Food interactions with once-a-day theophylline preparations: a review

At present, theophylline is used predominantly as sustained-release dosage forms. Since the mid-seventies many such products have been introduced and have found huge application for use with a dosage interval of 12 hr ('twice-a-day' preparations). Since 1983 theophylline has also been available as preparations that can be given with an interval of 24 hr ('once-a-day' preparations). The release of theophylline from sustained-release dosage forms can be influenced (either increased or decreased) by concomitant intake of food. Obviously, ultra-slow-releasing products are most vulnerable to food effects. With some preparations the composition of the meal, especially its fat content, determines the degree of the food effect. The effect of meal timing and content on once-a-day theophylline preparations must be known since rather large doses are ingested all at a single time. If food can alter the release of theophylline in an unexpected manner from ultra-slow preparations, drug effectiveness may be impaired if release is inhibited or toxicity might result if sudden release of drug occurs. Herein, information about food interaction with once-a-day theophylline preparations is reviewed as this topic is important both for clinicians as well as those concerned with chronopharmacologic investigations of such medications.