环己酮衍生物对吲哚美辛体外经皮吸收的影响。

Drug design and delivery Pub Date : 1989-06-01
Q Danyi, K Takayama, T Nagai
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引用次数: 0

摘要

我们之前已经证明了环己酮衍生物对吲哚美辛(IMC)的体内经皮吸收有促进作用,现在描述了体外渗透研究,以了解作用机制。体外实验结果与之前的体内实验结果一致。2-叔丁基环己酮是6种增强剂中最有效的。在含环己酮衍生物的缓冲液-辛醇体系中测定了环己酮衍生物的配分系数,并用亲脂指数讨论了这些衍生物的亲脂性。我们得出结论,环己酮衍生物通过流化或修饰角质层的硬疏水屏障,渗透到角质层,改变了IMC的皮肤渗透性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Effect of cyclohexanone derivatives on in vitro percutaneous absorption of indomethacin.

We have previously shown that cyclohexanone derivatives exert a promoting effect on the in vivo percutaneous absorption of indomethacin (IMC), and now describe in vitro permeation studies to gain understanding of the mechanism of action. The results of the in vitro experiment were consistent with those of the previous in vivo experiments. 2-tert-Butylcyclohexanone was the most effective of six enhancers examined. The partition coefficient of IMC was determined in a buffer-octanol system containing the cyclohexanone derivatives, and the lipophilicities of these derivatives are discussed using a lipophilic index. We conclude that the cyclohexanone derivatives penetrate into the stratum corneum and alter the skin permeability of IMC by fluidizing or modifying the hard hydrophobic barrier of the corneum.

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