Pharmacokinetics of pazufloxacin mesilate tablets in Chinese healthy volunteers

OBJECTIVE To investigate the pharmacokinetics of pazufloxacin mesilate tablets after oral administration in healthy volunteers.METHODS Thirty-four volunteers were divided into four groups,and were administrated orally with single doses (200 mg,400 mg,800 mg) and multiple doses of pazufloxacin mesilate tablets.The plasma concentrations of pazufloxacin mesilate were determined by HPLC and the pharmacokinetic parameters were calculated by DAS2.0 software.RESULTS The main pharmacokinetic parameters after single dose were as follows:Cmaxwas(6.1±1.1),(10.9±3.3),(20.5±5.2)mg·L-1 respectively;AUC0-∞ was(13.7±2.3),(28.9±5.7),(71.3±15.7)mg·h·L-1 respectively;Tmaxwas(0.6±0.3),(0.8±0.5),(0.9±0.4)h respectively;t1/2 was(1.8±0.4),(1.9±0.3),(1.90±0.20)h respectively.Cmax、AUC0-t、AUC0-∞are directly proportion to doses.After multi-dose,Cmax was (16.8±4.0)mg·L-1;Cmin was (0.13±0.06)mg·L-1,AUCss was(40.6±7.5)mg·h·L-1;Tmax was (0.8±0.6)h;t1/2 was (2.0±0.3)h.CONCLUSION The results showed that the pharmacokinetics of pazufloxacin mesilate in Chinese body is fit for two compartment model and exhibited linear pharmocokinetic characteristics over the dose range studied.Pazufloxacin would not be accumulated in the body after multiple doses.