Tomlinson A J, Benson L M, Gorrod J W, Naylor S
Department of Biochemistry and Molecular Biology, Mayo Clinic, Rochester, MN 55905.
J Chromatogr B Biomed Appl. 1994 Jul 15;657(2):373-81. doi: 10.1016/0378-4347(94)00142-1.
The in vitro metabolism of mifentidine, a prototype second-generation histamine H2-antagonist, is investigated using on-line capillary electrophoresis-mass spectrometry (CE-MS) by analysis of hepatic microsomal incubates. Consideration of the hydrophobicity of this drug and putative metabolites led to the development of a non-aqueous CE separation medium consisting of 5 mM NH4OAc in methanol containing 100 mM acetic acid. Benefits of non-aqueous media in CE-MS studies of small hydrophobic molecules are discussed. In addition, we elucidate both chemical transformations and the in vitro metabolism of mifentidine using guinea pig hepatic microsomes.
使用在线毛细管电泳-质谱联用（CE-MS）技术，通过分析肝微粒体孵育液，对第二代组胺H2拮抗剂原型药物米芬替丁的体外代谢进行了研究。考虑到该药物及其假定代谢物的疏水性，开发了一种非水CE分离介质，其由含100 mM乙酸的甲醇中的5 mM醋酸铵组成。讨论了非水介质在CE-MS对小疏水分子研究中的优势。此外，我们还利用豚鼠肝微粒体阐明了米芬替丁的化学转化和体外代谢情况。
