苯磺酸氨氯地平片人体生物等效性研究

Bioequivalent of amlodipine besylate tablets in healthy volunteers

目的:评价苯磺酸氨氯地平片的人体生物等效性。方法:20名男性健康志愿者随机交叉口服苯磺酸氨氯地平片试验制剂和参比制剂各10 mg,采用液相-串联质谱法(LC-MS/MS)测定血药浓度。以DAS2.0软件计算其药动学参数,考察其生物等效性。结果:苯磺酸氨氯地平片试验制剂和参比制剂的Tmax、Cmax、AUC0-144、AUC0-∞分别为(5.60±3.09)h和(6.30±2.85)h、(8.19±2.2)μg/L和(8.22±1.99)μg/L、(366±100)μg.L-1.h-1和(385.8±80)μg.L-1.h-1、(397±115)μg.L-1.h-1和(421±83)μg.L-1.h-1。以AUC0-144计算,苯磺酸氨氯地平片试验制剂和参比制剂比较的人体相对生物利用度为(96.1±26.6)%。结论:试验制剂苯磺酸氨氯地平片和参比制剂苯磺酸氨氯地平片具有生物等效性。

Objective：To investigate the bioequivalence of amlodipine besylate tablets in healthy volunteers. Methods： A single oral dose of 10 mg test or reference formulations were given to 20 male healthy volunteers in a randomized crossover design. The serum concentration of amlodipine was determined by LC-MS/MS method. Pharmacokinetic parameters and relative bioavailability were calculated with DAS 2.0 program to evaluate the bioequivalence of the two formulations. Results： Pharmacokinetic parameters of amlodipine besylate test formulation were obtained as follows ：Tmax was （5.60 ± 3.09 ） h ,Cmax was （8.19 ± 2.2 ） μg/L, AUC0-144 was （ 366 ± 100） μg · L^ -1 · h^ - 1, AUC0-∞ was （ 397 ± 115 ） μg · L^ - 1 ±· h ^- 1. For reference formulation ： Tmax was （ 6.30 ± 2.85 ） h, Cmax, was （8.22 ±1.99）μg/L,AUC0-144 was （385.8 ±80） μg · L^-1 μ· h^-1 ,AUC0-∞ was （421 ±83） μg · L^-1 · h^-1. Calculated with AUC0- 144, the bioavailability of two formulation was （ 96. 1 ± 26.6 ） %. Conclusions： The amlodipine besylate tablets test formulation and reference formulation were bioequivalent.