Berdel D, von Berg A, Reinhardt D, Heimann G, Steinijans V W, Sauter R
Marien-Hospital, Abteilung Kinderheilkunde, Wesel.
Pneumologie. 1991 Nov;45 Suppl 4:863-6.
To assess the pharmacokinetic parameters of theophylline (Euphylong as retard pellets) children were studied belonging to age groups between 9 to 13 and 5 to 9 years in twice-daily dosage with unequal distribution of the daily doses. For the older children the dose was 400 + 200 mg and for the younger ones 300 + 150 mg theophylline (these quantities represent the evening and morning doses). 16 and 14 children, respectively, completed the studies regularly. Pharmacokinetic evaluation resulted in a markedly parallel course of the individual serum theophylline profiles around the mean value. The average nocturnal concentration from 200 to 600 hours in the morning was higher than the average daytime concentration (11.4 to 10.5 mg/l or 12.3 to 11.4 mg/l). Due to the relatively stable baseline values the clinical parameters improved only slightly, but there were in particular significant changes in the peak-flow profile. In the older children we could also prove that they had a better protection against metacholine provocation. The side effects were generally mild and were in accordance with previous experiences collected with the studied preparation. The dosage scheme with unequal distribution of the total daily dose is recommended, on the basis of the present study, for all patients with rapid theophylline metabolism, i. e. children, habitually strong smokers or if the clearance is accelerated due to endogenous factors.
为评估氨茶碱（优菲龙缓释微丸）的药代动力学参数，对年龄在9至13岁以及5至9岁的儿童进行了研究，采用每日两次给药，且每日剂量分布不均。年龄较大儿童的剂量为氨茶碱400 + 200毫克，年龄较小儿童的剂量为300 + 150毫克（这些量分别代表晚上和早上的剂量）。分别有16名和14名儿童定期完成了研究。药代动力学评估结果显示，个体血清氨茶碱曲线在平均值周围呈现明显平行的趋势。早晨200至600小时的平均夜间浓度高于平均日间浓度（分别为11.4至10.5毫克/升或12.3至11.4毫克/升）。由于基线值相对稳定，临床参数仅略有改善，但峰流速曲线有特别显著的变化。在年龄较大的儿童中，我们还证实他们对乙酰甲胆碱激发有更好的保护作用。副作用一般较轻，与使用该研究制剂收集到的既往经验一致。基于本研究，对于所有氨茶碱代谢迅速的患者，即儿童、习惯性重度吸烟者或因内源性因素导致清除率加快的患者，建议采用总日剂量分布不均的给药方案。
