Pharmacokinetics of antofloxacin hydrochloride, a new fluoroquinolone antibiotic, after single oral dose administration in Chinese healthy male volunteers

2008 ◽  
Vol 29 (3) ◽  
pp. 167-172 ◽  
Author(s):  
Yonghong Xiao ◽  
Yuan Lu ◽  
Zisheng Kang ◽  
Ming Zhang ◽  
Yan Liu ◽  
...  
2001 ◽  
Vol 40 (Supplement 1) ◽  
pp. 19-25 ◽  
Author(s):  
John Lettieri ◽  
Ramon Vargas ◽  
Vipin Agarwal ◽  
Patrick Liu

1996 ◽  
Vol 40 (1) ◽  
pp. 92-96 ◽  
Author(s):  
C Lin ◽  
H Kim ◽  
E Radwanski ◽  
M Affrime ◽  
M Brannan ◽  
...  

The pharmacokinetics of genaconazole, a racemic triazole antifungal agent comprising 50% RR and 50% SS enantiomers, were studied in 12 healthy male volunteers after a single oral dose of 200 mg. The serum samples were analyzed for the two enantiomers by using a chiral high-pressure liquid chromatography assay. The concentrations of the RR and SS enantiomers in serum were virtually identical. The mean values for the maximum concentrations in serum (Cmax) (1.7 micrograms/ml), times to Cmax (4.0 to 4.2 h), half-lives (83 h), and areas under the concentration-time curve from 0 h to infinity (195 to 199 micrograms.h/ml) were similar for the two enantiomers. The results showed that the pharmacokinetic profiles of the two enantiomers were similar after a single oral dosing of the racemate. The pharmacokinetics of the RR enantiomer were also evaluated in 12 healthy male volunteers after a single oral dose of 100 or 200 mg. The ratios of the Cmaxs and of the areas under the concentration-time curves from 0 h to infinity for the two doses were about 2, indicating a dose proportionality. In a separate study, six healthy male volunteers received a single oral dose of 50 mg of 14C-labeled genaconazole. The Cmax values for total radioactivity (14C) and intact genaconazole were virtually identical (0.6 micrograms/ml). The mean half-lives in serum were about 73 h for both total radioactivity and genaconazole. The amounts of total radioactivity excreted in the 0 to 240-h interval (representing approximately three half-lives) in urine and feces were 66.6 and 9.3% of the dose, respectively; 64.4% of the dose was excreted in urine as parent drug. There were no detectable metabolites in either serum or urine. The data demonstrate that genaconazole (racemate) is well absorbed, undergoes negligible biotransformation, and is slowly excreted, primarily in the urine.


Xenobiotica ◽  
1997 ◽  
Vol 27 (1) ◽  
pp. 59-71 ◽  
Author(s):  
F. Waldmeier ◽  
G. Flesch ◽  
P. Mu Ller ◽  
T. Winkler ◽  
H.- P. Kriemler ◽  
...  

2021 ◽  
Vol 9 (3) ◽  
Author(s):  
Folke Sjöberg ◽  
Susanna Waters ◽  
Boel Löfberg ◽  
Clas Sonesson ◽  
Nicholas Waters ◽  
...  

2008 ◽  
Vol 199 (1-2) ◽  
pp. 115-125 ◽  
Author(s):  
Jan Hilpert ◽  
Johanna M. Beekman ◽  
Susanne Schwenke ◽  
Kristin Kowal ◽  
David Bauer ◽  
...  

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