Abstract
Interaction studies in dogs have indicated that antacids significantly decrease the oral bioavailability of cefixime. Twelve healthy adult male volunteers participated in a randomized, four-way crossover trial to evaluate the influence of an aluminum-magnesium antacid (Maalox; 20 ml) on the pharmacokinetics of cefixime (400 mg). Regimens were (i) cefixime alone; (ii) cefixime simultaneous with antacid; (iii) cefixime 2 h before antacid; and (iv) cefixime 2 h after antacid. Serial blood and urine samples were collected over a 24-h period following each dose of cefixime. There was a 1-week washout interval between regimens. Cefixime concentrations in serum and urine were analyzed by high-performance liquid chromatography. Maximum cefixime concentrations in serum for regimens i through iv were (mean +/- standard deviation) 4.9 +/- 1.4, 5.7 +/- 1.3, 5.1 +/- 1.0, and 5.5 +/- 1.5 micrograms/ml, respectively. Corresponding values for area under the serum concentration-time curve extrapolated to infinity were 38.3 +/- 14.5, 42.8 +/- 13.9, 38.5 +/- 9.8, and 41.6 +/- 16.7 micrograms.h/ml. There was a trend toward increased concentrations in serum and area under the curve of cefixime when it was administered concomitantly with antacid; however, these differences were not statistically significant (P greater than 0.05; analysis of variance). We conclude that single-dose administration of an aluminum-magnesium antacid does not significantly decrease the oral bioavailability of cefixime.
MeSH Terms
Adult
Aluminum Hydroxide/pharmacology
Antacids/pharmacology
Biological Availability
Cefixime
Cefotaxime/analogs & derivatives,pharmacokinetics
Drug Combinations/pharmacology
Drug Interactions
Half-Life
Humans
Magnesium/pharmacology
Magnesium Hydroxide/pharmacology
Male
Chemicals
Antacids
Drug Combinations
aluminum hydroxide, magnesium hydroxide, drug combination
Aluminum Hydroxide
Cefixime
Magnesium
Cefotaxime
Magnesium Hydroxide
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Healy D P
Department of Pharmacy and Pharmaceutics, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0581.
Sahai J V
Sterling L P
Racht E M
References (13)
13 references, click to expand
-
Decrease of tetracycline absorption in man by sodium bicarbonate.
Clin Pharmacol Ther. 1971 Sep-Oct;12(5):779-84
PMID: 4936141
-
Interactions with the absorption of tetracyclines.
Drugs. 1976;11(1):45-54
PMID: 946598
-
Application of Akaike's information criterion (AIC) in the evaluation of linear pharmacokinetic equations.
J Pharmacokinet Biopharm. 1978 Apr;6(2):165-75
PMID: 671222
-
Comparative in vitro activity and beta-lactamase stability of FR 17027, a new orally active cephalosporin.
Antimicrob Agents Chemother. 1984 Aug;26(2):174-80
PMID: 6333207
-
Influence of food and reduced gastric acidity on the bioavailability of bacampicillin and cefuroxime axetil.
Br J Clin Pharmacol. 1984 Oct;18(4):535-9
PMID: 6091711
-
Interactions affecting drug absorption.
Clin Pharmacokinet. 1984 Sep-Oct;9(5):404-34
PMID: 6388952
-
Absolute bioavailability of cefixime in man.
J Clin Pharmacol. 1988 Aug;28(8):700-6
PMID: 3216036
-
Degradation kinetics and mechanisms of a new cephalosporin, cefixime, in aqueous solution.
J Pharm Sci. 1987 Mar;76(3):208-14
PMID: 3585736
-
Pharmacokinetic profile of cefixime in man.
Pediatr Infect Dis J. 1987 Oct;6(10):963-70
PMID: 3696837
-
Determination of cefixime in biological samples by reversed-phase high-performance liquid chromatography.
J Chromatogr. 1987 Nov 27;422:145-52
PMID: 3437003
-
Drug interactions with quinolones.
Rev Infect Dis. 1988 Jan-Feb;10 Suppl 1:S132-6
PMID: 3279488
-
The pharmacokinetics of cefixime in the fasted and fed state.
Eur J Clin Pharmacol. 1988;34(5):525-8
PMID: 3203716
-
H+ gradient-dependent and carrier-mediated transport of cefixime, a new cephalosporin antibiotic, across brush-border membrane vesicles from rat small intestine.
J Pharmacol Exp Ther. 1987 May;241(2):594-601
PMID: 3572815