Objective：To establish a LC-MS/MS method for the determination of faropenem in human urine，and to investigate its urinary excretion after intravenous administration of faropenem in healthy volunteers. Methods：The hydrochlorothiazide was using as the internal standard. Chromatographic separation was carried on a Waters Cortecs C18（2.1 mm × 50 mm，2.7 μm）. The mobile phase was consisted of acetonitrile and 0.5% formic acid（10∶90）. Electrospray ionization source was applied and operated in the negativeion mode using multiple reaction monitoring. Urinary excretion parameters were calculated after single and multiple intravenous administration of faropenem at 300 mg and 400 mg to healthy volunteers. Results：The calibration curve was linear in the range of 0.506-506.000 μg/mL. The accuracy，inter- and intra- precision were all below 15%. The matrix effect did not affect the determination results. Analytes were stable during the study. The average cumulative excretion and average cumulative excretion rates of faropenem in healthy volunteers after single intravenous infusion of 300 mg were（65.16 ± 43.63）mg and（21.7 ± 14.5）%，respectively. Conclusion：This method is suitable for the determination of faropenem in human urine.