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Antimicrobial Agents and Chemotherapy, May 1999, p. 1067-1071, Vol. 43, No. 5
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

Pharmacokinetics of Gatifloxacin and Interaction with an Antacid Containing Aluminum and Magnesium

Silke Lober,1 Susanne Ziege,1 Margot Rau,1 Gabriele Schreiber,1 Alain Mignot,2 Peter Koeppe,3 and Hartmut Lode1,*

Department of Pulmonary and Infectious Diseases, City Hospital Berlin-Zehlendorf/Heckeshorn, Affiliated with Freie Universität Berlin,1 and Department of Physics and Laser Medicine, Klinikum Benjamin Franklin, Freie Universität Berlin,3 Berlin, Germany, and Cephac Bioanalytical Research Centre, Saint-Benoit Cedex, France2

Received 8 July 1998/Returned for modification 16 December 1998/Accepted 20 February 1999

The pharmacokinetics of gatifloxacin (400 mg orally) and the influence of the antacid aluminum magnesium hydroxide (20 ml of Maalox 70) on the bioavailability of gatifloxacin in 24 healthy volunteers were assessed. In an open, randomized, six-period crossover study, the volunteers received either gatifloxacin alone (treatments A and D); aluminum magnesium hydroxide concomitant with gatifloxacin (treatment C); or aluminum magnesium hydroxide 2 h before (treatment B), 2 h after (treatment E), or 4 h after gatifloxacin administration (treatment F). Gatifloxacin concentrations were measured by a validated bioassay and high-performance liquid chromatography. Pharmacokinetics of a single 400-mg dose of gatifloxacin alone were characterized as follows (mean ± standard deviation): peak concentration (Cmax), 3.8 ± 0.5 (treatment A) and 3.4 ± 0.9 (treatment D) µg/ml; time to Cmax, 1.4 ± 0.8 (treatment A) and 1.7 ± 0.7 (treatment D) h; area under the curve from time zero to infinity (AUC0-infinity ), 33.5 ± 5.9 (treatment A) and 31.4 ± 3.4 (treatment D) µg · h/ml; urine recovery, (83 ± 6)% (treatment A) and (84 ± 8)% (treatment D). Comparison of the results obtained by bioassay showed a good correlation. Aluminum magnesium hydroxide administration 2 h before (treatment B) or concomitant with (treatment C) gatifloxacin decreased the Cmax by 45% (2.1 ± 1.2 µg/ml) or even 68% (1.2 ± 0.4 µg/ml) highly significantly (P < 0.01). AUC0-infinity was significantly reduced from 33.5 ± 5.9 to 19.4 ± 6.9 µg · h/ml (by 42%) or even to 11.9 ± 3.3 µg · h/ml (by 64%) (P < 0.01). If aluminum magnesium hydroxide was given 2 h after gatifloxacin (treatment E), there was no significant reduction of concentration in serum but AUC0-infinity was significantly reduced from 31.4 ± 3.4 to 25.9 ± 5.3 µg · h/ml (18%) (P < 0.01). Aluminum magnesium hydroxide given 4 h after gatifloxacin (treatment F) showed no influence on the gatifloxacin pharmacokinetics. Therefore, the optimal time between gatifloxacin application and the intake of an aluminum-containing antacid should be 4 h.

* Corresponding author. Mailing address: Department of Pulmonary and Infectious Diseases, City Hospital Berlin-Heckeshorn, affil. Freie Universität Berlin, Zum Heckeshorn 33, 14109 Berlin, Germany. Phone: 49-30-8002-2222. Fax: 49-30-8002-2623. E-mail: haloheck{at}ze-dat.fu-berlin.de.

Antimicrobial Agents and Chemotherapy, May 1999, p. 1067-1071, Vol. 43, No. 5
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.


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