Jonkman J H
Pharma Bio-Research Int. b.v., Assen, The Netherlands.
Chronobiol Int. 1987;4(3):449-58. doi: 10.3109/07420528709083533.
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.
目前，茶碱主要以缓释剂型使用。自七十年代中期以来，许多此类产品已被推出，并在12小时给药间隔（“一日两次”制剂）中得到了广泛应用。自1983年以来，茶碱也有可间隔24小时给药的制剂（“一日一次”制剂）。食物的同时摄入会影响（增加或减少）茶碱从缓释剂型中的释放。显然，超缓释产品最容易受到食物影响。对于某些制剂，膳食的组成，尤其是其脂肪含量，决定了食物影响的程度。由于一日一次的茶碱制剂单次摄入剂量较大，因此必须了解进餐时间和内容对其的影响。如果食物会以意想不到的方式改变超缓释制剂中茶碱的释放，那么如果释放受到抑制，药物疗效可能会受损，如果药物突然释放，则可能会导致毒性。在此，本文综述了有关食物与一日一次茶碱制剂相互作用的信息，因为该主题对临床医生以及关注此类药物时辰药理学研究的人员都很重要。
