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某些氨基苯丙酮的经皮吸收与代谢评估

Evaluation of the percutaneous absorption and metabolism of some aminopropiophenones.

作者信息

Markantonis S L, Kyroudis A, Beckett A H

出版信息

J Pharm Pharmacol. 1986 Jul;38(7):515-9. doi: 10.1111/j.2042-7158.1986.tb04626.x.

Abstract

The absorption of diethylpropion (DEP I), dimethylpropion (DMP I) and some of their basic metabolites into and passage through the skin was investigated and a comparison of their metabolism following oral and percutaneous administration made. High percentages (60-80%) of DEP I and its metabolites and a small percentage of DMP I and its metabolites were taken up into the skin in less than 2 min--the remaining percentages of the compounds were absorbed into the skin by a first order process. The rate of appearance of the compounds in the blood, which reflects their rate of passage through the skin, did not correlated with their rate of absorption into the skin. More metabolism occurred with all the compounds after their oral administration than after their percutaneous application.

摘要

研究了二乙丙胺(DEP I)、二甲丙胺(DMP I)及其一些碱性代谢产物的经皮吸收及透皮过程,并对口服和经皮给药后的代谢情况进行了比较。在不到2分钟的时间内,DEP I及其代谢产物的高比例(60 - 80%)被皮肤吸收,而DMP I及其代谢产物只有小比例被吸收,其余部分的化合物则以一级过程被皮肤吸收。化合物在血液中的出现速率反映了它们透过皮肤的速率,这与它们被皮肤吸收的速率并无关联。所有化合物口服给药后的代谢比经皮给药后更多。

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