Vol.60 No.4 July 2012
Study on the penetration of sitafloxacin into the prostatic fluid
1)Department of Urology, Kobe Red Cross Hospital, 1-3-1 Wakinohamakaigandori, Chuo-ku, Kobe, Hyogo, Japan
2)Division of Urology, Department of Surgery Related, Kobe University Graduate School of Medicine
Abstract
To investigate the accumulation of sitafloxacin(STFX, Gracevit®) in the prostatic fluid, a single dose of STFX was orally administered to healthy adult males while fasting. We determined the STFX concentration in the serum and prostatic fluid at 1 and 2 hours after administration, and also calculated the ratio of the prostatic fluid STFX concentration to the serum STFX concentration at 1 and 2 hours. A dose of 50 mg was administered to 6 subjects and a dose of 100 mg was given to 6 subjects (total: 12 subjects).
The mean prostatic fluid STFX concentration (mean±SD) at 1 and 2 hours after administration was respectively 0.147±0.190 μg/mL and 0.147±0.126 μg/mL at a dose of 50 mg versus 0.163±0.188 μg/mL and 0.347±0.187 μg/mL at a dose of 100 mg. The mean prostatic fluid/serum STFX concentration ratio at 1 and 2 hours after administration was respectively 0.287±0.223 and 0.408±0.262 at a dose of 50 mg versus 0.394±0.212 and 0.506±0.181 at a dose of 100 mg.
Diarrhea occurred in one subject receiving a dose of 100 mg and a causal relationship between the diarrhea and STFX could not be ruled out. There were no abnormalities of vital signs or laboratory test results for which a causal relationship with STFX could not be ruled out.
The mean prostatic fluid/serum STFX concentration ratio ranged from 0.287 to 0.506. These results suggest that STFX is equivalent to other quinolone antibiotics.
Key word
sitafloxacin, quinolone, pharmacokinetics, prostatic fluid
Received
March 23, 2012
Accepted
May 1, 2012
Jpn. J. Chemother. 60 (4): 492-495, 2012
