Objective To study the bioequivalence of the single oral test nilotinib capsules and reference nilotinib capsules(Tasigna®)in Chinese healthy adult volunteers under fasting conditions.Methods This was a single-dose,randomized,open-label,double-sequence,two-period,crossover designed study.A total of 64 volunteers were enrolled under fasting condition.Volunteers were randomly divided into two groups(T-R and R-T),single oral test formulation 0.2 g and reference formulation 200 mg.The plasma concentrations of nilotinib were determined by a LC-MS/MS method.The pharmacokinetic parameters were calculated with WinNonlin® 8.2 and the bioequivalence was evaluated through SAS 9.4 software.Results After the volunteers administrated test and reference formulations under fasting conditions,the pharmacokinetic parameters of nilotinib as follows:Cmax of(507.67±155.96)and(457.95±176.30)ng/ml,AUC0-t of(10 293.63±3 634.11)and(9 810.67±3 929.39)ng·h/ml,AUC0-∞ of(10 900.19±4 237.58)and(10 814.34±4 871.26)ng·h/ml,respectively.The 90%confidential interval of the log-transformed Cmax,AUC0-t and AUC0-∞ for the test and reference formulation under fasting conditions were 107.62%～122.18%,101.62%～113.68%,98.24%～111.02%,respectively.Conclusion Two kinds of nilotinib capsules were bioequivalent in Chinese healthy volunteers.
维普
万方数据