Objective To evaluate the bioequivalence and safety of two kinds of tebipenem pivoxil granules in healthy Chinese volunteers under fasting and fed conditions. Methods This study was designed as a single-center, random, open-label, single dose, two-way crossover trail. A single oral dose of test formulation or reference formulation 1 package (50mg/0.5 g) was given in every period, and the cleaning period was 7 d. The plasma concentration of tebipenem was determined by HPLC-MS/MS, and the pharmacokinetic parameters were calculated, the bioequivalence and safety of the two formulations were evaluated. Results The main pharmacokinetic parameters of test and reference formulations under fasting conditions were as follow:C_(max)were (2 671.00±1 027.40)and (2 584.00±627.20) ng·m L∼(-1), AUC_(0-t)were (2 571.96±626.72) and (2 558.96±628.02) ng·h·m L∼(-1), AUC_(0-∞)were (2 594.91±621.55) and (2 582.37±626.94) ng·h·m L∼(-1), t_(max)were (0.43±0.17) and(0.45±0.08) h;the 90%confidence intervals for the ratios of C_(max), AUC_(0-t)and AUC_(0-∞)were 84.02%-115.95%, 94.23%-107.63%, 94.16%-107.72%. The main pharmacokinetic parameters of test and reference formulations under fed condition were as follows:C_(max)were (751.50±192.87) and (791.50±170.87) ng·m L∼(-1), AUC_(0-t)were(2 124.12±310.52) and (2 181.37±327.07) ng·h·m L∼(-1), AUC_(0-∞)were (2 145.08±312.39) and(2 212.74±329.67) ng·h·m L∼(-1), t_(max)were (1.83±0.84) and (1.91±0.74) h;the 90%confidence intervals for the ratios of C_(max), AUC_(0-t)and AUC_(0-∞)were 78.42%-113.13%, 92.46%-102.61%, 92.35%-101.81%. In addition to C_(max)of fed condition, the other parameters were within the bioequivalence range of 80.00%-125.00%. During the study period, 0 case and 2 cases of adverse events occurred under the fasting and the fed condition. No serious adverse events occurred. Conclusion The two kinds of tebipenem pivoxil granules were bioequivalent in human under the fasting condition, were not bioequivalent in human under fed condition, and the formulations were safe.