依普利酮在健康志愿者体内代谢物依普利酮酸的药代动力学研究

The Pharmacokinetic Study of the Metabolite of Eplerenone in the Human Body After Administration

目的对单次给药后,依普利酮在健康志愿者体内代谢物依普利酮酸的药代动力学进行研究。方法健康志愿者单次服用不同剂量依普利酮片后,采用液相色谱串联质谱法测定依普利酮的代谢物依普利酮酸的浓度,用DAS2.0药动学软件计算药动学参数。结果单次口服25、50、100mg依普利酮片的主要药代动力学参数:t1/2分别为(4.2±1.6)、(4.5±2.3)、(5.1±1.3)h;Cmax分别为(151.5±38.36)、(203.9±60.49)、(543.0±139.8)ng/ml;AUC(0-30)分别为(756.7±300.4)、(1103±363.0)、(2660±638.0)μg.h/L。结论在25～100mg给药剂量范围内,依普利酮片在体内呈现线性药代动力学特征。

Objective To investigate the pharmacokinetics of eplerenone′s open-lactone-ring form （EPA） in Chinese healthy volunteers after a single-dose administration.Methods Liquid chromatography/tandem mass spectrometry was used for the determination of EPA in plasma after a single oral dose of eplerenone tablets by healthy volunteers.The important pharmacokinetic parameters were caculated by DAS 2.0.Results The main pharmacokinetic parameters of EPA were as follows：t1/2 was （4.2±1.6）,（4.5±2.3） and （5.1±1.3） h;Cmax was （151.5±38.36）,（203.9±60.49） and （543.0±139.8） ng/ml;AUC（0-30） was （756.7±300.4）,（1103±363.0） and（2660±638.0） μg·h/L,respectively for a single-dose administration of 25,50,100 mg eplerenone in Chinese healthy volunteers.Conclusion The pharmacokinetic parameters of EPA are linear in the dose range from 25-100 mg eplerenone.