Intestinal elimination of sparfloxacin, fleroxacin, and ciprofloxacin in rats.
The intestinal transepithelial elimination of sparfloxacin and fleroxacin was compared with that of ciprofloxacin in a rat model following a single parenteral administration of 25 mg of each of the antibiotics per kg of body weight. All three fluoroquinolones were eliminated through the small intestine. Ciprofloxacin was eliminated in the proximal jejunum at a rate of 1.97 +/- 0.70 micrograms/cm2, while the elimination rates of fleroxacin and sparfloxacin were 0.64 +/- 026 and 0.21 +/- 0.10 micrograms/cm2, respectively, over a 90-min collection period. In the ileum, the elimination rates of ciprofloxacin, fleroxacin, and sparfloxacin over the same period were 1.44 +/- 0.77, 1.00 +/- 0.33, and 0.41 +/- 0.26 micrograms/mc2, respectively. These data suggest that these fluoroquinolones undergo a transepithelial elimination process in the small intestine. This route of elimination may be important in the therapy of bacterial diarrhea.
Rubinstein
E
E
Department of Internal Medicine, Bichat-Claude Bernard Hospital, Faculty of Medicine, University of Paris VII, France.
Dautrey
S
S
Farinoti
R
R
St Julien
L
L
Ramon
J
J
Carbon
C
C
D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D002939:Ciprofloxacin / Q000493:pharmacokinetics*; D016576:Fleroxacin / Q000493:pharmacokinetics*; D024841:Fluoroquinolones; D007082:Ileum / Q000378:metabolism*; D007583:Jejunum / Q000378:metabolism*; D008297:Male; D015363:Quinolones / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; D002939:Ciprofloxacin; D016576:Fleroxacin; C061363:sparfloxacin