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目的:研究国产与进口硫酸氢氯吡格雷片在健康人体内的药动学特征及生物等效性。方法:采用标准两周期交叉设计自身对照试验方法,20名健康志愿者单剂量口服硫酸氢氯吡格雷片受试制剂(国产)或参比制剂(进口)75mg后,用液-质联用(LC-MS)法测定人血浆中氯吡格雷的浓度,计算其药动学参数并评价2种制剂的生物等效性。结果:受试制剂与参比制剂的各主要药动学参数分别为:tmax(0.64±0.21)、(0.68±0.27)h,cmax(1.724±1.38)、(1.752±1.856)ng·mL-1,t1/2(6.6±4.9)、(6.3±7.0)h,AUC0～36h(1.996±1.223)、(2.112±1.493)ng·h·mL-1,AUC0～∞(2.114±1.209)、(2.117±1.500)ng·h·mL-1。受试制剂相对于参比制剂的生物利用度为(108.9±52.2)%。结论:2种硫酸氢氯吡格雷片具有生物等效性。
Objective: To study the pharmacokinetics and bioequivalence of domestic and imported clopidogrel bisulfate tablets in healthy volunteers. Methods: The standard two-cycle crossover design of self-control test method, 20 healthy volunteers single oral dose of clopidogrel hydrogen sulfate tablets test preparations (domestic) or reference preparation (import) 75mg, with liquid chromatography - LC-MS) was used to determine the concentration of clopidogrel in human plasma. The pharmacokinetic parameters were calculated and the bioequivalence of the two preparations was evaluated. Results: The main pharmacokinetic parameters of test preparation and reference preparation were: tmax (0.64 ± 0.21), (0.68 ± 0.27) h, cmax (1.724 ± 1.38), (1.752 ± 1.856) ng · mL -1 , AUC0 ~ ∞ (2.114 ± 1.209), (2.117 ± 1.209), AUC0 ~ 36h (1.996 ± 1.223), (2.112 ± 1.493) ng · h · mL- ± 1.500 ng · h · mL-1. The bioavailability of the test formulation relative to the reference formulation was (108.9 ± 52.2)%. Conclusion: Two kinds of clopidogrel bisulfate tablets are bioequivalent.