Abstract
We investigated the effect of an antacid (dried aluminum hydroxide gel, AL) and cimetidine, histamine H2-antagonist on the gastrointestinal absorption of pazufloxacin (PZFX) in 6 healthy male volunteers. 200 mg of PZFX was given orally to fasting subjects with and without 1 g of AL or 200 mg of cimetidine.
The pharmacokinetic parameters for PZFX obtained after each of treatments were as follows: the Cmax, Tmax, T1/2, AUC0→∞ and urinary excretion rate for PZFX alone were 4.28μg/ml, 0.88 h, 2.15 h, 8.85 μg ·h/ml and 87.2%, respectively; those for coadministration with AL were 1.77 μg/ml, 1.17 h, 1.98 h, 6.24 μg ·h/ml and 69.7%; and those for coadministration with cimetidine were 2.75 μg/ml, 0.76 h, 2.00h, 8.93 μg ·h/ml and 84.8%.
Gastrointestinal absorption of PZFX was inhibited (58.6% of the Cmax, 29.5% of the AUC0→∞) by interaction with antacid, but the inhibition was slight compared with that of other quinolone antimicrobial agents. Coadministration of cimetidine resulted in decrease (35.7%) in the Cmax, but the AUC00→∞ was not inhibited.
