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目的:建立人血浆中硫普罗宁浓度的LC-MS/MS测定方法,研究硫普罗宁在健康人体内的药动学行为,评价2种制剂的生物等效性。方法:20例健康志愿者交叉口服试验制剂硫普罗宁片剂或参比制剂硫普罗宁肠溶胶囊200mg,血药浓度-时间数据经DAS2.0统计软件处理,计算主要药动学参数,并对2种制剂进行等效性评价。结果:硫普罗宁在4.05～8100μg·L-1范围内线性关系良好,最低检测为4.05μg·L-1。方法回收率(n=5)为85.0%～91.3%,日内和日间精密度均小于15%。硫普罗宁片剂与肠溶胶囊的主要药动学参数分别是:Cmax为(2151.1±1135.0)μg·L-1和(2363.0±1055.1)μg·L-1;tmax分别为(4.8±1.3)h和(4.3±1.2)h;AUC(0-t)分别为(11618.2±3625.5)μg·h·L-1和(12824.0±4464.1)μg·h·L-1;AUC(0-∞)分别为(12677.7±3874.9)μg·h·L-1和(13803.1±4686.0)μg·h·L-1。结论:该法操作简单、灵敏度高、专属性强;统计学分析结果显示2种制剂具有生物等效性。
OBJECTIVE: To establish a LC-MS / MS method for the determination of tiopronin in human plasma. To study the pharmacokinetics of tiopronin in healthy volunteers and evaluate the bioequivalence of the two preparations. Methods: Twenty healthy volunteers were given oral administration of test compound tiopronin tablet or reference preparation tiopronin enteric-coated capsules 200mg, blood concentration-time data by DAS2.0 statistical software to calculate the main pharmacokinetic parameters, and The two formulations were evaluated for equivalence. Results: There was a good linear relationship of tiopronin in the range of 4.05 ~ 8100μg · L-1, the lowest detection was 4.05μg · L-1. The recovery rate (n = 5) was 85.0% ~ 91.3%. The intra- and inter-day precision was less than 15%. The main pharmacokinetic parameters of tiopronin and enteric capsules were: Cmax (2151.1 ± 1135.0) μg · L-1 and (2363.0 ± 1055.1) μg · L-1, respectively; tmax was (4.8 ± 1.3) h and (4.3 ± 1.2) h, AUC (0-t) were (11618.2 ± 3625.5) μg · h · L -1 and (12824.0 ± 4464.1) μg · h · L -1, respectively (12677.7 ± 3874.9) μg · h · L-1 and (13803.1 ± 4686.0) μg · h · L-1. Conclusion: The method is simple, sensitive and specific, and the statistical analysis shows that the two preparations are bioequivalent.