PMID- 21362374
OWN - NLM
STAT- MEDLINE
DCOM- 20110804
LR  - 20171116
IS  - 2542-5641 (Electronic)
IS  - 0366-6999 (Linking)
VI  - 124
IP  - 2
DP  - 2011 Jan
TI  - Pharmacokinetic study of single and multiple oral dose administration of 
      antofloxacin hydrochloride in healthy male volunteers.
PG  - 242-5
AB  - 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-infinity)) of antofloxacin were (1.89 +/- 0.65) mg/L, 
      (1.29 +/- 0.26) hours, and (25.24 +/- 7.26) mgxh(-1)xL(-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) mgxh(-1)xL(-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-infinity) was (1.14 +/- 0.50) hours, (2.52 +/- 0.38) mg/L, and (48.77 +/- 8.44) 
      mgxh(-1)xL(-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.
FAU - Lu, Yuan
AU  - Lu Y
AD  - Institute of Clinical Pharmacology, First Hospital, Peking University, Beijing 
      100191, China. lyzx5857@163.com
FAU - Kang, Zi-Sheng
AU  - Kang ZS
FAU - Zhu, Yan
AU  - Zhu Y
FAU - Zhang, Ming
AU  - Zhang M
FAU - Liu, Yan
AU  - Liu Y
FAU - Zhang, Man
AU  - Zhang M
FAU - Li, Tian-Yun
AU  - Li TY
FAU - Xiao, Yong-Hong
AU  - Xiao YH
LA  - eng
PT  - Clinical Trial
PT  - Journal Article
PL  - China
TA  - Chin Med J (Engl)
JT  - Chinese medical journal
JID - 7513795
RN  - 0 (Anti-Bacterial Agents)
RN  - 56A192VX1Q (antofloxacin)
RN  - 6GNT3Y5LMF (Levofloxacin)
RN  - A4P49JAZ9H (Ofloxacin)
SB  - IM
MH  - Administration, Oral
MH  - Adolescent
MH  - Adult
MH  - Anti-Bacterial Agents/administration & dosage/blood/*pharmacokinetics/urine
MH  - Chromatography, High Pressure Liquid
MH  - Humans
MH  - *Levofloxacin
MH  - Male
MH  - Ofloxacin/administration & dosage/*analogs & 
      derivatives/blood/pharmacokinetics/urine
MH  - Young Adult
EDAT- 2011/03/03 06:00
MHDA- 2011/08/05 06:00
CRDT- 2011/03/03 06:00
PHST- 2011/03/03 06:00 [entrez]
PHST- 2011/03/03 06:00 [pubmed]
PHST- 2011/08/05 06:00 [medline]
PST - ppublish
SO  - Chin Med J (Engl). 2011 Jan;124(2):242-5.