ABSTRACT
AIM: To study the pharmacokinetics of multiple doses intravenous infusion of levofloxacin instillation in Chinese healthy volunteers. METHODS: Intravenous infusion of levofloxacin instillation 200 mg within 60 min was given to 10 male healthy volunteers for 7 d, on d 1 and d 7, once-daily, from 2-6 d twice-daily dosing. The concentrations of levofloxacin in serum and urine were assayed by HPLC. RESULTS: The main pharmacokinetic parameters af ter the first dosing were as follows: Cmax was (2.4+/-0.4) mg/L; AUC0- was (16.1 +/- 1.4) mg . h . L-1; T1/2beta was (6.3 +/- 0.3) h. The concentration in serum reached steady state within 72 h. The main parameters after the last dosing were as follows: Cssmax was (2.9 +/- 0.4) mg/L; Cssmin was (0.71 +/- 0.19) mg/L; Cav was (1.40 +/- 0.29) mg/L; AUCss0-12 was (17 +/- 3) mg . h . L-1; T1/2beta was (6.2 +/- 0.8) h. The 24-h cumulative urinary excretion rate was (88 +/- 5) %. From the calculation, the cumulative rate was 1.20; the fluctuation index was 1.30. The difference of T1/2beta and AUC between the first dosing and the last dosing was not significant, and the elimination rate of levofloxacin was not changed after multiple dosing. No clear adverse events were noted during this study. CONCLUSION: There was no accumulation of drug after the repeated intravenous infusion with 200 mg levofloxacin instillation for 7 d.
