静脉注射蟾毒它灵和华蟾毒它灵后大鼠胆汁中代谢产物的UPLC-UV-MS法分析  

Analysis of Metabolites in Rat Bile after Intravenously-administrated Bufotalin and Cinobufotalin by UPLC-UV-MS

作　　者：王也牧[1] 丁存刚[1] 于垂亮[1] 李周[1] 葛庆华[1] 

机构地区：[1]中国医药工业研究院总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2011年第9期676-680,共5页Chinese Journal of Pharmaceuticals

摘　　要：建立了超高效液相色谱-紫外分光光度-质谱(UPLC-UV-MS)法研究蟾毒它灵和华蟾毒它灵静脉给药后大鼠胆汁中的代谢产物。UPLC的高分辨率能够基线分离胆汁中的原药和代谢物,UV光谱图揭示了各种化合物量的关系,MS进一步对代谢物进行结构表征。结果显示,大鼠胆汁中原药的含量小于5%,主要代谢物是去乙酰基并羟基化蟾毒它灵和去乙酰基华蟾毒它灵。表明蟾毒它灵在大鼠体内代谢途径主要是水解并羟基化,华蟾毒它灵主要是水解反应。The metabolites of bufotalin and cinobufotalin in rat bile were investigated by UPLC-UV-MS. High resolution UPLC was applied in the separation of the drug and metabolite peaks. An UV detector was employed to reveal the relative amount while MS was used to characterize the metabolites. It was indicated that the major metabilic pathway of bufotalin was deacetylation and hydroxylation after iv, and cinobufotalin was mostly changed into deacetylcinobufotalin. The content of bufotalin or cinobufotalin in rat bile was lower than 5%. It was concluded that the main metabolic pathway in rat bile for bufotalin was hydrolysis and hydroxylation, while for cinobufotalin was hydrolysis.

关 键 词：蟾毒它灵 华蟾毒它灵 蟾蜍甾烯 超高效液相色谱 药物代谢 

分 类 号：R917[医药卫生—药物分析学] O657.72[医药卫生—药学]