title: Pharmacokinetics of sparfloxacin in humans after single oral administration at doses of 200, 400, 600, and 800 mg.
abstract: The pharmacokinetics of sparfloxacin at oral doses of 200, 400, 600, and 800 mg were studied in 12 healthy volunteers in a randomized double-blind crossover study. Each dose administration was separated by a 1-week washout period. Plasma and urine samples were collected up to 120 hours postdosing, for determination of free and total (free plus glucurono-conjugated) sparfloxacin levels by high-performance liquid chromatography assay and ultraviolet detection. Mean Cmax values ranged from 705 +/- 158 to 1966 +/- 620 ng/mL for the 200 to 800 mg doses, at median tmax ranging from 4 to 5 hours. A slight decrease of sparfloxacin bioavailability with increasing dose was observed because AUC was 87% to 88% of the expected area when the dose was doubled. The elimination half-life values were constant over the dose range (with values ranging from 18 to 21 hours) as well as the renal clearance. The metabolic ratio conjugated/free drug was not modified by increasing dose.
authors.affiliation: Institut de Biopharmacie, Rhone Poulenc Rorer, Antony, France.
authors.forename: G
authors.initials: G
authors.lastname: Montay
authors.forename: R
authors.initials: R
authors.lastname: Bruno
authors.forename: J C
authors.initials: JC
authors.lastname: Vergniol
authors.forename: M
authors.initials: M
authors.lastname: Ebmeier
authors.forename: Y
authors.initials: Y
authors.lastname: Le Roux
authors.forename: C
authors.initials: C
authors.lastname: Guimart
authors.forename: A
authors.initials: A
authors.lastname: Frydman
authors.forename: D
authors.initials: D
authors.lastname: Chassard
authors.forename: J J
authors.initials: JJ
authors.lastname: Thebault
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D024841:Fluoroquinolones; D006801:Humans; D008297:Male; D015363:Quinolones / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; C061363:sparfloxacin