Osman M A, Patel R B, Irwin D S, Welling P G
Biopharm Drug Dispos. 1983 Jan-Mar;4(1):63-72. doi: 10.1002/bdd.2510040109.
The influence of prior food ingestion, and also of varying fluid volumes, on plasma theophylline levels was examined following single oral doses of two sustained-release formulations, Theobid (260 mg) and Theo-Dur (200 mg) and one partially enteric-coated formulation, Choledyl (128 mg), to 9 healthy volunteers. Prior food ingestion tended to delay the absorption of theophylline from all formulations to a small extent. This effect was observed only at early sampling times, and plasma drug profiles were similar for all treatments within a particular formulation. Theobid and Theo-Dur gave rise to plasma profiles that were characteristic of sustained-release formulations, with mean Cmax values of 5.5-5.7 micrograms ml-1 (Theobid) and 2.8-3.2 micrograms ml-1 (Theo-Dur) occurring at 5.8-9.1 h after dosing. Choledyl gave rise to a longer absorption lag time than the other formulations but was subsequently absorbed at a faster rate yielding mean Cmax values of 3.2-3.5 micrograms ml-1 at 2.8-4.1 h. The intersubject variability in theophylline plasma levels, and also in most pharmacokinetic parameter values, was generally less following Theo-Dur compared to the other formulations.
对9名健康志愿者单次口服两种缓释制剂（茶喘平（260毫克）和优喘平（200毫克））以及一种部分肠溶衣制剂（胆茶碱（128毫克））后，研究了先前摄入食物以及不同液体量对血浆茶碱水平的影响。先前摄入食物往往会在一定程度上略微延迟所有制剂中茶碱的吸收。这种影响仅在早期采样时间观察到，并且在特定制剂内所有治疗的血浆药物曲线相似。茶喘平和优喘平产生了具有缓释制剂特征的血浆曲线，给药后5.8 - 9.1小时的平均Cmax值为5.5 - 5.7微克/毫升（茶喘平）和2.8 - 3.2微克/毫升（优喘平）。胆茶碱的吸收滞后时间比其他制剂更长，但随后以更快的速度被吸收，在2.8 - 4.1小时产生的平均Cmax值为3.2 - 3.5微克/毫升。与其他制剂相比，优喘平给药后茶碱血浆水平以及大多数药代动力学参数值的受试者间变异性通常较小。
