Study on Pharmacokinetics and Pharmacodynamics of Pazufloxacin Mesilate in Healthy Volunteers

Objective:To investigate the pharmacokinetics and pharmacodynemics of Pazufloxacin mesilate injection.Methods:Twelve healthy volunteers were administrated 500mg Pazufloxacin mesilate single and multiple-doses intravenously.The plasma and urine concentrations were determined by RPHPLC-UV method and the pharmacokinetic parameters were calculated by DASver1.0 software.Rusults:The pharmacokinetics of pazufloxacin is fit to two compartment model.The pharmacokinetic parameters after single administration:Tmax was 0.47±0.09h,Cmax was 13.71±1.81mg/L,AUC0-t was 24.60±4.15mgh/L,T1/2 was 1.46±0.64h.The pharmacokinetic parameters after successive administration:Tmax was 0.48±0.10h,Cmax was 15.41±1.67mg/L,AUC0-t was 8.42±4.90mg·h/L,T1/2 was 1.33±0.49h,(Css)av was 2.34±0.43mg/L,DF was 99.48±0.38%.There were no significant differences in all pharmacokinetic parameters except Cmax between the first and the last administraion of Pazufloxacin and cumulation coefficient was very small.That indicates there may have no accumulation after successive administration.No serious adverse effect was observed in volunteers.Conclusion:Effective concentration in vivo could achieved after intravenous infusion of 500mg Pazufloxacin mesilate twice a day and there may have no accumulation in human body for 5 days administration.The dosing schedule was recommended.