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Effect of antacids on the bioavailability of diflunisal in the fasting and postprandial states
Author(s) -
Tobert J A,
DeSchepper P,
Tjandramaga T B,
Mullie A,
Buntinx A P,
Meisinger M A P,
Huber P B,
Hall T L P,
Yeh K C
Publication year - 1981
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1981.177
Subject(s) - antacid , diflunisal , chemistry , bioavailability , postprandial , hydroxide , excretion , magnesium , chromatography , medicine , endocrinology , pharmacology , inorganic chemistry , biochemistry , organic chemistry , insulin
Diflunisal is a long‐acting salicylate derivative. We examined the effect of single concomitant doses of three antacids on diflunisal bioavailability under fasting or fed conditions (30 min after finishing a standard meal). With the use of an open, randomized, and balanced design, one 250‐mg diflunisal tablet was given to each of 12 healthy men under six conditions: fasted, no antacid; fed, no antacid; fasted, 15 ml of aluminum hydroxide gel; fed, 15 ml of aluminum hydroxide gel; fasted, 10 ml magnesium hydroxide suspension; and fed, 15 ml of an aluminum hydroxide/magnesium hydroxide mixture. Diflunisal plasma 0‐ to 48‐hr area under the time curve (AUC), peak plasma concentrations, and 0‐ to 96‐hr urinary excretion were determined. Food (alone) decreased peak plasma concentrations by 16% (P < 0.05) but did not affect AUC or urinary excretion. Under fasting conditions, aluminum hydroxide reduced AUC by 26% (P < 0.01), peak plasma concentrations by 46% (P < 0.01), and urinary excretion by 14% (P < 0.05). Magnesium hydroxide suspension (in the fasting state) increased the early plasma concentrations (by 130% at 0.5 hr and 64% at 1 hr, P < 0.05) and increased AUC by 10% (P < 0.05) but had no effect on urinary excretion. In the fed state neither aluminum hydroxide nor the aluminum hydroxide/magnesium hydroxide mixture had any detectable effect. Clinical Pharmacology and Therapeutics (1981) 30 , 385–389; doi: 10.1038/clpt.1981.177