角质层与活性皮肤层对硝酸异山梨酯透皮吸收的影响

Influence of Stratum Corneum and Viable Layer of Skin on the Iransdermal Absorption of Isosorbide Dinitrate

目的:评价皮肤角质层和真皮层对药物经皮吸收的影响。方法:以硝酸异山梨酯(ISDN)为模型药物,采用Franz吸收池法,考察药物单独或与吸收促进剂肉豆蔻酸异丙酯(IPM)合用时,经完整皮肤和角质层剥离皮肤的透皮能力。结果:IS-DN经剥离角质层皮肤的表观透皮系数的Kp是经完整皮肤的1.68倍,IPM能分布在活性皮肤层,并可明显增加ISDN在角质层或真皮层的分布量及经皮累积透皮吸收百分率。结论:本实验为研究皮肤病态条件下(如皮肤受伤或溃疡等),药物透皮吸收规律,提供了一种新的方法。

Objective: To study the influence of stratum comium and viable layer of skin on the transdermal absorption of drug. Method: Isosorbide dinitrate (ISDN)was served as a model drug, patch containing saturated concentration of ISDN with isopropyl myristate (IPM) were prepared. The transdermal permeation experiments via different rat's skin layers were carried out in vitro. Results: The Kp of ISDN via stripped skin was about 1.68 times higher than that of intact skin, IPM could distribute into the viable layer of skin, and significantly increasing the distributing amount ISON in the of ISDN in the stratum corneum and the viable layer of skin as well as an absorbed amount of transdermal accumulation. Conclusion:This test provides a novel approach to evaluate the effects of skin damage and skin disease in transdermal drug absorption.