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模型渗透剂在人体皮肤中的蒸汽扩散和液体扩散;与热力学活性的相关性。

Vapour and liquid diffusion of model penetrants through human skin; correlation with thermodynamic activity.

作者信息

Barry B W, Harrison S M, Dugard P H

出版信息

J Pharm Pharmacol. 1985 Apr;37(4):226-36. doi: 10.1111/j.2042-7158.1985.tb05050.x.

Abstract

This work investigates vapour and liquid permeation through human skin of model penetrants benzyl alcohol, benzaldehyde, aniline, anisole and 2-phenylethanol applied in model vehicles butanol, butyl acetate, isophorone, isopropyl myristate, propylene carbonate, toluene, n-heptane and water. Vapour permeation was a linear function of thermodynamic activity as measured by headspace gas chromatography, except when the vehicle was n-heptane. Liquid permeation did not always follow simple thermodynamic predictions, e.g. for the penetrant, benzyl alcohol, when the vehicle damaged the skin (toluene, n-heptane) or when propylene carbonate produced low fluxes and isopropyl myristate, high values. At comparable thermodynamic activities, liquid fluxes were often ten-fold higher than vapour fluxes, and these differences were reflected by the partition coefficients and the amount of penetrant entering the stratum corneum membrane. The conclusion was that liquid fluxes were membrane controlled, whereas an interfacial effect probably contributed to low vapour permeation.

摘要

本研究考察了模型渗透剂苯甲醇、苯甲醛、苯胺、苯甲醚和2-苯乙醇在模型载体丁醇、乙酸丁酯、异佛尔酮、肉豆蔻酸异丙酯、碳酸丙烯酯、甲苯、正庚烷和水中时,通过人体皮肤的蒸汽渗透和液体渗透情况。除了载体为正庚烷时,蒸汽渗透是通过顶空气相色谱法测得的热力学活度的线性函数。液体渗透并不总是遵循简单的热力学预测,例如对于渗透剂苯甲醇,当载体损害皮肤时(甲苯、正庚烷),或者当碳酸丙烯酯产生低通量而肉豆蔻酸异丙酯产生高通量时。在相当的热力学活度下,液体通量通常比蒸汽通量高一个数量级,这些差异通过分配系数和进入角质层膜的渗透剂量得以体现。结论是液体通量受膜控制,而界面效应可能导致了低蒸汽渗透。

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