Selvig K, Alme A, Rugstad H E, Aas K, Bjerve K S
Acta Paediatr Scand. 1981 Nov;70(6):929-33. doi: 10.1111/j.1651-2227.1981.tb06253.x.
A new, low dose sustained-release tablet of theophylline has been developed in order to facilitate a correct dose regimen in asthmatic children treated with theophylline. The formulation (Euphyllin retard mite w/groove) contains 128 mg of theophylline, and can easily be divided. The extent of bioavailability in adults is 0.91, and the peak serum concentration is reached after 8.7 h. 25 children treated with plain theophylline tablets were followed when changing to the sustained-release tablets. Compared to the plain tablets, the serum theophylline concentration before the morning dose was 29 mumol/l higher (range 12-51) when the same daily dose was given as a sustained-release preparation. The serum concentration fluctuations during one dosing interval were reduced with 13 mumol/l (0-26). Mild gastrointestinal side effects reported by the children when using the plain theophylline tablets all disappeared on changing to the sustained-release tablets.
为了便于接受茶碱治疗的哮喘儿童采用正确的给药方案，已研制出一种新型低剂量缓释茶碱片。该制剂（优菲林缓释微粒带刻痕）含有128毫克茶碱，且易于分割。在成年人中的生物利用度为0.91，8.7小时后达到血清峰值浓度。在25名接受普通茶碱片治疗的儿童改用缓释片时进行了跟踪观察。与普通片相比，当给予相同日剂量的缓释制剂时，晨服前的血清茶碱浓度高出29微摩尔/升（范围为12 - 51）。一个给药间隔期间的血清浓度波动降低了13微摩尔/升（0 - 26）。改用缓释片后，儿童在使用普通茶碱片时报告的轻度胃肠道副作用全部消失。
