Pharmacokinetics of faropenem sodium for injection after a single and multiple intravenous dose in healthy volunteers / 中国药理学通报

ABSTRACT

Aim To study the pharmacokinetics of faropenem sodium for injection after a single and multiple intravenous dose in 12 healthy volunteers.Methods Multiple-dose regiments used 12-hour dosing intervals for 5 doses.Plasma and urine faropenem sodium concentrations were measured using high-performance liquid chromatography.The concentration-time curves of faropenem sodium were fitted to a two-compartment open model.The excretion data in urine were disposed by the method of excretion rate in urine.Results The pharmacokinetic parameters obtained from the single-dose study were as follows: C_(max) =(45.20±8.73) mg·L ~(-1); T_(1/2α) =(0.401±0.096) h; T_(1/2β) =(1.419±0.267) h;AUC_(0-12) =(59.216±11.886) mg·h·L~(-1) .The steady-state pharmacokinetic parameters were: C ss min =(0.03±0.02) mg·L~(-1) ; C ss max =(44.60±9.08) mg·L~(-1) ; C_(av)=(4.939±1.048) mg·L~(-1) ; T_(1/2α) =(0.340±0.105) h; T_(1/2β) =(1.257±0.173) h;AUC~(ss)_(0-12) =(59.268±12.571) mg·h·L~(-1) .The amount of cumulative recovery of faropenem sodium in urine for single and multiple dose within 12 h was(30.48±12.77)% and (40.55±17.53)%, respectively.The pharmacokinetic parameters in urine of the single-dose study were: T_(1/2) =(0.993±0.088) h, K_e=(0.227±0.097) h~(-1) .The steady-state pharmacokinetic parameters in urine were: T_(1/2) =(1.085±0.069) h, K_e=(0.296±0.136) h~(-1) .Conclusions The distribution and elimination rates of faropenem sodium for injection are not changed after multiple intravenous administrations.Effective concentrations in vivo can be achieved after the repeated administration with 400 mg twice a day regiment.The dosing schedule can be recommended.