Pharmacokinetic study of pazufloxacin mesylate in Chinese healthy volunteers

OBJECTIVE To investigate the pharmacokinetics of pazufloxacin mesylate in Chinese healthy volunteers.METHODS Twelve healthy volunteers were received a single dose(300 mg),then multi-doses(300 mg bid)within 30 min intravenous infusion of pazufloxacin mesylate in an open randomized cross-over study.The plasma concentration of pazufloxacin were determined by HPLC-fluorescence.RESULTS The quantitation limit was 0.028 mg·L-1 The relative standard deviations for within-day and between-day were all 5%,And the recoveris were 90%.A good linearity was obtained from 0.028 to 14.50 mg·L-1.The results showed that the plasma concentration-time curve conformed to two compatment model.Pharmacokinetic profiles were fitted to an open two-compartment model analyzed by using 3P97.The mean pharmacokinetic parameters of singl dose and multi dose were:Cmax(7.2±0.8)mg·L-1 and(7.3±0.8)mg·L-1;t1/2(2.04±0.17)h and(2.24±0.23)h;AUC0-t(14.0±1.5)mg·h·L-1 and(13.1±1.5)mg·h·L-1;Vc(27.2±4.6)L and(25.3±8.8)L;CL(22.1±2.6)L·h-1 and(23.7±2.1)L·h-1,respectively.No significant diference existed between a single dose and multiple doses.but significant diffences of T1/2 and MRT occurred within man and fimale whether by a single dose or multiple doses.CONCLUSION Pazufloxacin mesylate is tolerant with a single dose or multi-doses.by intravenous infusion in Chinese healthy volunteers.No accumulation in the body was observed after 5 days administration.Significant diference in pharmacokinetic parameters such as t1/2 and MRT may be due to sex differenc.