OBJECTIVE To study the
pharmacokinetics and relative bioavailability of
tropisetron hydrochloride capsules in healthy volunteers
and to evaluate the bioequivalence.METHODS A single dose of 10 mg reference and test tropisetron capsules was given to 18 healthy volunteers in a randomized 2-way cross-over study.The concentrations of
tropisetron hydrochloride in plasma were determined by RP-HPLC-UV.RESULTS The main pharmacokinetic parameters of two formulations,reference and test drug were as follows:t_(max)(1.86±0.43) and(2.03±0.52)h,ρ_(max)(11.73±3.05) and(11.25±3.30) μg·L~(-1),AUC_(0～24)(111.89±39.86) and(113.61±40.34) μg·h·L~(-1);AUC_(0-inf)(139.71±60.35) and(142.22±57.34) μg·h·L~(-1),t_(1/2(kα))(0.79±0.29) and(0.82±0.25)h;t_(1/2(ke))(5.08±1.92) and((5.48±2.08)) h,Ke(0.16±0.06) and(0.14±0.05) h~(-1),respectively.The relative bioavailability of AUC_(0～24) and AUC_(0-inf) were(98.55±10.37)% and(99.77±18.66)%.Using 3P97 program,the results of variance and two one-sided test statistical analysis for Lnρ_(max),LnAUC_(0～24) and LnAUC_(0-inf) showed that two formulations were bioequivalent.CONCLUSION The reference and test tropisetron capsules are bioequivalent.