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Clinical Trial
. 2004 Mar;48(3):804-8.
doi: 10.1128/AAC.48.3.804-808.2004.

Pharmacokinetics of posaconazole coadministered with antacid in fasting or nonfasting healthy men

Rachel Courtney  1 , Elaine Radwanski, Josephine Lim, Mark Laughlin
Affiliations
Clinical Trial

Pharmacokinetics of posaconazole coadministered with antacid in fasting or nonfasting healthy men

Rachel Courtney et al. Antimicrob Agents Chemother. 2004 Mar.

Abstract

Posaconazole is a potent broad-spectrum azole antifungal agent in clinical development for the treatment of invasive fungal infections. This study evaluated the potential for a pH-dependent pharmacokinetic interaction between posaconazole and an antacid (Mylanta), under fasting and nonfasting conditions. Twelve men completed this randomized, four-period crossover, single-dose study. Subjects received 200 mg of posaconazole following a 10-h fast, with 20 ml of Mylanta and a 10-h fast, with 20 ml of Mylanta and a high-fat breakfast, and with a high-fat breakfast alone. Antacid coadministration had no statistically significant effects on posaconazole bioavailability under fasting or nonfasting conditions. In the fasting state, antacid slightly increased the relative oral bioavailability of posaconazole by 15% (P = 0.296); in the nonfasting state, antacid decreased the relative bioavailability of posaconazole by 12% (P = 0.352). Food increased the relative oral bioavailability of posaconazole by 400% (P = 0.001). In conclusion, the effect of antacid on posaconazole exposure in the fasting or nonfasting state was small and is not considered clinically significant.

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Figures

FIG. 1.
FIG. 1.
Mean concentration in plasma-time profile of posaconazole alone and in combination with antacid under nonfasting and fasting conditions.
FIG. 2.
FIG. 2.
Individual posaconazole AUCtf values following administration of posaconazole alone and in combination with antacid under nonfasting (fed) and fasting conditions.
See this image and copyright information in PMC

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