中枢神经系统的药代动力学参数及其意义

血脑屏障可阻碍药物进入中枢神经系统。本文系统介绍了中枢神经系统的药代动力学研究常用的几个参数:PS积、内清除率(Kin,CLin,)、外清除率(Kout,CLout)、T1/2eq,in、摄取百分比(%ID/g)、脑/血分配系数(Kp,Kp,u和Kp,uu),游离药物表观分布容积(Vu,brain)和脑内药物半衰期(T1/2,brain)。其中,PS积用来评价药物通过血脑屏障的能力、内清除率(Kin,CLin,)、外清除率(Kout,CLout)、T1/2eq,in、T1/2,brain用来描述药物进出中枢神经系统内的速度;%ID/g、Kp,uu用来评价药物进入大脑的程度;Vu,brain评价药物在脑内的分布特点。

Pharmacokinetic parameters and its significances in central nervous system

It is popularly accept that blood-brain barrier affects drug transport and distribution.Pharmacokinetic parameters will help us predict the pharmacological action,drug-interactions and adverse reaction.This article reviewed the major pharmacokinetic parameters in central nervous system,such as PS product(permeability surface area product),Kin or CLin(influx clearance into the brain),Kout or CLout(efflux clearance from the brain),T1/2eq,in(intrinsic brain equilibrium half-life),%ID/g(percent of injected dose...