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经皮吸收动力学的扩散模型:4. 角质层内缓慢平衡过程对吸收和解吸动力学的影响。

Diffusion modelling of percutaneous absorption kinetics: 4. Effects of a slow equilibration process within stratum corneum on absorption and desorption kinetics.

作者信息

Anissimov Yuri G, Roberts Michael S

机构信息

School of Biomolecular and Physical Sciences, Griffith University, Nathan, Queensland, Australia.

出版信息

J Pharm Sci. 2009 Feb;98(2):772-81. doi: 10.1002/jps.21461.

Abstract

One of the main functions of the skin is to control the ingress and egress of water into and out of the body. The transport kinetics of water in the stratum corneum (SC), the dominant site of resistance in the skin, is normally described assuming a homogeneous membrane model. In the present work, the desorption of water from SC was studied and profiles obtained for amount desorbed versus time profiles that were more consistent with water transport occurring in a heterogeneous membrane. Analysis of the resulting profiles yields a model that is consistent with a slow equilibration/slow binding of water within SC as well as its permeation through the SC. Diffusion model solutions were used to derive the steady-state flux, lag time and mean desorption time for water in SC. The slow binding kinetics of water in the SC are limited and most pronounced in the early transient stages of transport and are not easily discerned using steady-state penetration studies. The practical importance of this work is in its use of desorption experiments to recognise and define the skin reservoir for water and other solutes as well as penetration parameters in defining their transdermal kinetics.

摘要

皮肤的主要功能之一是控制水进出身体。角质层(SC)是皮肤中主要的阻力部位,通常假定为均质膜模型来描述角质层中水的传输动力学。在本研究中,对水从角质层的解吸进行了研究,并获得了脱附量与时间的关系曲线,这些曲线与非均质膜中发生的水传输更为一致。对所得曲线的分析得出了一个模型,该模型与角质层内水的缓慢平衡/缓慢结合及其透过角质层的渗透相一致。利用扩散模型解来推导角质层中水的稳态通量、滞后时间和平均解吸时间。角质层中水的缓慢结合动力学是有限的,并且在传输的早期瞬态阶段最为明显,使用稳态渗透研究不易辨别。这项工作的实际重要性在于利用解吸实验来识别和定义皮肤中储存水和其他溶质的库,以及在定义它们的透皮动力学时的渗透参数。

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