Pharmacokinetics of antofloxacin hydrochloride, a novel fluoroquinolone, after single-dose intravenous administration in healthy Chinese male volunteers

Abstract

1. The purpose of the study was to evaluate the pharmacokinetic characteristics of a single, intravenous dose of antofloxacin hydrochloride in healthy Chinese male volunteers.

2. 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.

3. All three dosages were well tolerated. No clinically adverse reactions or abnormal laboratory results were detected.

4. 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–∞) were 25.14 ± 2.95, 37.63 ± 5.42, and 53.87 ± 9.48 mg l⁻¹·h, respectively. The t_1/2β was around 20 h; and the urinary excretion was measured as being from 58% to 60% within 96 h.

5. Based on these results, 300 mg of antofloxacin hydrochloride administered once daily is the dose suggested for further investigation in multiple-dose administration studies.

Keywords::

• Antofloxacin hydrochloride
• pharmacokinetics
• single
• intravenous dose
• healthy Chinese male volunteers
• serum

Acknowledgements

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.