Falliers C J
Int J Clin Pharmacol Biopharm. 1979 Mar;17(3):125-30.
A prolonged therapeutic effect following a single oral dose of theophylline and maintenance of an adequate therapeutic blood level of theophylline is an important factor in the management of chronic bronchial asthma. Eighteen adult asthmatics, nine of whom were females and nine males, aged between 21-53 years, were given a sustained release theophylline capsule, 250 mg, every 12 hours and pulmonary mechanical functions as well as serum theophylline levels were studied. All patients received Elixophyllin Elixir, 250 mg, and their serum level as well as pulmonary functions were studied and compared to those after receiving the sustained release capsules. In these patients, after isoproterenol inhalation, an average of 25.6% improvement in FEV1 was observed while after placebo there were very minimum changes. At the steady-state of sustained release theophylline capsule administration, an average of 20% improvement of FEV1 was observed at the five hour period and sufficient bronchodilation expressed as FEV1 was observed for a 10-12 hour period. Indeed, a sustained release theophylline capsule fulfilled the requirement that it adequately maintained therapeutic theophylline level of the blood and improved bronchodilation lasting up to 12 hours.
单次口服茶碱后产生的延长治疗效果以及维持足够的茶碱治疗血药浓度是慢性支气管哮喘管理中的一个重要因素。18名成年哮喘患者,其中9名女性和9名男性,年龄在21至53岁之间,每12小时服用一粒250毫克的缓释茶碱胶囊,并对肺机械功能和血清茶碱水平进行了研究。所有患者均服用250毫克的Elixophyllin Elixir,并对其血清水平和肺功能进行了研究,并与服用缓释胶囊后的情况进行了比较。在这些患者中,吸入异丙肾上腺素后,观察到第一秒用力呼气量(FEV1)平均改善25.6%,而服用安慰剂后变化极小。在缓释茶碱胶囊给药的稳态期,在5小时期间观察到FEV1平均改善20%,并且在10至12小时期间观察到以FEV1表示的足够的支气管扩张。实际上,缓释茶碱胶囊满足了充分维持血液中茶碱治疗水平并改善长达12小时的支气管扩张的要求。