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

来源：

XENOBIOTICA | 2015年 / 45卷 / 12期

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

页码：1054 / 1062

页数：9

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