Wiesner B, Sehrt I, Iwainsky H
Z Erkr Atmungsorgane. 1984;162(1):3-10.
In the treatment of obstructive lung diseases theophylline is one of the most important drugs. But its therapeutic range is narrow, therefore attempts are made for an optimal therapy (dosage adjusted to the theophylline concentration in the serum, treatment with microcrystalline theophylline or retard preparations). Pharmacokinetic studies are undertaken with two theophylline formulations commercially available and the commonly used aminophylline to achieve the optimal therapeutic benefit. Regarding the results Aminophylline retard belongs to the formulations with diminished bioavailability and is therefore not satisfactorily qualified for an optimal treatment. On the other hand the development of a formulation of microcrystalline theophylline like Bronkodyl promises advantages for the long-continued treatment of obstructive lung diseases because of the smaller differences of the individual pharmacokinetic values from the median values.
在阻塞性肺部疾病的治疗中，茶碱是最重要的药物之一。但其治疗范围较窄，因此人们尝试进行优化治疗（根据血清中茶碱浓度调整剂量、使用微晶茶碱或缓释制剂进行治疗）。对两种市售茶碱制剂以及常用的氨茶碱进行了药代动力学研究，以实现最佳治疗效果。就研究结果而言，氨茶碱缓释制剂属于生物利用度降低的制剂，因此不太适合进行优化治疗。另一方面，像博利康尼这样的微晶茶碱制剂的研发，由于个体药代动力学值与中位数之间的差异较小，有望在阻塞性肺部疾病的长期治疗中发挥优势。
