Mellstrand T, Svedmyr N, Fagerström P O
Eur J Respir Dis Suppl. 1980;109:54-60.
Healthy adults were treated in periods of 4 days with fast dissolving theophylline tablets (Oxyphyllin, Draco, Sweden) and sustained-release tablets (Theo-Dur, Draco, Sweden). To some of the volunteers, a single dose of i.v. aminophyllamine was administered. The absorption of theophylline, calculated from a single dose administration, of uncoated tablets (Oxyphyllin) was completed within 2 hours, whereas the absorption of sustained-release tablets (Theo-Dur) continued during 12 hours. There was no significant difference in bioavailability between aminophylline i.v., Oxyphyllin tablets and Theo-Dur tablets. The slow release tablets gave a stable plasma level in steady state that implies the possibility of using 12-hour dosage intervals and still achieve a stable theophylline concentration in steady state with a small difference between peak and trough concentrations. This investigation shows that it is possible to simulate the plasma concentration of theophylline in steady state by means of oral administration, using the simple one-compartment model calculated from data registered after a single i.v. dose.
健康成年人分别接受了为期4天的速溶茶碱片(Oxyphyllin,瑞典德拉科公司)和缓释片(Theo-Dur,瑞典德拉科公司)治疗。部分志愿者接受了单次静脉注射氨茶碱。从单次给药计算得出,未包衣片(Oxyphyllin)中茶碱的吸收在2小时内完成,而缓释片(Theo-Dur)的吸收则持续12小时。静脉注射氨茶碱、Oxyphyllin片和Theo-Dur片之间的生物利用度无显著差异。缓释片在稳态时可提供稳定的血浆水平,这意味着有可能采用12小时的给药间隔,并且在稳态时仍能达到稳定的茶碱浓度,峰浓度与谷浓度之间差异较小。本研究表明,通过口服给药,利用单次静脉注射剂量后记录的数据计算得出的简单一室模型,可以模拟稳态时茶碱的血浆浓度。