title: Effect of sucralfate on pharmacokinetics of fleroxacin in healthy volunteers.
abstract: The effect of sucralfate on the pharmacokinetics of fleroxacin was assessed in 20 healthy male volunteers. The study was of a two-way crossover design in which subjects were randomized to one of the following two regimens at the time of entry: (i) a single 400-mg dose of fleroxacin alone or (ii) a 400-mg dose of fleroxacin given once and 1 g of sucralfate given every 6 h starting 24 h before fleroxacin treatment and continuing for 48 h after fleroxacin treatment. Blood samples were collected immediately before fleroxacin administration and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 36, and 48 h postdosing. Fleroxacin concentrations in plasma and urine were determined by high-performance liquid chromatography. While concurrent of fleroxacin and sucralfate resulted in a decrease in the area under the plasma concentration-time curve, a decrease in the maximum concentration, and an increase in the time to the maximum concentration (P < 0.05), these changes were modest compared with the interaction of other quinolones with sucralfate. The relative bioavailability of fleroxacin given with sucralfate, calculated from the area under the concentration-time curve, was 76% compared with that of fleroxacin alone. This is significantly better than the bioavailabilities of other quinolones (1.8 to 12.3%) when they are administered with sucralfate.
authors: Department of Pharmacy, Hartford Hospital, Connecticut 06115.
authors: T J
authors: TJ
authors: Lubowski
authors: C H
authors: CH
authors: Nightingale
authors: K
authors: K
authors: Sweeney
authors: R
authors: R
authors: Quintiliani
mesh_terms: D000328:Adult; D001682:Biological Availability; D004347:Drug Interactions; D016576:Fleroxacin / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D011897:Random Allocation; D013392:Sucralfate / Q000494:pharmacology*
chemical_list: D013392:Sucralfate; D016576:Fleroxacin