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目的:以毒理效应法和药理效应法分别测定麻黄汤的体内过程,比较两法的异同。方法:毒理效应法以小鼠死亡率为指标,不同时间先后2次ip麻黄汤19.69 g·kg-1测定其表观药动学参数;药理效应法采用大鼠酵母致热模型,以解热效应为指标,ig给予麻黄汤11.2 g·kg-1测定表观药动学参数。DAS 2.1.1程序拟合表观药动学数据并计算参数。结果:毒理效应法测得麻黄汤体内呈二室开放模型,主要药动学参数t1/2β=9.36 h,AUC=46.80 g·kg-1.h,CL=0.32(g·kg-1)/(h·g·kg-1)。药理效应法测得麻黄汤体内呈一室模型,主要药动学参数t1/2=4.15 h,AUC=55.01 g·kg-1.h,CL=0.27(g·kg-1)/(h·g·kg-1)。结论:2法测得参数存在一定差异,毒理半衰期长于效应半衰期。生物效应法可用于探讨中药方剂体内过程,但所得参数意义及数值均与经典药动学有差异。
OBJECTIVE: To determine the in vivo process of Mahuang Decoction by toxicological effect and pharmacological effects, and to compare the similarities and differences between the two methods. Methods: Toxicity effect method was used to measure the mortality of mice. The pharmacokinetic parameters were determined by the rat model of thermophilic yeast induced by 2 times ip ephedrine 19.69 g · kg-1 Thermal effect as an indicator, ig given ephedra Decoction 11.2 g · kg-1 determination of apparent pharmacokinetic parameters. The DAS 2.1.1 program fits the apparent pharmacokinetic data and calculates the parameters. The main pharmacokinetic parameters t1 / 2β = 9.36 h, AUC = 46.80 g · kg-1.h, CL = 0.32 (g · kg-1) / (h · g · kg -1). Pharmacodynamic method measured Mahuang decoction was a one-compartment model, the main pharmacokinetic parameters t1 / 2 = 4.15 h, AUC = 55.01 g · kg-1.h, CL = 0.27 (g · kg-1) / g · kg -1). Conclusion: There are some differences in the parameters measured by the method 2, toxicological half-life longer than the half-life of effect. Biological effect method can be used to explore the process of traditional Chinese medicine prescription, but the significance of the parameters and values are different from the classic pharmacokinetics.