![Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days]({"type":"image" , "src" : "/sda/5925/TOC-Subject-Sample-2021-Bioscience.jpg"})
Abstract
Objective: The aim of this study was to investigate the pharmacokinetics and dose proportionality of a single, intravenous dose of pazufloxacin mesilate, an injectable fluoroquinolone antibiotic, in healthy Korean male volunteers.
Methods: In this open-label, four-dose, parallel study, subjects were randomized to receive a single dose of pazufloxacin mesilate 300, 500, 600, and 1,000 mg (n = 6, 20, 6, and 8, respectively) administered as a 1-h intravenous infusion. Blood and urine samples were collected serially from 0 to 24 h after drug administration and analyzed using a validated HPLC method. Tolerability was assessed by monitoring clinical laboratory parameters and adverse events.
Results: After single-dose intravenous administration of pazufloxacin mesilate, the mean Cmax for groups treated with 300, 500, 600, and 1,000 mg doses ranged from 5.11 to 18.06 μg/mL; the mean AUC0-t ranged from 13.70 to 58.60 μg × h/mL. Pazufloxacin exhibits lack of dose proportionality over the dose range of 300 – 1,000 mg, based on linear regression model and power model. At all four dosages studied, pazufloxacin mesilate was well tolerated.
Conclusions: Our data suggest that all regimens of pazufloxacin administration were well tolerated. Pazufloxacin exhibits lack of dose proportionality over the dose range of 300 – 1,000 mg.
Acknowledgements
There is some overlap (in part) between this manuscript and an abstract that was presented (poster) at the annual meeting of the American Society of Clinical Pharmacology and Therapeutics (ASCPT; March 18–21, 2009; in Washington DC, USA). The authors would like to thank SW Kim, DDS, HanAll BioPharma Co. Ltd, SI Lee, HanAll Pharmaceutical Co. Ltd, and JH Park, HanAll Pharmaceutical Co. Ltd, for their helpful comments. J Lee and SJ Seong contributed equally to this work.