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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
引用本文:王也牧,丁存刚,于垂亮,李周,葛庆华.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[J].中国医药工业杂志,2011,42(9).
作者姓名:王也牧  丁存刚  于垂亮  李周  葛庆华
作者单位: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
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.

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

Analysis of Metabolites in Rat Bile after Intravenously-administrated Bufotalin and Cinobufotalin by UPLC-UV-MS
Authors:WANG Yemu  DING Cungang  YU Chuiliang  LI Zhou  GE Qinghua
Institution:WANG Yemu,DING Cungang,YU Chuiliang,LI Zhou,GE Qinghua~* (National Pharmaceutical Engineering and Research Center,China State Institute of Pharmaceutical Industry,Shanghai 201203)
Abstract: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 wa...
Keywords:bufotalin  cinobufotalin  bufadienolide  UPLC  metabolites  
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