|Pharmacokinetics of antofloxacin hydrochloride in healthy male subjects after multiple intravenous dose administration|
|Wang, J.; Xiao, Y.; Lu, Y.; Kang, Z.; Zhang, M.; Liu, Y.; Liang, J.; Zhang, M.; Li, T.|
|关键词||Antofloxacin hydrochloride multiple-dose pharmacokinetics intravenous healthy male volunteers|
|WOS标题词||Science & Technology|
|类目[WOS]||Pharmacology & Pharmacy ; Toxicology|
|研究领域[WOS]||Pharmacology & Pharmacy ; Toxicology|
|关键词[WOS]||CHINESE MALE-VOLUNTEERS ; FLUOROQUINOLONE ; LEVOFLOXACIN ; RATS|
The purpose of the study was to evaluate pharmacokinetic characteristics of antofloxacin hydrochloride, a new fluoroquinolone antibiotic, during a multiple, intravenous dosing regimen.
Twelve healthy, Chinese male volunteer subjects were each given 300 mg of antofloxacin by intravenous infusion once daily for 7 days. Blood and urine samples were taken at designated time points for analysis of antofloxacin concentration by high-performance liquid chromatography (HPLC). Safety and tolerability were assessed by evaluation of subject complaints, vital signs, electrocardiograms, electroencephalograms, clinical chemistry parameters, haematology and urinalysis and prothrombin time.
The serum steady concentration of antofloxacin was obtained in 96 h after the administration of a daily intravenous dose of 300 mg of the drug. In the present study, the following pharmacokinetic parameters after 7 days of treatment with antofloxacin were determined to be: C(max) 3.81 +/-+/- 0.66 mg/L, C(min) 0.85 +/-+/- 0.19 mg/L, AUC(0--24) 60.51 +/-+/- 8.30 mg/L center dot center dot h, C(av) 2.52 +/-+/- 0.35 mg/L, PTF 87.45 +/-+/- 3.37%, t(1/2)beta beta 20.34 +/-+/- 1.88 h. The C(max) and AUC(0--24) after 7-day treatment were both higher than after the first dose (by 43% and 110%, respectively). The cumulative urinary elimination of antofloxacin within 96 h after the last dose was about 56%.
During the study, there were neither subject complaints nor significant adverse clinical findings.
Antofloxacin, administered intravenously as a single, daily 300 mg dose for 7 days, demonstrated favourable pharmacokinetic characteristics and tolerability. The results of this study indicate that antofloxacin hydrochloride is suitable for further clinical study.
|作者单位||Peking Univ, Inst Clin Pharmacol, Hosp 1, Beijing 100191, Peoples R China|
|Wang, J.,Xiao, Y.,Lu, Y.,et al. Pharmacokinetics of antofloxacin hydrochloride in healthy male subjects after multiple intravenous dose administration[J]. XENOBIOTICA,2011,41(7):561-566.|
|APA||Wang, J..,Xiao, Y..,Lu, Y..,Kang, Z..,Zhang, M..,...&Li, T..(2011).Pharmacokinetics of antofloxacin hydrochloride in healthy male subjects after multiple intravenous dose administration.XENOBIOTICA,41(7),561-566.|
|MLA||Wang, J.,et al."Pharmacokinetics of antofloxacin hydrochloride in healthy male subjects after multiple intravenous dose administration".XENOBIOTICA 41.7(2011):561-566.|