Steffensen G, Pedersen S
Br J Clin Pharmacol. 1986 Nov;22(5):571-7. doi: 10.1111/j.1365-2125.1986.tb02937.x.
Bioavailability and the absorption pattern of theophylline from the sustained release theophylline (SRT) product, Uniphyllin, were studied in eight adults and eight children under fasting conditions in the morning, after a standardised breakfast in the morning, and under fasting conditions in the evening (adults only). Theophylline given intravenously was used as a reference. The extent of absorption of theophylline was complete for all administrations of SRT both in adults and children. In adults the absorption profiles after the three administrations of SRT were very similar and at no time point was there any difference in serum theophylline concentration or fraction absorbed between the three regimens. In addition, inter and intra individual variations in absorption were small. In children food caused a substantial change in the absorption pattern of theophylline so that the profiles became rather unpredictable with delays in absorption and periods of rapidly increasing serum drug concentrations. In three of the patients the dose dumping phenomenon resulted in toxic serum drug concentrations. Dumping of the dose could take place at any time interval between 3 and 15 h post dosing. Cmax was about 50% higher after fed than after fasting medication (P less than 0.01). It is concluded that children should not take SRT in large doses in combination with food.
在8名成人和8名儿童中，于早晨空腹状态下、早晨标准化早餐后以及晚上空腹状态下（仅针对成人），研究了缓释型茶碱产品优喘平（Uniphyllin）中茶碱的生物利用度和吸收模式。静脉注射的茶碱用作对照。成人和儿童服用优喘平后，茶碱的吸收程度均为完全吸收。在成人中，三次服用优喘平后的吸收曲线非常相似，在任何时间点，三种给药方案之间的血清茶碱浓度或吸收分数均无差异。此外，个体间和个体内的吸收差异较小。在儿童中，食物会使茶碱的吸收模式发生显著变化，导致吸收曲线变得难以预测，出现吸收延迟和血清药物浓度快速上升的时期。在三名患者中，出现了剂量倾泻现象，导致血清药物浓度达到中毒水平。剂量倾泻可在给药后3至15小时的任何时间间隔发生。进食后服用药物的Cmax比空腹服药后高约50%（P<0.01）。得出的结论是，儿童不应大剂量服用优喘平并同时进食。
