A method to determine pharmacokinetic parameters based on andante constant-rate intravenous infusion

作者：Yu, Rui-hong; Cao, Yong-xiao^*

来源：Scientific Reports, 2017, 7(1): 13279.

DOI：10.1038/s41598-017-13437-6

On account of the disturbance from the distribution phase, the concentration-time curve of drugs cannot fully reflect the characteristics of elimination, and thus, it is difficult for present methods to obtain ideal pharmacokinetic parameters. This paper presents a method to determine pharmacokinetic parameters based on an andante constant-rate intravenous infusion. A mathematical model of the constant-rate intravenous infusion combined with the elimination of first-order kinetics was established. During infusion, the accumulation tendency of drugs was deduced as C-t = C-0 +(C-ss - C-0) (1 - e(-Kt)) using the principle of calculus. Then, the method to determine the pharmacokinetic parameters was summed up. After collecting the blood drug concentration (C-t) -time (t) data from a constant-rate (v) infusion period, an exponential regression analysis was conducted to obtain the elimination rate constant (K) and plateau concentration (C-ss). Then, the half-life (t(1/2)), apparent volume of distribution (V-d) and clearance rate (CL) were calculated based on the equations, t(1/2) = 0.693/K, V-d = (v/K)/C-ss and CL = v/C-ss, respectively. In addition, an application example of cimetidine in a beagle dog was used to demonstrate the implementation process of the method.

• 出版日期2017-10-16
• 单位西安交通大学