摘要
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 investigate the major metabolites of 2-hydroxy-1-methoxyaporphine in Beagle dogs. METHODS The blood samples were collected from vein after a single dose of 1.5 mg.kg-1 2-hydroxy-1-methoxyaporphine. The plasma samples were purified by a SPE column (SPE-CIs) and analyzed with LC/MSn for potential metabolites. RESULTS 2-hydroxy-l-methoxyaporphine and its three metabolites were first identified in Beagle dogs plasma. CONCLUSION The major metabolic pathway of 2-hydroxy-1-methoxyaporphine in Beagle dogs is conjugating with glucuronic acid, forming phase II mctabolites.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第20期1574-1577,共4页
Chinese Pharmaceutical Journal
基金
"十一五"国家科技支撑计划(2006BAI08B03-04)
国家自然科学基金(90409011)
北京市自然科学基金(7061002)