Abstract: AIM: To establish an LC-MS-MS method for determination of faropenem in human plasma and investigate the pharmacokinetics of faropenem sodium granules in Chinese healthy volunteers. METHODS: 10 Healthy volunteers (5 male, 5 female) were given a 100 mg dose of faropenem sodium granules.The single dose and multiple dose experiment were carried out. Blood samples were collected from elbow vein, and trichloroacetic acid was used as protein precipitation agents. The analyte were detected by HPLC tandem triple stage quadrupole MS detector. RESULTS: Faropenem had a good linear range of 5.02-6528 ng/mL, with a limit of detection 2 ng/mL. The average recovery was more than 90%. The average RSD was within 10% for intra-batch and inter-batch precision. The major pharmacokinetic parameters of single dose administration were as follows: C_max (2322±1345) ng/mL; t_max (0.78±0.32) h; t_1/2(0.98±0.34) h; MRT(1.8±0.4) h;AUC_0-8(3953±1906) ng·mL^-1·h;AUC_0-∞(3980±1936) ng·mL^-1·h, and multiple dose administration as follows: C_ssmax (2870±1178) ng/mL; C_ssmin (72±55) ng/mL;C_ssav(658±439) ng/mL;t_max(0.80±0.20) h;t_1/2(0.91±0.16) h;AUC_ss(5263±3513)ng·mL^-1·h. CONCLUSION: The LC-MS-MS method is convenient, fast, sensitive and accurate. It is suit for determination of faropenem in human plasma. For the main pharmacokinetic parameters, there is no significant difference of between single dose and multiple doses, which indicates that there is not accumulation phenomenon.

Key words: Faropenem sodium granule, LC-MS-MS, Pharmacokinetics, Plasma concentration