The effect of ferrous sulphate and sucralfate on the bioavailability of oral gemifloxacin in healthy volunteers

• Published in: International journal of antimicrobial agents 2000-08, Vol.15 (4), p.283-289
• Main Authors: Allen, A, Bygate, E, Faessel, H, Isaac, L, Lewis, A
• Format: Article
• Language: English
• Subjects: Adolescent; Adult; Anti-Infective Agents - adverse effects; Anti-Infective Agents - pharmacokinetics; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Area Under Curve; Biological and medical sciences; Biological Availability; Cross-Over Studies; Drug interactions; Ferrous Compounds - pharmacology; ferrous sulfate; Ferrous sulphate; Fluoroquinolone; Fluoroquinolones; Gemifloxacin; Humans; Male; Medical sciences; Middle Aged; Naphthyridines - adverse effects; Naphthyridines - pharmacokinetics; Pharmacokinetics; Pharmacology. Drug treatments; Reference Values; Sucralfate; Sucralfate - pharmacology
• ISSN: 0924-8579; 1872-7913
• DOI: 10.1016/S0924-8579(00)00187-4

Sucralfate is a cytoprotectant with antacid properties and ferrous sulphate is commonly prescribed for iron-deficiency anaemia. This open, randomized, single-dose, five-way crossover study investigated the effect of sucralfate and ferrous sulphate on the bioavailability of gemifloxacin, a novel fluoroquinolone antimicrobial. Twenty-seven healthy male volunteers received gemifloxacin, 320 mg p.o., alone, 3 h after sucralfate (2 g) or ferrous sulphate (325 mg), or 2 h before sucralfate or ferrous sulphate. Each subject received all five dosing regimens in random order with at least 6 days between regimens. Plasma samples collected up to 48 h after dosing with gemifloxacin, were assayed for gemifloxacin to determine pharmacokinetic parameters. Administration of gemifloxacin 3 h after sucralfate produced a marked decrease of 53% in the area under the plasma concentration–time curve from time zero extrapolated to infinity (AUC 0–∞), and a decrease of 69% in the maximal plasma concentration ( C max). Administration of gemifloxacin 3 h after ferrous sulphate resulted in only a modest reduction of 11% in AUC 0–∞ and of 20% in C max, which was not considered to be clinically significant. In contrast, at the doses used neither sucralfate nor ferrous sulphate altered gemifloxacin bioavailability when it was administered 2 h before either of these agents. Gemifloxacin was well tolerated in all the regimens. The results of this study support the dosing recommendation that gemifloxacin can be safely administered at least 2 h before sucralfate or ferrous sulphate, or at least 3 h after ferrous sulphate.