用小鼠急性死亡率法测定4-苯基丁酮-2的表观药动学参数

Determination of Apparent Pharmacokinetic Parameters of 4-phenylbutanone-2 by Acute Mortality of Mice

本文采用小鼠急性死亡率法。测定了4-苯基丁酮-2的药动学参数。ip4-苯基丁酮-2在小鼠体内的经时过程为二房室开放模型。用最小二乘法和残余量法求得α、β、A、B四项表观动力学参数分别为1.809h^(-1),0.126h^(-1),507mg/kg(125.9％)和228mg/kg(56.7％)。按药动学公式分别求得分布相表观半寿期(t_(1/2))和消除相表现半寿期为(t 1/2β0.38h和5.50h;表观转运速率常数k_(12)、k_(21)、k_(10)分别为0.935h^(-1),0.648h^(-1)和0.352h^(-1);观表观曲线下面积(AVC)为2090mg.h/kg;表观清除率是0.19kg/kg;;表观分布容积v、v_c、v_p分别是1.530kg/kg、0.548kg/kg、0.982kg/kg。

Apparent pharmacokinetic parameters of 4-phenylbutanone-2, a antianssive, were determined by acute mortality of mice. Experimental results were as follows; The ip LD_(50) and 95% confidence limit of 4-phenylbutanone-2 in mice were 582.90± 31.03 / mg/ kg,The distribution and elimination phase of a two compartment models can be seen before and after 2.ohours respectively. Their pharmacokinetic parameters are: apparent rate constants of distribution phase and elmination phase, 1\809^(-1) and 0\126h^(-1), respectively; the apaarent residual % at zero hours of distribution phase and eliminfion phase, 125.9 and 57.7, respective; their corresponding resicluul amount. 507mg / kg and 228mg / kg.respectively; aparent half-lives of distribution phase and 228mg / kg.respectively; apparent half—lives of distrbution phase and elimination phsae, 0\4h and 5\5h, respectively; apparent AUS, 2090mg.h/kg, apparent clearance, 0.19kg/(kg.h), apparent distribution volume of center compartment (Vc), 0.55kg / kg; apparent distribution volume of peripheral compartment (VP), 0.98kg/kg; total apparent distribution volume (V), 1.53kg/kg; apparent rate constants k_(12), K_(21) and k_(10), 0.935h^(-1) 0.648h^(-1) and 0.352h^(-1), respectively.