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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。
A high performance liquid chromatography-ultraviolet spectrophotometry-mass spectrometry (UPLC-UV-MS) was developed to study the metabolites of rat bufalin after bupivacaine and bufalin intravenous injection. The high resolution of UPLC enables the baseline separation of the prodrugs and metabolites in bile, UV spectroscopy reveals the relationship between amounts of various compounds, and MS further characterizes the metabolites. The results showed that the rat bile Zhongyuan drug content of less than 5%, the main metabolites are deacetylated and hydroxylated bufalin and deacetylated bufalodine. It showed that bufogenin is mainly hydrolyzed and hydroxylated in the rat metabolic pathways, and lanthanon toxin is mainly hydrolyzed.