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肠道吸收-分配关系:一个试探性的功能性非线性模型。

Intestinal absorption-partition relationships: a tentative functional nonlinear model.

作者信息

Plá-Delfina J M, Moreno J

出版信息

J Pharmacokinet Biopharm. 1981 Apr;9(2):191-215. doi: 10.1007/BF01068082.

Abstract

Models and equations designed to elucidate passive intestinal absorption mechanisms by analysis of the relationship between the absorption rate constant (ka) and either the partition coefficients (P) or a related partition constant for homologous series of substances, are reviewed. Classical nonlinear physical models, such as those which assume the existence of a nonstirred layer or equilibrium extraction, predict sigmoidal or hyperbolic relationships between ka and P, whereas other models, which regard the membrane as a heterogeneous multicompartment system, predict parabolic or bilinear relationships between log ka and log P. In the present paper, an alternative model is proposed, which incorporates the Wagner-Sedman equilibrium extraction model together with the existence of pores, which play a fundamental role for compounds below 250 in molecular weight. Several apparently contradictory absorption-partition literature data are shown to be highly consistent with the tentative model proposed.

摘要

通过分析吸收速率常数(ka)与物质同系物的分配系数(P)或相关分配常数之间的关系来阐明被动肠道吸收机制的模型和方程进行了综述。经典的非线性物理模型,如假设存在非搅拌层或平衡萃取的模型,预测ka与P之间呈S形或双曲线关系,而其他将膜视为异质多隔室系统的模型,则预测log ka与log P之间呈抛物线或双线性关系。在本文中,提出了一种替代模型,该模型将瓦格纳-塞德曼平衡萃取模型与孔隙的存在相结合,孔隙对分子量低于250的化合物起着重要作用。一些明显相互矛盾的吸收-分配文献数据被证明与所提出的暂定模型高度一致。

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