经皮吸收促进剂对左旋18-甲基炔诺酮穿透离体大鼠皮肤的影响(英文)

Penetration of Levonorgestrel In Vitro Through Excised Rat Skin by Enhancers

本文研究了多种物质对左旋18-甲基炔诺酮经离体大鼠皮肤的促进作用。结果表明,乙酸乙酯、乙醇或二者的复合溶剂均能有效地促进左旋18-甲基炔诺酮经皮渗透。同时,还首次发现异丙醇肉豆蔻酯对该药物具有促渗效果。左旋18-甲基炔诺酮的经皮渗透阻力及促进剂的作用部位研究表明,该药物的渗透阻力主要来自表皮层,促进剂的增强效应是通过其对表皮层的作用而实现。

Development of ideal transdermal delivery system of Levonorgestrel (LN) requires effective penetration enhancer. Some substances were tested in this research. The results demonstrated that ethyl acetate (EtAc), ethanol (EtOH) alone, or their combination were effective in LN permeation. Isopropyl myristate (IPM) being used as an effective enhancer for LN penetration was first recommended. The skin resistance to LN's permeation and the penetration enhancing effect by EtOH had also been studied. It was found that epidermis provides more important diffusional resistance with comparison of stratum corneum. EtOH promotes LN permeation by its action on epidermis.