Bioequivalence of bicalutamide capsules and tablets in Chinese healthy volunteers

AIM:To establish a HPLC method for the determination of bicalutamide plasma concentration and to evaluate the bioequivalence of bicalutamide capsules(test)and tablets(reference).METHODS:A single oral dose of 50 mg bicalutamide capsules or tablets were given to 48 Chinese healthy volunteers in a one period parallel design test.The plasma concentrations of bicalutamide were determined by HPLC method and the pharmacokinetic parameters of bicalutamide test and reference were calculated and the bioequivalence was evaluated with DAS 2.0.RESULTS:The main pharmacokinetic parameters of bicalutamide test and reference were as follows,t_(1/2),(138±s 32)and(146±27)h,t_(max),(17±5)and(17±5)h,c_(max),(911±130) and(869±115)μg·L~(-1),AUC_(0-672),(172437±39863)and(176842±35734)μg·h·L~(-1),AUC_(0-∞), (179457±43128)and(185270±39689)μg·h·L~(-1),respectively.The two-one side t-test analysis showed that the confidence intervals of c_(max),AUC_(0-672)and AUC_(0～∞)were 98.9%-100.7%,98.8%-100.6% and 99.7%-101.7%,respectively.CONCLUSION:The relative bioavailability of bicalutamide capsules was 97.51% and the pharmacokinetic parameters of bicalutamide test and reference show no statistical difference and the two-one side t-test shows that they are bioequivalent.