Staib A H, Loew D, Harder S, Graul E H, Pfab R
Eur J Clin Pharmacol. 1986;30(6):691-7. doi: 10.1007/BF00608217.
The absorption of a theophylline solution containing 80-120 mg doses delivered to different sites in the gastro-intestinal tract has been determined in 3 male volunteers using a remote controlled drug release system (HF-capsule). There was no difference between the stomach, ileum and the colon in the amount of theophylline absorbed (AUC). The T 1/2abs of theophylline absorbed via the colon was prolonged when compared with that entering via the upper gastro-intestinal tract. The results provide a rational basis for the further development of theophylline formulations and are indispensable for planned development and to account for variation in the bioavailability of retarded release drug preparations.
使用遥控药物释放系统(高频胶囊),在3名男性志愿者中测定了含有80 - 120毫克剂量的茶碱溶液在胃肠道不同部位的吸收情况。在吸收的茶碱量(曲线下面积)方面,胃、回肠和结肠之间没有差异。与通过上胃肠道吸收的茶碱相比,通过结肠吸收的茶碱的吸收半衰期延长。这些结果为茶碱制剂的进一步开发提供了合理依据,对于缓控释药物制剂的计划开发以及解释其生物利用度的变化不可或缺。