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目的研究2-羟基-1-甲氧基阿朴啡在Beagle犬体内的代谢行为。方法选择健康Beagle犬3只单剂量1.5×10-3g·kg-1灌胃2-羟基-1-甲氧基阿朴啡,于给药后60min前肢静脉取血,3000r·min-1离心10min,分取血浆,将血浆经SPE-C18固相柱纯化后,采用LC-MSn方法对血浆中待测代谢产物进行总离子监测(TIM)和多级全扫描质谱分析(MSn)。结果在Beagle犬血浆中检测到母体成分2-羟基-1-甲氧基阿朴啡和3种代谢产物。结论2-羟基-1-甲氧基阿朴啡在Beagle犬体内主要与葡萄糖醛酸相结合形成II相代谢产物。
Objective To study the metabolic behavior of 2-hydroxy-1-methoxy apomorphine in Beagle dogs. Methods Three healthy Beagle dogs were administrated with 1.5 × 10-3g · kg-1 single dose of 2-hydroxy-1-methoxy apomorphine and the forelimb vein was taken 60min after the administration and centrifuged at 3000r · min-1 for 10min The plasma was separated and the plasma was purified by SPE-C18 solid phase column. Total metabolites (TIMs) and multistep MS (MSn) were analyzed by LC-MSn. Results The parent component 2-hydroxy-1-methoxy aporphine and 3 metabolites were detected in Beagle dog plasma. Conclusion 2-Hydroxy-1-methoxy apomorphine is mainly combined with glucuronic acid in Beagle dogs to form phase II metabolites.