论文部分内容阅读
目的用高效液相色谱-质谱法测定健康男性受试者单次空腹口服受试及参比托拉塞米片后的血药浓度,计算受试制剂和参比制剂的药动学参数,评价两种制剂是否生物等效。方法采取两制剂、双周期、交叉的设计试验,24例男性健康受试者单剂量口服受试制剂和参比制剂的托拉塞米片,以HPLC-MS测定血浆中的托拉塞米浓度。采用SPSS及BAPP2.2软件处理计算主要药动学参数。结果受试制剂与参比制剂中托拉塞米的ρ_(max)分别为(1 408.29±337.27)和(1 487.86±360.24)ng·mL~(-1),t_(max)分别为(0.90±0.42)和(1.03±0.50)h,t_(1/2)分别为(4.43±0.57)和(4.43±0.60)h,MRT分别为(3.90±0.60)和(4.01±0.72)h,AUC_(0-24 h)分别为(3 886.86±865.99)和(3 906.06±761.72)ng·h·mL~(-1),AUC_(0-∞)分别为(3 936.57±903.93)和(3 956.96±789.98)ng·h·mL~(-1)。按AUC_(0-24 h)和AUC_(0-∞)计算,受试制剂的相对生物利用度分别为(99.8±11.7)%和(99.7±12.0)%。结论两种制剂在健康人体内具有生物等效性。
Objective To determine the plasma concentration of single oral fasting oral test and reference torsemide tablet in healthy male subjects by high performance liquid chromatography-mass spectrometry (HPLC-MS), and to calculate the pharmacokinetic parameters of the test and reference preparations Whether two formulations are bioequivalent. Methods Two formulations, two-cycle and crossover design tests were conducted. Torasemide tablets of 24 male healthy subjects were tested by single-dose oral test formulation and reference formulation. The concentration of torsemide in plasma was determined by HPLC- . Using SPSS and BAPP2.2 software to calculate the main pharmacokinetic parameters. Results The maximal values of torsemide in test and reference preparations were (1 408.29 ± 337.27) and (1 487.86 ± 360.24) ng · mL -1, respectively, and the t max were 0.90 ± 0.42) and (1.03 ± 0.50) h, t 1/2 (4.43 ± 0.57) and (4.43 ± 0.60) h, respectively. MRT was (3.90 ± 0.60) and (4.01 ± 0.72) 0-24 h) were (3 886.86 ± 865.99) and (3 906.06 ± 761.72) ng · h · mL -1, respectively, and the AUC 0- ∞ were respectively (3 936.57 ± 903.93) and (3 956.96 ± 789.98) ng · h · mL -1. The relative bioavailabilities of the tested formulations were (99.8 ± 11.7)% and (99.7 ± 12.0)%, respectively, based on AUC_ (0-24 h) and AUC_ (0-∞) Conclusions Both formulations are bioequivalent in healthy humans.