Journal of Antimicrobial Chemotherapy (1999) 43, Suppl. A, 49-54
© 1999 The British Society for Antimicrobial Chemotherapy
Oral bioequivalence of three ciprofloxacin formulations following single-dose administration: 500 mg tablet compared with 500 mg/10 mL or 500 mg/5 mL suspension and the effect of food on the absorption of ciprofloxacin oral suspension
a Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516-4175, USA; b Bayer Inc., Etobicoke, Ontario, Canada
The oral bioequivalence and tolerability of two ciprofloxacin formulations (tablet and
suspension)
and
the effect of food on the absorption of ciprofloxacin oral suspension were investigated.
Sixty-eight
young, healthy male subjects participated in two separate, randomized, crossover studies. In
study
1,
ciprofloxacin as a single 500 mg tablet or as 500 mg/10 mL oral suspension was administered in
a
fasted state on day 1. In study 2, subjects participated in a three-way crossover study in which
ciprofloxacin suspension was administered as 500 mg/ 10 mL in a fasted state, or 500 mg/10 mL
with
food, or 500 mg/5 mL in a fasted state. Plasma ciprofloxacin concentrations were measured by
high-performance liquid chromatography. Standard pharmacokinetic parameters were estimated
using
non-compartmental methods. In study 1, geometric mean C
max values of ciprofloxacin following the single 500 mg tablet and 500 mg/10 mL
suspension doses were 2.36 and 2.18 mg/L, respectively; corresponding geometric mean t
max values were 1.1 and 1.6 h, respectively. Geometric mean AUC
0–
values were 12.0 and 11.8 mg•h/L, respectively. In study 2,
geometric
least
squares mean C
max values following ciprofloxacin 500 mg/10 mL and 500 mg/5 mL suspension
during
fasted conditions were 1.54 and 1.59 mg/L, respectively. Corresponding geometric least squares
mean
AUC
0– values were 7.3 and 8.0 mg•h/L. Administration of
ciprofloxacin 500
mg/10
mL suspension, in either a fasted or fed state, was not associated with significant changes in C
max (1.54 mg/L for fasted vs 1.37 mg/L for fed) or AUC
0– values (7.28 mg·h/L for fasted vs 8.19 mg·h/L for
fed).
Each
ciprofloxacin formulation was well tolerated for the duration of each study. These studies
demonstrated
bioequivalence between ciprofloxacin 500 mg tablet and two strengths of ciprofloxacin
suspension (500
mg/10 mL and 500 mg/5 mL). Bioavailability was unaltered by food.