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目的:研究硫普罗宁肠溶胶囊与片剂在健康人体的生物等效性。方法:18例健康受试者采用双用期交叉试验,单剂量口服硫普罗宁肠溶胶囊剂或片剂300mg,LC-MS法测定血清中硫普罗宁浓度,3P97软件拟合主要药动学参数,并进行2种制剂的生物等效性评价。结果:硫普罗宁肠溶胶囊与片剂的主要药动学参数分别为:t_(1/2)(2.8±0.5)和(2.6±0.4)h,C_(max) (1453.0±263.1)和(1526.8±288.1)ng·ml~(-1),T_(max)(3.3±0.3)h和(3.1±0.5)h,AUC_(0-1)(7414.3±1248.3)和(7347.2±1286.8)ng·h·ml~(-1),AUC_(0-∞)(8102.0±1310.9)和(7902.8±1346.7)ng·h·ml~(-1)。肠溶胶囊与片剂比较相对生物利用度为(101.2±5.4)%。两药T_(max)差异无统计学意义,肠溶胶囊AUC_(0→t)和C_(max)的90%可信限分别落在片剂的98.8%～103.4%和93.1%～97.5%。结论:两种制剂生物等效。
Objective: To study the bioequivalence of tiopronin enteric-coated capsules and tablets in healthy volunteers. Methods: Eighteen healthy volunteers were enrolled in this study. A single oral dose of tiopronin enteric-coated capsules or tablets 300 mg, the concentration of tiopronin in serum was determined by LC-MS, and the pharmacokinetics Parameters, and bioequivalence evaluation of two formulations was performed. Results: The main pharmacokinetic parameters of tiopronin enteric-coated capsules and tablets were: t 1/2 (2.8 ± 0.5) and (2.6 ± 0.4) h, C max (1453.0 ± 263.1) and 1526.8 ± 288.1 ng · ml -1, T max (3.3 ± 0.3) h and (3.1 ± 0.5) h, AUC 0-1 (7414.3 ± 1248.3) and (7347.2 ± 1286.8) ng · h · ml ~ (-1), AUC_ (0-∞) (8102.0 ± 1310.9) and (7902.8 ± 1346.7) ng · h · ml ~ (-1) respectively. The relative bioavailability of enteric capsules and tablets was (101.2 ± 5.4)%. The T_ (max) of the two drugs showed no significant difference. The 90% confidence limits of AUC_ (0 → t) and C_max of enteric-coated capsules were 98.8% ~ 103.4% and 93.1% ~ 97.5% of the tablets, respectively. Conclusions: Both formulations are bioequivalent.