Abstract: AIM　To study bioequivalence of bambuteral and its metablites terbutaline in 20 healthy male volunteers. METHODS　A single oral dose of domestic or imported bambuteral tablet was given according to a randomized 2-way cross-over design. The plasma bambuteral and terbutaline concentrations were determined by HPLC/MS. RESULTS　The pharmacokinetic parametrs of domestic and imported bambuteral: AUC_0-t were (52±21) μg·h·L^-1 and (51±20) μg·h·L^-1, T_max were (2.9±0.9) h and (2.6±0.7) h, C_max were (6.0±2.6) μg·L^-1 and (6.2±2.9) μg·L^-1, T_1/2Ke were (11.2±2.3) h and (11.2±1.9) h, respectively; terbutaline: AUC_0-t were (191±30) μg·h·L^-1 and (197±37) μg·h·L^-1; T_max were (4.2±1.0) h and (4.2±1.0) h; C_max were (10±5) μg·L^-1 and (10±4) μg·L^-1; T_1/2Ke were (20±3) h and (21±4) h, respectively. The bioavaiability of the domestics was 102%±8% (bambuteral) and 100%±12% (terbutaline). CONCLUSION　The results demonstrate that the two forms of bambuteral and terbutaline were bioequivalent by analysis of variance, two-one sided test and 90% confidential limit.