数字中医药（英文）2018，Vol.1Issue(3)：198-210,13.
用药物代谢速度代替浓度线性化Hill量效曲线的研究
Study of Linearization of Hill Dose-Effect Curve with Metabolic Velocity Instead of Drug Concentration
摘要
Abstract
Objective To explore the velocity-effect relationship in order to the establish linearization of effect on an equation with regard to the consistency of the Hill dose-effect expression with the metabolic kinetics of receptors. Methods The linear velocity-effect expression was obtained by solving multivariant differential equation groups, which were established to compare the coincidences and basic relations between the Hill dose-effect and metabolic kinetic Michaelis-Menten equation for receptors. The validation test was conducted with acetylcholine, adrenaline, and their mixture as model drugs. Results The linear velocity-effect modelling was represented in vivo or in vitro, for single and multidrug systems. Pharmacodynamic parameters, especially suitable for multicomponent CMM formulas, could be determined and calculated for single or multicomponent formulas at high saturating or low linear concentration for receptors. The validation test showed that the pharmacodynamic parameters of acetylcholine were: k, 2.675×10-3 s-1; ka, 5.786×10-9 s-1; km, 2.500×10-7 s-1; α, 4.619×109 张 s· m g-1; E0, 13 张 (P < 0.01) and those of adrenaline were: k, 1.415×10-3 s-1; ka, 5.846×10-9 s-1; km, 2.300×10-7 s-1; α, -1.627×109 张 s· m g-1; E0, 9.2 张(P < 0.01). For the mixture of the two components, the values were: α, 1.375×1010 张 s· m g-1; -6.150×109 张 s m g-1 for acetylcholine and adrenaline, respectively, and E0 was 7.08 张in both, with the other parameters unchanged (P < 0.01). Conclusion The velocity-effect equation can linearize the Hilldose-effect relationship, which can be applied to study the pharmacodynamics and availability of CMM formulations in vivo and in vitro.关键词
Hill量效方程/速效方程/药(谱)效动力学/药(谱)效学/药(谱)动学/中药复方有效性/乙酰胆碱/肾上腺素/定量药理学引用本文复制引用
刘润南,邓凯文,唐昱,刘平安,刘文龙,樊启猛,陈思阳,贺鹏,李海英,贺福元..用药物代谢速度代替浓度线性化Hill量效曲线的研究[J].数字中医药（英文）,2018,1(3):198-210,13.基金项目
We thank for the funding support from the National Natural Science Foundation of China (No. 81073142 and No. 30901971). （No. 81073142 and No. 30901971）
