Pharmacokinetics of antofloxacin hydrochloride, a novel fluoroquinolone, after single-dose intravenous administration in healthy Chinese male volunteers.
The purpose of the study was to evaluate the pharmacokinetic characteristics of a single, intravenous dose of antofloxacin hydrochloride in healthy Chinese male volunteers. Twelve subjects were randomly assigned to groups that received a single, intravenous dose of 200, 300, or 400 mg antofloxacin hydrochloride in a three-way crossover design study. The serum and urine concentrations of antofloxacin were then assayed with high-performance liquid chromatography (HPLC). Major pharmacokinetic parameters and urine excretion were obtained up to 96 h after administration. All three dosages were well tolerated. No clinically adverse reactions or abnormal laboratory results were detected. After single-dose intravenous administration, antofloxacin hydrochloride exhibited linear pharmacokinetic characteristics with increasing dosages. The C(max) for groups treated with 200, 300, or 400 mg dosages were 2.05 +/- 0.38, 3.01 +/- 0.60, and 3.80 +/- 0.78 mg l(-1), respectively; the areas under the curve from zero to infinity (AUC(0-infinity)) were 25.14 +/- 2.95, 37.63 +/- 5.42, and 53.87 +/- 9.48 mg l(-1).h, respectively. The t(1/2)(beta) was around 20 h; and the urinary excretion was measured as being from 58% to 60% within 96 h. Based on these results, 300 mg of antofloxacin hydrochloride administered once daily is the dose suggested for further investigation in multiple-dose administration studies.
Institute of Clinical Pharmacology, First Hospital, Peking University, Beijing China.
J
J
Wang
Y
Y
Xiao
Y
Y
Lu
Z
Z
Kang
M
M
Zhang
Y
Y
Liu
J
J
Liang
M
M
Zhang
T
T
Li
D000328:Adult; D044466:Asian People; D002681:China; D004305:Dose-Response Relationship, Drug; D024841:Fluoroquinolones / Q000008:administration & dosage* / Q000032:analysis / Q000737:chemistry / Q000493:pharmacokinetics*; D006262:Health; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D015242:Ofloxacin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000032:analysis / Q000737:chemistry / Q000493:pharmacokinetics; D013997:Time Factors; D055815:Young Adult
D024841:Fluoroquinolones; C522674:antofloxacin; D015242:Ofloxacin