使用人工膜Strat-M™预测化合物的皮肤渗透情况。
Prediction of skin permeation by chemical compounds using the artificial membrane, Strat-M™.
作者信息
Uchida Takashi, Kadhum Wesam R, Kanai Sayumi, Todo Hiroaki, Oshizaka Takeshi, Sugibayashi Kenji
机构信息
Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
出版信息
Eur J Pharm Sci. 2015 Jan 25;67:113-118. doi: 10.1016/j.ejps.2014.11.002. Epub 2014 Nov 14.
PURPOSE
The usefulness of the synthetic membrane, Strat-M™ as an alternative to human and animal skins was evaluated by estimating the skin permeabilities of chemical compounds.
METHOD
Thirteen chemical compounds with molecular weights (M.W.) of 152-289 and lipophilicities (log Ko/w) of -0.9 to 3.5 were selected. Strat-M™, excised human skin, or hairless rat skin was set in a Franz-type diffusion cell and a saturated solution of each chemical compound was applied to determine membrane permeation profiles. The obtained permeability coefficients (log P) were compared among these membranes.
RESULTS AND DISCUSSION
Elevations were observed in log P for Strat-M™ with an increase in the log Ko/w of the applied compounds, and similar results were observed with the human and hairless rat skins. A correlation was obtained in log P values between Strat-M™ and human or hairless rat skin. Furthermore, the diffusion and partition parameters of chemicals in Strat-M™ were similar to those in the excised human and rat skins. These results suggest that Strat-M™ could be used as an alternative to animal or human skin in permeation studies.
目的
通过评估化合物的皮肤渗透性，来评价合成膜Strat-M™作为人和动物皮肤替代品的有效性。
方法
选择了13种分子量为152 - 289且亲脂性（log Ko/w）为 - 0.9至3.5的化合物。将Strat-M™、切除的人皮肤或无毛大鼠皮肤置于Franz型扩散池中，并施加每种化合物的饱和溶液以测定膜渗透曲线。比较了这些膜获得的渗透系数（log P）。
结果与讨论
随着所施加化合物log Ko/w的增加，Strat-M™的log P升高，人皮肤和无毛大鼠皮肤也观察到类似结果。Strat-M™与人或无毛大鼠皮肤的log P值之间存在相关性。此外，Strat-M™中化学物质的扩散和分配参数与切除的人皮肤和大鼠皮肤中的相似。这些结果表明，Strat-M™可作为渗透研究中动物或人皮肤的替代品。
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