摘要
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 evaluate the bioequivalence of tiopronine enteric capsules versus tablets. Method. A single oral dose of tiopronine enteric capsules or tablets 300rag was performed on 2 groups of 18 Chinese healthy volunteers （9 subjects for each group） in a randomized crossover protocol. The serum concentrations of tiopronine were measured by LC-MS . The pharmacokinetics parameters were calculated by a 3P97 pharmacokinetic program on a PC computer. Result： The pharmacokinetic parameters of tiopronine enteric capsules and tablets were as follows ： t （2.8 ± 0.5 ） and （2.6 ± 0.4） h , C,,a~ （ 1453.0 ± 263.1 ） and （ 1526.8 ± 288.1 ） ng·ml^-1, Tmax（3.3 ±0.3） and （3.1±0.5） h, AUC0-1（7414.3 ± 1248.3）and（8102.0 ± 1310.9）ng.h.ml^-1 ,AUC0-1 （7347.2 ± 1286.8）and （7902.8 ± 1 346.7 ） ng·h ^- 1·ml^- 1 , respectively. The relative bioavailability of tiopronine enteric capsules was （ 101.2± 5.4） %. Wilcoxon test showed non-significant difference between Tmax of the two formulas. The 90% confidential intervals of AUC0-1, and Cmax, were 98.8% -103.4% and 93.1% -97.5% , respectively. Conclusion： The tiopronine enteric capsules are bioequivalent compared with the tablets.
出处
《中国药师》
CAS
2007年第12期1183-1185,共3页
China Pharmacist
关键词
硫普罗宁
胶囊
片剂
液质联用法
生物等效性
Tiopronine
Capsule
Tablets
Liquid chromatography-mass spectrometry （LC-MS）
Bioequivalence
