Jackson S H, Wright J M
Eur J Clin Pharmacol. 1983;24(2):205-8. doi: 10.1007/BF00613818.
Theophylline concentrations were measured in a clinical setting in 15 patients given a slow release theophylline preparation (Theo-Dur) every 12 h for reversible obstructive airways disease. Doses of 300-600 mg (464 +/- 134), 12 hourly, resulted in mean serum concentrations which increased from 11.2 +/- 2.9 micrograms/ml at 0 h to a peak of 15.5 +/- 4.6 micrograms/ml at 6 h and decreased again to 10.4 +/- 2.9 micrograms/ml at 12 h. The mean percentage fluctuation of serum concentrations (maximum minus minimum expressed as a % of the maximum) was 38.6 +/- 10.1%, range 20.3% to 54.9%. There was a significant positive correlation between % fluctuation and theophylline steady-state clearance determinations. Excluding a single heavy smoker, theophylline clearance also showed a significant inverse relationship with age. These data suggest that when this slow release preparation is given 12 hourly, satisfactorily sustained serum theophylline concentrations will be achieved in most adults.
对15例患有可逆性阻塞性气道疾病的患者在临床环境中进行了茶碱浓度测定,这些患者每12小时服用一次缓释茶碱制剂(Theo-Dur)。每12小时服用300 - 600毫克(464±134毫克)的剂量,导致血清平均浓度从0小时时的11.2±2.9微克/毫升增加到6小时时的峰值15.5±4.6微克/毫升,并在12小时时再次降至10.4±2.9微克/毫升。血清浓度的平均波动百分比(最大值减去最小值表示为最大值的百分比)为38.6±10.1%,范围为20.3%至54.9%。波动百分比与茶碱稳态清除率测定之间存在显著正相关。排除一名重度吸烟者后,茶碱清除率也与年龄呈显著负相关。这些数据表明,当每12小时给予这种缓释制剂时,大多数成年人将实现令人满意的持续血清茶碱浓度。