Single-dose pharmacokinetics and dose proportionality of intravenous pazufloxacin mesilate in healthy Korean volunteers.
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 C(max) for groups treated with 300, 500, 600, and 1,000 mg doses ranged from 5.11 to 18.06 μg/mL; the mean AUC(0-t) ranged from 13.70 to 58.60 μg × h/mL. Pazufloxacin exhibits Lack of dose proportionality was concluded 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.
Kyungpook National University Graduate School and Hospital, Department of Biomedical Science and Clinical Trial Center, Daegu, Republic of Korea.
Joomi
J
Lee
Sook Jin
SJ
Seong
Mi-sun
MS
Lim
Sung Min
SM
Park
Jeonghyeon
J
Park
Jeong Ju
JJ
Seo
Hae Won
HW
Lee
Young-Ran
YR
Yoon
D061605:Administration, Intravenous; D000328:Adult; D019540:Area Under Curve; D044466:Asian People; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D024841:Fluoroquinolones / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D006801:Humans; D016014:Linear Models; D008297:Male; D008698:Mesylates / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D010078:Oxazines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D056910:Republic of Korea; D055815:Young Adult
D024841:Fluoroquinolones; D008698:Mesylates; D010078:Oxazines; C078052:pazufloxacin