Van Aerde P, Moerman E, Van Severen R, Braeckman P
Pharmazie. 1984 Mar;39(3):171-2.
In order to find a suitable animal model for biopharmaceutical studies after rectal application of theophylline, the pharmacokinetics of theophylline following the administration in rabbits of three different rectal preparations were examined and compared with those of the oral and i. v. route. No significant formulation related impact from the studied rectal dosage forms on the bioavailability of the drug was found. However, the unexpected rapid achievement of peak serum concentration after insertion of the suppository lacked any correlation with human experiments. It was concluded that the evaluation of rectal theophylline medication for man cannot directly be based on the data obtained from rabbits.
为了找到一种适合直肠应用茶碱后进行生物制药研究的动物模型,研究了三种不同直肠制剂在兔体内给药后茶碱的药代动力学,并与口服和静脉注射途径的药代动力学进行了比较。未发现所研究的直肠剂型对药物生物利用度有显著的制剂相关影响。然而,插入栓剂后血清峰值浓度意外快速达到,这与人体实验没有任何相关性。得出的结论是,不能直接根据从兔子身上获得的数据来评估人类直肠应用茶碱的情况。