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封闭对两种具有不同理化性质的化合物体外经皮吸收的影响。

Effect of occlusion on in vitro percutaneous absorption of two compounds with different physicochemical properties.

作者信息

Treffel P, Muret P, Muret-D'Aniello P, Coumes-Marquet S, Agache P

机构信息

Service de Dermatologie, Hôpital St-Jacques, Besançon, France.

出版信息

Skin Pharmacol. 1992;5(2):108-13. doi: 10.1159/000211027.

Abstract

It is a general rule that percutaneous absorption is increased when the site of application is occluded. In this study we compared the in vitro permeation profiles of two molecules with different physicochemical properties under occluded versus unoccluded conditions. Human abdominal skin samples were mounted on Dianorm Teflon macro 1 cells and Franz diffusion cells which represented occluded or unoccluded conditions, respectively. Our data show that occlusion increased the permeation of citropten (lipophilic compound) 1.6 times whereas that of caffeine (amphiphilic compound) remained unchanged. This lack of penetration enhancement under occluded conditions has also been observed by other authors, especially concerning hydrophilic and slightly lipophilic molecules. Our results support the view that occlusion does not necessarily increase the percutaneous absorption of a chemical.

摘要

一般规则是,当应用部位被封闭时,经皮吸收会增加。在本研究中,我们比较了两种具有不同理化性质的分子在封闭与未封闭条件下的体外渗透曲线。将人腹部皮肤样本分别安装在代表封闭或未封闭条件的Dianorm特氟龙宏观1细胞和Franz扩散池中。我们的数据表明,封闭使柠檬苦素(亲脂性化合物)的渗透率提高了1.6倍,而咖啡因(两亲性化合物)的渗透率保持不变。其他作者也观察到在封闭条件下缺乏渗透增强的情况,尤其是关于亲水性和轻度亲脂性分子。我们的结果支持这样一种观点,即封闭不一定会增加化学物质的经皮吸收。

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