皮吸收与其浓度有关,促透剂的种类和用量对其皮肤透过量均有影响。250μg/ml浓度的延胡索乙素透皮吸收效果较好,2%冰片的促透作用较其它促透剂作用更强。【结论】选择适当的透皮吸收促进剂可显著提高延胡索乙素的经皮渗透速率,延胡索乙素有望开发成经皮给药制剂。

【Objective】To explore the effect of different penetration enhancers on transdermal absorption of tetrahydropalmatine, and provide basis for the selection of penetration enhancers.【Methods】The in vitro Franz diffusion set was used as transdermal barrier.The concentration of tetrahydropalmatine in receiving solution was determined with UV spectrophotometry. The penetration rules of tetrahydropalmatine via in vitro rat skin were studied by calculating the cumulative transdermal ratio of tetrahydropalmatine. The in vitro transdermal effect of different penetration enhancers in different concentrations on tetrahydropalmatine was explored.【Results】The transdermal penetration effect of tetrahydropalmatine was relevant to its concentrations. The types and dosage of the penetration enhancers affected the transdermal penetration. The transdermal permeation rate of tetrahydropalmatine in a concentration of 250 μg/ml was faster. Compared with other penetration enhancers, the effect of 2% borneol was more powerful.【Conclusion】The transdermal penetration rate of tetrahydropalmatine can be significantly improved by choosing proper penetration enhancers. Therefore tetrahydropalmatine has the potential to be developed into a new transdermal preparation.