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[两种形态学上均一的法莫替丁口服制剂在中国健康志愿者体内的药代动力学和药效学研究]

[Pharmacokinetics and pharmacodynamics of two morphologically homogenous forms of famotidine per os in Chinese healthy volunteers].

作者信息

Liu G L, Gao S, Wang S X, Shen W J, Tan J Q

机构信息

Department of Clinical Pharmacology, Changhai Hospital, Second Military Medical University, Shanghai, China.

出版信息

Zhongguo Yao Li Xue Bao. 1993 May;14(3):257-9.

PMID:8237405
Abstract

The lg C of famotidine (Fam) A and B forms in plasma vs time curve following a single oral dose of 40 mg showed an one-compartment open model in 5 healthy volunteers. The T1/2Ke of Fam A and B forms = 3.06 and 3.48 h, Tmax = 2.96 and 2.68 h, The Cmax = 115 and 145 ng.ml-1, AUC = 811 and 1190 h.ng.ml-1, respectively. No significant difference was found in the pharmacokinetic and pharmacodynamic properties between Fam A and B forms. The mathematical model describing the whole course of blood concentration of Fam A and B forms in relation to inhibiting effects on gastric acid were: E (A) = 100.C2.04/(C2.04 + 15.0(2.04)) and E (B) = 100.C1.67/(C1.67 + 14.0(1.67)). Predication of blood drug concentration from pharmacodynamics or vice versa became possible using the mathematical equations.

摘要

在5名健康志愿者单次口服40毫克后,法莫替丁(Fam)A和B型在血浆中lg C与时间曲线显示为一室开放模型。Fam A和B型的T1/2Ke分别为3.06和3.48小时,Tmax分别为2.96和2.68小时,Cmax分别为115和145 ng.ml-1,AUC分别为811和1190 h.ng.ml-1。Fam A和B型在药代动力学和药效学特性方面未发现显著差异。描述Fam A和B型血药浓度全过程与胃酸抑制作用关系的数学模型为:E(A)=100.C2.04/(C2.04 + 15.0(2.04))和E(B)=100.C1.67/(C1.67 + 14.0(1.67))。使用这些数学方程可以实现从药效学预测血药浓度,反之亦然。

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