Abstract: AimTo study bioequivalences of bambuterol and its metabolites terbutaline in 20 healthy male volunteers. MethodsA single oral dose of domestic bambuterol capsule or imported bambuterol tablet was given according to a randomized 2-way cross-over design. The plasma bambuterol and terbutaline concentrations were determined by high performance capillary zone electrophoresis (HPCZE). ResultsThe pharmacokinetic parameters of the capsule and tablet of bambuterol: AUC0-t were (72±18) and (72±13) μg·h·L^-1, C_max were (8.1±1.8) and (9.2±2.3) μg·L^-1, t_max were (3.6±1.3) and (3.7±1.0) h, respectively; terbutaline: AUC0-t were (129±32) and (130±34) μg·h·L^-1, C_max were (7.8±2.2) and (8.5±2.9) μg·L^-1, t_max were (5.4±0.8) and (5.6±1.1) h, respectively. The bioavaiability of the capsule was (100±16)% (bambuterol) and (101±13)% (terbutaline). Conclusion The results demonstrated that the two preparations of bambuterol and terbutaline were bioequivalent by analysis of variance, with two-one sided test at 90% confidential level.