异丙喘宁、特布他林和异丙肾上腺素经气管内注入大鼠后的生理处置

The physiological disposition of ibuterol, terbutaline and isoproterenol after endotracheal instillation to rats.

Ryrfeldt A, Bodin N O

Xenobiotica. 1975 Sep;5(9):521-9. doi: 10.3109/00498257509056122.

Abstract

The absorption from the respiratory tract and biotransformation of three bronchodilating drugs, terbutaline, ibuterol (diisobutyrate ester of terbutaline) and isoproterenol, have been studied in rats after endotracheal instillation. 2. At 2-15 min after dosage, ibuterol is more rapidly absorbed from the respiratory tract than terbutaline, but later (15-35 min), absorption of ibuterol is about the same as terbutaline. Absorption of isoproterenol is rapid throughout the experiment. Absorption rates have been related to the physical-chemical properties of the compounds. 3. No significant biotransformation of terbutaline was noted in the rat lung at any time after dosage, but ibuterol is extensively hydrolysed to terbutaline. Extensive biotransformation of isoproterenol to 3-methoxy-isoproterenol and an unidentified metabolite occurred. Metabolites of terbutaline and isoproterenol were found in serum and liver.

摘要

对大鼠进行气管内滴注后，研究了三种支气管扩张药物特布他林、异丁特罗（特布他林的二异丁酸酯）和异丙肾上腺素从呼吸道的吸收及生物转化情况。2. 给药后2至15分钟，异丁特罗从呼吸道的吸收比特布他林更快，但之后（15至35分钟），异丁特罗的吸收与特布他林大致相同。在整个实验过程中，异丙肾上腺素的吸收都很快。吸收速率与化合物的物理化学性质有关。3. 给药后任何时间，在大鼠肺中均未观察到特布他林有明显的生物转化，但异丁特罗被广泛水解为特布他林。异丙肾上腺素广泛生物转化为3-甲氧基-异丙肾上腺素和一种未鉴定的代谢产物。在血清和肝脏中发现了特布他林和异丙肾上腺素的代谢产物。