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口腔药物吸收研究:影响仓鼠颊囊吸收的物理化学因素。

Studies on drug absorption from oral cavity: physicochemical factors affecting absorption from hamster cheek pouch.

作者信息

Kurosaki Y, Aya N, Okada Y, Nakayama T, Kimura T

出版信息

J Pharmacobiodyn. 1986 Mar;9(3):287-96. doi: 10.1248/bpb1978.9.287.

Abstract

A new experimental method using a hamster cheek pouch in vivo for studying absorption processes across the keratinized oral mucous membrane was developed and some characteristics of the oral-mucosal absorption were clarified. A positive correlation between the absorption rate and the lipophilicity was observed in 18 aromatic compounds examined. The absorption of ionizable compounds was poor in the ionized form. These results suggest that the absorption from the keratinized hamster cheek pouch is due to a passive diffusion mechanism and obeys pH-partition hypothesis. The systemic transfer of salicylic acid after intra-cheek-pouch administration could be approximated by the first-order absorption model including a lag time process and the plasma levels found were consistent with this model.

摘要

开发了一种新的实验方法,即利用金黄地鼠颊囊在体内研究角质化口腔黏膜的吸收过程,并阐明了口腔黏膜吸收的一些特性。在所检测的18种芳香族化合物中,观察到吸收速率与亲脂性之间呈正相关。可电离化合物以离子形式存在时吸收较差。这些结果表明,角质化金黄地鼠颊囊的吸收是由于被动扩散机制,并且符合pH分配假说。颊囊内给药后水杨酸的全身转运可以用包含滞后时间过程的一级吸收模型来近似,并且所测得的血浆水平与该模型一致。

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