Pharmacokinetics and bioequivalence of carvedilol tablets in healthy volunteers

Objective: To investigate the pharmacokinetics and relative bioavailability of carvedilol tablets in healthy volunteers,and to evaluate the bioequivalence.Methods: A single oral dose of 12.5 mg test or reference carvedilol tablets was given to 20 male healthy volunteers in a randomized,two-way crossover study.The concentration of carvedilol in plasma was determined by LC-MS.The pharmacokinetics parameters and relative bioavailability were calculated with DAS 2.0 software to evaluate the bioequivalence of the two preparations.Results: The main pharmacokinetic parameters of test and reference preparations were as follows: t1/2(9.05±4.49) and(8.64±4.99) h;Tmax(1.00±0.57) and(0.90±0.81) h;Cmax(50.7±30.9) and(50.2±24.3) ng·mL-1;AUC0~48h(205.5±123.7) and(182.3±93.6)ng·h·mL-1;AUC0~∞(211.5±124.0) and(187.2±94.2) ng·h·mL-1,respectively.The differences of the major pharmacokinetic parameters between test and reference tablets were not significant.The relative bioavailability was(110.5±33.5)%.Conclusion: The statistical analysis of the results shows that the two preparations are bioequivalent.