OBJECTIVE:To determine the pharmacokinetics and relative bioavailability of oxetacillin and sulbactam in oxetacillin-sulbactam tablets.METHODS:20healthy male volunteers were randomly divided into2groups.In a crossover de?sign,a single oral dose of two tablets of domestic oxetacillin-sulbactam tablets or imported Tai Ba Meng LBL 500 tablets(one tablet of the two formulations contains oxetacillin250mg,sulbactam250mg)were given,then the drug concentrations in plas?ma were assayed by RP-HPLC.RESULTS:The pharmacokinetic parameters of oxetacillin in domestic and imported tablets were as follows:T max were(1.04?0.26)h and(1.10?0.28)h;C max were(5.16?1.30)mg/L and(5.25?1.21)mg/L;AUC 0～∞ were(13.30?3.12)mg/(h?L)and(13.33?3.53)mg/(h?L)respectively.The pharmacokinetic parameters of sulbactam in domestic and imported tablets were as follows:T max were(0.80?1.0)h and(0.81?0.17)h,C max were(5.73?1.44)mg/L and(5.70?1.46)mg/L,AUC 0～∞ were(13.25?2.41)mg/(h?L)and(13.28?2.26)mg/(h?L)respectively.CONCL_ USION:Domestic oxetacillin-sulbactam tablets and imported Tai Ba Meng LBL 500 tablets were bioequivalent.