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[用于生理药代动力学模型的组织-血液分配系数R的评估]

[Evaluation of the tissue-to-blood partition coefficient R for physiological pharmacokinetic models].

作者信息

Ding Y, Huang D K, Luo J P

机构信息

Nanjing Medical College, Department of Biomathematics, China.

出版信息

Zhongguo Yao Li Xue Bao. 1992 Jul;13(4):345-8.

PMID:1456057
Abstract

The tissue-to-blood partition coefficient R, fraction of drug unbound in blood fB and intrinsic clearance of elimination organ/tissue Cl'L are important parameters used in physiological pharmacokinetic models. Simple equations to evaluate R by AUC were derived in this paper for single bolus iv, the tissue-to-blood partition coefficient of nonelimination organ/tissue was exactly the ratio of AUC between tissue and blood, those equations were examined by the experimental data of rats following iv ethoxybenzamide 20 mg.kg-1, and compared with other methods. Equations to evaluate fBCl'L and other parameters were also given for linear elimination model.

摘要

组织-血液分配系数R、血液中游离药物分数fB以及消除器官/组织的内在清除率Cl'L是生理药代动力学模型中使用的重要参数。本文推导了通过AUC评估R的简单方程用于单次静脉推注,非消除器官/组织的组织-血液分配系数正是组织与血液之间AUC的比值,这些方程通过静脉注射20mg·kg-1乙氧基苯甲酰胺后大鼠的实验数据进行了检验,并与其他方法进行了比较。对于线性消除模型,还给出了评估fBCl'L和其他参数的方程。

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