Objective To investigate the
pharmacokinetics of
gatifloxacin methanesulfonate after multiple-dose administration in Chinese
healthy volunteers. Methods The protocal was designed according to GCP principle. The 10 selected healthy male volunteers in 18-40 year old were administrated 400mg
gatifloxacin methanesulfonate once a day for 10 days. The peak and trough concentrations were monitoring everyday. The plasma concentrations were determined by HPLC method and the parameters of pharmacokinetics were calculated by 3P97 software. Results It is two compartment model in vivo after gatifloxacin was administrated in volunteers. The AUC0-8, and AUC0-t, on the 10th day were significantly increased compared with the 1st administration, but there was no significant difference between AUC0-t on 10th day and AUC0-8 on 1st day .The other parameters Cmax t1/2βVd neither. The mean stable concentration Cav was 0.84 ± 0.18 mg·L-1, AUCSS was 26.16±4.53 mg.h-L-1.The accumulation ratio was 1.35±0.87 and fluctuation coefficient was 1.68 ±0.16. There was no significant difference in valley and peak concentrations of 10th day and the 1st day. No serious adverse effect was observed in volunteers. Conclusion Effective concentration in vivo could achieved after intravenous infusion of 400mg gatifloxacin
Methanesulfonate once a day for 10 days and no accumulation in human body was observed for 10 days administration. The dosing schedule was recommended.