Pharmacokinetic-pharmacodynamic modeling of daurisoline and dauricine in beagle dogs  

蝙蝠葛苏林碱和蝙蝠葛碱在犬体内的药动学-药效学模型(英文)

作　　者：师少军[1] 陈汇[1] 顾世芬[1] 曾繁典[1] 

机构地区：[1]华中科技大学同济医学院药理学系

出　　处：《Acta Pharmacologica Sinica》2003年第10期1011-1015,1062,共6页中国药理学报（英文版）

基　　金：Project supported by the Scientific Research Foundation of Committee of Science and Technology of Hubei Province. №991P1609.

摘　　要：AIM: To study the combined pharmacokinetic-pharmacodynamic(PK-PD) model of daurisoline and dauricine, and compare their effects on cardiac electrophsiology, blood pressure, and hemodynamics in beagle dogs. METHODS: The plasma drug concentration was determined by the reversed-phase HPLC method and the effects on cardiac and hemodynamics were recorded by polygraph. The pharmacokinetic and PK-PD model parameters were calculated. RESULTS: The pharmacokinetics were best fitted to a two-compartment open model, and the relationship between effect and effect compartment concentration of both drugs could be represented by the sigmoid-E_(max) model. There were no significant differences in main pharmacokinetics and PK-PD parameters between the two drugs. CONCLUSION: No statistically different kinetic disposition characteristics and potencies of inhibitory effects on myocardial function of daurisoline and dauricine were found in beagle dogs.目的:研究蝙蝠葛苏林碱和蝙蝠葛碱在beagle犬体内的药动学-药效学结合模型,并比较两种药物对其心电、血压和血流动力学的作用。方法:利用反相高效液相色谱法测定其血约浓度,生理记录仪观察药理效应,并计算药动学和药动学-药效学结合模型参数。结果:血药浓度-时间数据符合二房室开放模型,药效与效应室药物浓度之间的关系符合sigmoid-E_(max)模型,主要药动学和药动学-药效学结合模型参数在两种药物间差异无显著性。结论:蝙蝠葛苏林碱和蝙蝠葛碱在beagle犬体内的处置规律和对心血管系统的抑制作用基本一致。

关 键 词：DAURISOLINE DAURICINE PHARMACOKINETICS PHARMACODYNAMICS 

分 类 号：R285[医药卫生—中药学]