Díez Sales O, López Castellano A, Maiques Lacer F J, Herráez Domínguez M
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Valencia, Spain.
Pharmazie. 1993 Sep;48(9):684-6.
Generally, the mechanisms of percutaneous absorption are studied from correlations between representative penetration parameters (permeability coefficients) and variables accounting for lipophilicity or other related physicochemical properties. The present study was developed on the basis of the in vitro permeability coefficients through human skin, 280 microns in thickness, of a non-ionic homologous series of compounds (phenylalkanols). The corresponding penetration/lipophilicity correlations were compared with those found for a basic homologous series (4-n-alkylanilines) through a membrane of similar characteristics. The in vitro behaviour of both series of compounds may be regarded as similar. Differences were only observed in the permeability coefficients of those elements which in both series exhibited lipophilicity values above that considered optimum, as predicted by the selected biophysical penetration model. Consequently, it appears that the removal of the thick dermal tissue leads to increased permeation rates for the more lipophilic compounds and suggests that the dermis acts as an aqueous matrix.
一般来说,经皮吸收机制是通过代表性渗透参数(渗透系数)与反映亲脂性或其他相关物理化学性质的变量之间的相关性来研究的。本研究基于一系列非离子型同系物(苯基链烷醇)通过厚度为280微米的人体皮肤的体外渗透系数展开。将相应的渗透/亲脂性相关性与通过具有相似特性的膜的碱性同系物系列(4-正烷基苯胺)的相关性进行了比较。这两个系列化合物的体外行为可视为相似。如所选生物物理渗透模型所预测的,仅在两个系列中亲脂性值高于最佳值的那些元素的渗透系数中观察到差异。因此,似乎去除厚的真皮组织会导致亲脂性更强的化合物的渗透速率增加,这表明真皮起到了水性基质的作用。