Food-induced changes in theophylline absorption from controlled-release formulations. Part I. Substantial increased and decreased absorption with Uniphyl tablets and Theo-Dur Sprinkle

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Abstract
Food‐induced changes in absorption from two controlled‐release formulations of theophylline (Uniphyl tablets [Purdue Frederick Co.] and Theo‐Dur Sprinkle [Key Pharmaceuticals, Inc.]) were studied in healthy male nonsmokers. Although the two forms exhibited a theophylline in vitro dissolution rate that was independent of changes in pH from 1 to 8, they showed substantial but opposite food‐induced absorption changes. In a 12‐subject, three‐way, single‐dose, randomized, crossover study the bioavailability of theophylline relative to immediate‐release aminophylline tablets increased from 53% ± 23% (X̄ ± SD) to 96% ± 46% when Uniphyl (two 400 mg tablets) was taken under fasting and nonfasting (high fat content meal) conditions, respectively. On the other hand, in a separate six‐subject, two‐way, randomized, crossover study, food reduced the bioavailability of theophylline from Theo‐Dur Sprinkle: Theophylline bioavailability in the nonfasting state was only 53% ± 9% that in the fasting state. Clinical Pharmacology and Therapeutics (1985) 38, 77–83; doi:10.1038/clpt.1985.138