渗透
亲脂性
化学
人体皮肤
硅酮
分配系数
色谱法
膜
对羟基苯甲酸酯
合成膜
溶解度
氟比洛芬
磁导率
有机化学
生物化学
防腐剂
药理学
生物
医学
遗传学
作者
Takashi Uchida,Masafumi Yakumaru,Keisuke Nishioka,Yoshihiro Higashi,Tomohiko Sano,Hiroaki Todo,Kenji Sugibayashi
出处
期刊:Chemical & Pharmaceutical Bulletin
[Pharmaceutical Society of Japan]
日期:2016-01-01
卷期号:64 (9): 1338-1346
被引量:19
标识
DOI:10.1248/cpb.c16-00322
摘要
We evaluated the effectiveness of a silicone membrane as an alternative to human skin using the skin permeation parameters of chemical compounds. An in vitro permeation study using 15 model compounds was conducted, and permeation parameters comprising permeability coefficient (P), diffusion parameter (DL(-2)), and partition parameter (KL) were calculated from each permeation profile. Significant correlations were obtained in log P, log DL(-2), and log KL values between the silicone membrane and human skin. DL(-2) values of model compounds, except flurbiprofen, in the silicone membrane were independent of the lipophilicity of the model compounds and were 100-fold higher than those in human skin. For antipyrine and caffeine, which are hydrophilic, KL values in the silicone membrane were 100-fold lower than those in human skin, and P values, calculated as the product of a DL(-2) and KL, were similar. For lipophilic compounds, such as n-butyl paraben and flurbiprofen, KL values for silicone were similar to or 10-fold higher than those in human skin, and P values for silicone were 100-fold higher than those in human skin. Furthermore, for amphiphilic compounds with log Ko/w values from 0.5 to 3.5, KL values in the silicone membrane were 10-fold lower than those in human skin, and P values for silicone were 10-fold higher than those in human skin. The silicone membrane was useful as a human skin alternative in an in vitro skin permeation study. However, depending on the lipophilicity of the model compounds, some parameters may be over- or underestimated.
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