Mathematical analysis and drug exposure evaluation of pharmacokinetic models with endogenous production and simultaneous first-order and Michaelis–Menten elimination: the case of single dose
Mathematical analysis and drug exposure evaluation of pharmacokinetic models with endogenous production and simultaneous first-order and Michaelis–Menten elimination: the case of single dose
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内源性产生同时一级消除和米氏消除的药代动力学模型的数学分析和药物暴露评价：以单剂量为例
DOI：
10.1007/s10928-018-9599-4
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发表时间：
2018-07
影响因子：
2.5
通讯作者：
Jun Li
中科院分区：
文献类型：
--
作者：
Xiaotian Wu;Fahima Nekka;Jun Li
具有额外内源性来源的药物通常同时表现出一级消除和米氏消除，并在药代动力学模型中变得非常常见。在本文中，我们研究一室模型的单剂量静脉推注给药的情况。依赖于先前引入的超越函数，我们能够解析地表示该模型的血药浓度时程，并提供其各组分的药代动力学解释。利用修正浓度的概念，给出了浓度-时间曲线(AUC)下的部分面积和总面积的数学表达式。讨论了对校正浓度和AUC的影响，以及在存在内源生产时外源部分的相对贡献。这些发现从理论上阐明了所考虑的药物化合物的几个药代动力学问题，并为合理估计它们的药代动力学参数提供了指导。
Drugs with an additional endogenous source often exhibit simultaneous first-order and Michaelis–Menten elimination and are becoming quite common in pharmacokinetic modeling. In this paper, we investigate the case of single dose intravenous bolus administration for the one-compartment model. Relying on a formerly introduced transcendent function, we were able to analytically express the concentration time course of this model and provide the pharmacokinetic interpretation of its components. Using the concept of the corrected concentration, the mathematical expressions for the partial and total.areas under the concentration time curve (AUC) were also given. The impact on the corrected concentration and AUC is discussed as well as the relative contribution of the exogenous part in presence of endogenous production. The present findings theoretically elucidate several pharmacokinetic issues for the considered drug compounds and provide guidance for the rational estimation of their pharmacokinetic parameters.
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DOI：
10.1016/0022-247x(72)90034-0
发表时间：
1972-10
影响因子：
1.3
作者：
C. H. Anderson
通讯作者：
C. H. Anderson
DOI：
10.1007/bf01059062
发表时间：
1983-01-01
期刊：
JOURNAL OF PHARMACOKINETICS AND BIOPHARMACEUTICS
影响因子：
--
作者：
BEAL, SL
通讯作者：
BEAL, SL
影响因子：
1.7
作者：
Corless, RM;Gonnet, GH;Knuth, DE
通讯作者：
Knuth, DE
影响因子：
--
作者：
Scholz M;Schirm S;Wetzler M;Engel C;Loeffler M
通讯作者：
Loeffler M
影响因子：
3
作者：
A. Gouyette;D. Kerr;S. Kaye;A. Setanoians;J. Cassidy;C. Bradley;G. Forrest;M. Soukop
通讯作者：
A. Gouyette;D. Kerr;S. Kaye;A. Setanoians;J. Cassidy;C. Bradley;G. Forrest;M. Soukop