Vondra V, Spicák V, Trnavská Z, Reisová M, Pohunek P, Tomíska F
Cas Lek Cesk. 1989 May 5;128(19):595-8.
Monitoring of theophyllinaemia in the course of 24 h during treatment with theophylline anhydrate capsules (Euphyllin CR) was used in 20 children (9-15 years) and in 20 adults (18-61 years) with bronchial asthma. The doses used in children were 5.96 mg/kg at 7 a.m. and 10.2 mg/kg at 7 p.m., while in adults the morning and evening doses were similar (4.35 and 4.89 mg/kg). After the first dose in the morning the serum theophylline concentration (STC) did not differ in children and adults (10.4 and 10.5 mg/l). In adults the half-time of absorption was twice as high as in children (0.63 and 0.3 h), as well as the time when the peak theophylline concentration was reached (2.7 and 1.39 h). In children a double dose of the drug at night ensured a STC of 11.2 mg/l and a maximum theophyllinaemia (C max = 13.5 mg/l between 8 p.m. and 6 a.m. (measured by the EMIT method). In adults the values during the night were significantly lower than in day-time (STC: ANOVA test P less than 0.05, C max: T-test P less than 0.01). The percentage fluctuation in individual subjects was small (36-49) interindividual, fluctuations in children and adults were considerable (105 to 207). From the chronoprofile of the pharmacokinetics of Euphyllin CR ensues that at the age of 9-15 years the most important indicators are similar to those in adults and that both groups should be given at night a double dose, as compared with that administered in the morning.
对20名儿童（9至15岁）和20名成人（18至61岁）支气管哮喘患者，在使用无水茶碱胶囊（优菲林控释片）治疗过程中进行了24小时的血药浓度监测。儿童使用的剂量为上午7点5.96毫克/千克，晚上7点10.2毫克/千克，而成人早晚剂量相似（分别为4.35和4.89毫克/千克）。上午首次给药后，儿童和成人的血清茶碱浓度（STC）无差异（分别为10.4和10.5毫克/升）。成人的吸收半衰期是儿童的两倍（分别为0.63和0.3小时），达到茶碱峰值浓度的时间也是儿童的两倍（分别为2.7和1.39小时）。儿童夜间加倍剂量用药可使STC达到11.2毫克/升，最高血药浓度（Cmax = 13.5毫克/升，在晚上8点至早上6点之间，采用酶放大免疫测定法测定）。成人夜间的值明显低于白天（STC：方差分析检验P < 0.05，Cmax：t检验P < 0.01）。个体受试者的波动百分比小（个体间为36 - 49），儿童和成人的个体间波动相当大（105至207）。从优菲林控释片的药代动力学时间曲线可以看出，9至15岁儿童的最重要指标与成人相似，与上午给药相比，两组在夜间均应加倍剂量给药。
