Effect of a fat- and calcium-rich breakfast on pharmacokinetics of fleroxacin administered in single and multiple doses.
The effect of a fat- and liquid-calcium-rich meal on the pharmacokinetics of single and multiple doses of fleroxacin in 20 healthy men and women was investigated in a randomized crossover fashion. Fleroxacin was administered as 400 mg daily for 3 days and as a single 400 mg dose. Concurrent administration of fleroxacin with food resulted in a statistically significant (P < or = 0.05) decrease in the area under the curve (13.9% for multiple-dose administration, 10% for single-dose administration) and in the peak concentration (25.9% for multiple-dose administration, 27% for single-dose administration) and a lengthening of the time to peak (more than doubled for single- and multiple-dose phases). In addition, by using an equivalence criteria of 80 to 125%, the two one-sided tests procedure indicated that the mean areas under the curves for fleroxacin administered in a fed and a fasted state were statistically bioequivalent (P < or = 0.05) for both the single- and multiple-dose regimens. Although a meal high in fat and containing liquid calcium reduces the peak concentration by approximately 25%, a minimal effect on bioavailability is seen with concomitant food administration. In addition, multiple-dose bioavailability studies appear to give similar information to single-dose studies while representing the clinical setting more closely.
Bertino
J S
JS
Department of Pharmacy Services, Mary Imogene Bassett Hospital, Cooperstown, New York 13326.
Nafziger
A N
AN
Wong
M
M
Stragand
L
L
Puleo
C
C
D000328:Adult; D000818:Animals; D001682:Biological Availability; D002136:Calcium, Dietary / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D004041:Dietary Fats / Q000494:pharmacology*; D005260:Female; D016576:Fleroxacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008892:Milk; D013810:Therapeutic Equivalency
D002136:Calcium, Dietary; D004041:Dietary Fats; D016576:Fleroxacin