Horiuchi Y, Takemura T, Ueno K
Division of Pediatrics, National Sengokusoh Hospital.
Arerugi. 1991 Sep;40(9):1186-93.
Three different theophylline preparations, theophylline syrup, granule and tablets, were examined to determine their pharmacokinetics and changes in urinary metabolites for each steady state phase. The theophylline syrup was as rapidly and as essentially bioavailable as the theophylline granule preparation. In addition, peak to trough differences in serum theophylline concentrations were largest for theophylline syrup and lowest for tablets. Tmax was greater in theophylline tablets and a significant difference was apparent in the tablet-syrup and tablet-granule populations. AUC and T1/2 were similar in these populations. Cmax and Cmin achieved satisfactory therapeutic theophylline levels in three different preparations, and t-test showed no significant difference between them. CL and Vd were also similar. The urinary metabolites of theophylline were expressed as internal standard equivalents on a molar basis. There were no significant changes between either tested preparations different or different age groups. Therefore, we concluded that theophylline syrup and granules should be administered on a 3-times-daily basis, considering trough plasma theophylline levels. Theophylline tablets are preferable, if they can be taken.
对三种不同的茶碱制剂（茶碱糖浆、颗粒剂和片剂）进行了研究，以确定它们在每个稳态阶段的药代动力学及尿代谢产物的变化。茶碱糖浆与茶碱颗粒制剂的生物利用度一样迅速且基本相同。此外，茶碱糖浆的血清茶碱浓度峰谷差异最大，片剂的最小。茶碱片剂的达峰时间（Tmax）更长，在片剂 - 糖浆组和片剂 - 颗粒剂组中存在显著差异。这些组中的曲线下面积（AUC）和半衰期（T1/2）相似。三种不同制剂的峰浓度（Cmax）和谷浓度（Cmin）均达到了令人满意的治疗性茶碱水平，t检验显示它们之间无显著差异。清除率（CL）和分布容积（Vd）也相似。茶碱的尿代谢产物以摩尔为基础表示为内标当量。不同测试制剂之间以及不同年龄组之间均无显著变化。因此，考虑到茶碱的血浆谷浓度，我们得出结论，茶碱糖浆和颗粒剂应每日给药3次。如果可以服用，茶碱片剂更可取。
