Food-Induced Theophylline Release/Absorption Changes from Controlled-Release Formulations: A Proposed In Vitro Model

AbstractThe rate and extent of absorption of theophylline from controlled-release products may change dramatically when these products are administered after a high fat meal and the direction of the change may vary with the formulation (1-3). In an effort to understand the reason for these changes the release rates of four theophylline controlled- release products were tested in a variety of fluids chosen to simulate the gastrointestinal environment. In vitro systems which combined fatty acid, high pH and bile salts resulted in release rate changes which showed the same direction of change as those observed after the high fat meal. These studies provide some insight into the possible interactions of gastrointestinal fluids with the rate controlling polymers of the controlled-release dosage forms.

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