title: Pharmacokinetic study of single and multiple oral dose administration of antofloxacin hydrochloride in healthy male volunteers.
abstract: BACKGROUND
  A new fluroquinolone antibacterial agent, antofloxacin hydrochloride, developed in China, is an 8-NH(2) derivant of levofloxacin. The purpose of the study was to evaluate the pharmacokinetic characteristics of single and multiple oral doses of antofloxacin hydrochloride in Chinese healthy male volunteers.
  
  
  METHODS
  An open-label, non-randomized, single and multiple dose clinical trial was conducted. In single dose study, 12 subjects took 200 mg antofloxacin hydrochloride. In multiple dose study, 12 subjects took antofloxacin hydrochloride 400 mg once on day 1 and 200 mg once daily from day 2 to day 7. HPLC was used to assay the serum and urinary concentrations of antofloxacin.
  
  
  RESULTS
  In single dose study, the maximum concentration of drug in serum (C(max)), the time to reach C(max) (T(max)), and the area under the serum concentration-time curve (AUC (0-∞)) of antofloxacin were (1.89 ± 0.65) mg/L, (1.29 ± 0.26) hours, and (25.24 ± 7.26) mg×h(-1)×L(-1), respectively. Accumulating elimination rate of antoflocaxin from urine within 120 hours was 39.1%. In multiple dose study, blood concentration of antofloxiacin achieved stable state on day 2 after dosing. The minimum concentration drug in serum (C(min)), AUCss, mean concentration of drug in serum (C(av)), and degree of fluctuation (DF) were (0.73 ± 0.18) mg/L, (47.59 ± 7.85) mg×h(-1)×L(-1), (1.98 ± 0.33) mg/L, and 1.74 ± 0.60, respectively. On day 7 after dosing, T(max), C(max), and AUC (0-∞) was (1.14 ± 0.50) hours, (2.52 ± 0.38) mg/L, and (48.77 ± 8.44) mg×h(-1)×L(-1), respectively. Accumulating elimination rate of antofloxaxin from urine within 120 hours after the last dosing was 60.06%.
  
  
  CONCLUSIONS
  The regimen of 400 mg loading dose given on the first treatment day and then 200 mg dose once daily results in satisfactory serum drug concentration.
authors.affiliation: Institute of Clinical Pharmacology, First Hospital, Peking University, Beijing 100191, China. lyzx5857@163.com
authors.forename: Yuan
authors.initials: Y
authors.lastname: Lü
authors.forename: Zi-Sheng
authors.initials: ZS
authors.lastname: Kang
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhu
authors.forename: Ming
authors.initials: M
authors.lastname: Zhang
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Man
authors.initials: M
authors.lastname: Zhang
authors.forename: Tian-Yun
authors.initials: TY
authors.lastname: Li
authors.forename: Yong-Hong
authors.initials: YH
authors.lastname: Xiao
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D064704:Levofloxacin; D008297:Male; D015242:Ofloxacin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000652:urine; D055815:Young Adult
chemical_list: D000900:Anti-Bacterial Agents; C522674:antofloxacin; D064704:Levofloxacin; D015242:Ofloxacin