Disposition, metabolism and mass balance of delafloxacin in healthy human volunteers following intravenous administration

被引:20
|
作者
McEwen, Andrew [1 ]
Lawrence, Laura [2 ]
Hoover, Randy [2 ]
Stevens, Lloyd [3 ]
Mair, Stuart [3 ]
Ford, Gill [1 ]
Williams, Dylan [1 ]
Wood, Stuart [1 ]
机构
[1] Quotient Biores, Dept Metab, Pegasus Way, Rushden NN106ER, Northants, England
[2] Melinta Therapeut Inc, New Haven, CT USA
[3] Quotient Clin, Nottingham, England
关键词
Delafloxacin; human; metabolism; quinolone;
D O I
10.3109/00498254.2015.1042946
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. The pharmacokinetics and disposition of delafloxacin was investigated following a single intravenous (300 mg, 100 mu Ci) dose to healthy male subjects. 2. Mean C-max, AUC(0-infinity), T-max and t(1/2) values for delafloxacin were 8.98 mu g/mL, 21.31 mu g h/mL, 1 h and 2.35 h, respectively, after intravenous dosing. 3. Radioactivity was predominantly excreted via the kidney with 66% of the radioactive dose recovered in the urine. Approximately 29% of the radioactivity was recovered in the faeces, giving an overall mean recovery of 94% administered radioactivity. 4. The predominant circulating components were identified as delafloxacin and a direct glucuronide conjugate of delafloxacin.
引用
收藏
页码:1054 / 1062
页数:9
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