Enhancing effect of piperidone derivatives on the percutaneous absorption of indomethacin.

Drug design and delivery Pub Date : 1990-05-01
D Y Quan, R I Higuchi, K Takayama, K Higashiyama, T Nagai
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Abstract

Following our previous demonstration that Azone and 2-n-alkylcyclohexanones enhanced the percutaneous absorption of indomethacin, six 1-n-alkylpiperidones were prepared and examined as potential transdermal absorption enhancers. In vitro skin experiments showed that indomethacin absorption enhancement was related to the lipophilicity of the enhancer, and that 1-n-dodecyl piperidone caused the greatest enhancement. The structure of this piperidone is similar to that of Azone, and both compounds had similar lipophilicity and drug absorption enhancement activity. We suggest that they act in the same way by decreasing diffusional resistance in the stratum corneum, and so modifying the hard barrier of the stratum corneum.

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哌啶酮衍生物对吲哚美辛经皮吸收的促进作用。
根据我们之前的研究,氮酮和2-n-烷基环己酮增强了吲哚美辛的透皮吸收,我们制备了6种1-n-烷基哌啶酮,并对它们作为潜在的透皮吸收促进剂进行了研究。体外皮肤实验表明,吲哚美辛的吸收增强作用与增强剂的亲脂性有关,其中1-十二烷基哌酮的增强作用最大。该哌酮的结构与氮酮相似,具有相似的亲脂性和增强药物吸收活性。我们认为它们通过降低角质层的扩散阻力,从而改变角质层的硬屏障,以相同的方式起作用。
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