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目的:建立LC-MS法测定人血中硫普罗宁的药物浓度,并对2种制剂进行生物等效性评价。方法:20例健康受试者单剂量交叉口服400mg硫普罗宁供试制剂或参比制剂后,采用LC-MS测定人血中不同时间点硫普罗宁的浓度,计算其药代动力学参数和相对生物利用度,评价两制剂的生物等效性。结果:硫普罗宁供试制剂和参比制剂主要药代动力学参数如下:Cmax分别为(2.31±0.64)、(2.33±0.83)μg/ml,AUC0-15分别为(6.70±1.57)、(6.68±1.53)μg·h·ml-1,Tmax分别为(3.1±0.7)、(3.7±0.6)h,t1/2分别为(3.08±0.86)、(2.90±0.84)h。本方法在0.04～10.0μg/ml浓度范围内线性关系良好。最低定量浓度为0.04μg/ml,两制剂主要药动学参数经统计学检验无显著性差异。结论:本方法简单、快速、准确,2种制剂具有生物等效性。
OBJECTIVE: To establish a LC-MS method for the determination of tiopronin in human blood and evaluate the bioequivalence of the two preparations. Methods: The concentrations of tiopronin in human blood at different time points were determined by LC-MS after taking a single dose of 400 mg tiopronin in 20 healthy subjects. The pharmacokinetic parameters and Relative bioavailability was evaluated for bioequivalence of both formulations. RESULTS: The main pharmacokinetic parameters of tiopronin were (2.31 ± 0.64), (2.33 ± 0.83) μg / ml and AUC0-15 (6.70 ± 1.57) and ( 6.68 ± 1.53) μg · h · ml-1 respectively. The Tmax values were (3.1 ± 0.7) and (3.7 ± 0.6) h respectively, and the values of t1 / 2 were (3.08 ± 0.86) and (2.90 ± 0.84) h, respectively. The method in the range of 0.04 ~ 10.0μg / ml linearity good. The lowest quantitative concentration of 0.04μg / ml, two formulations of the main pharmacokinetic parameters by statistical tests showed no significant difference. Conclusion: The method is simple, rapid and accurate. The two preparations have bioequivalence.