Cocchiara G, Battaglia R, Pevarello P, Strolin Benedetti M
Farmitalia Carlo Erba R&D, Erbamont Group, Milan, Italy.
Eur J Drug Metab Pharmacokinet. 1991 Jul-Sep;16(3):231-9. doi: 10.1007/BF03189965.
The purpose of this study was to compare the disposition and the metabolic pattern of Reboxetine in several species, including man. [14C]-Reboxetine was given orally to the rat, the dog, the monkey (5 mg/kg) and man (2 and 4 mg/kg). Radioactivity was eliminated both by the renal and faecal route in the rat and the dog, mainly in urine in the monkey and man. Reboxetine was extensively metabolized. A number of urinary metabolites were quantified by radio-HPLC and tentatively identified by comparison with the retention times of reference compounds. Suggested routes of metabolic transformation are: 2-O-dealkylation; hydroxylation of the ethoxyphenoxy ring; oxidation of the morpholine ring; morpholine ring-opening; and combinations of these. Metabolites were partially or completely conjugated with glucuronic acid and/or sulphuric acid.
本研究的目的是比较瑞波西汀在包括人类在内的几种物种中的处置和代谢模式。给大鼠、狗、猴子（5mg/kg）和人类（2mg/kg和4mg/kg）口服[14C] - 瑞波西汀。放射性通过大鼠和狗的肾和粪便途径消除，在猴子和人类中主要通过尿液消除。瑞波西汀被广泛代谢。通过放射性高效液相色谱法对多种尿液代谢物进行定量，并通过与参考化合物的保留时间比较进行初步鉴定。推测的代谢转化途径为：2 - O - 去烷基化；乙氧基苯氧基环的羟基化；吗啉环的氧化；吗啉环开环；以及这些反应的组合。代谢物部分或完全与葡萄糖醛酸和/或硫酸结合。
