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目的建立体外人源肝微粒体孵育体系,应用UPLC-Q-TOF-MS法,首次对连翘脂素在人肝微粒体中的代谢产物进行鉴定。方法采用Phenomenex Kinetex C_(18)色谱柱(2.1 mm×100 mm,2.6μm),以0.1%甲酸水-乙腈为流动相进行梯度洗脱,流速为400μL·min~(-1);进样量5μL。采用正离子模式进行检测,电喷雾离子源,源温度为550℃,质量数扫描范围m/z 100~1 000。结果对ESI-MS正离子模式下连翘脂素可能的裂解途径进行了推测,同时鉴定了连翘脂素在肝微粒体中的8个代谢产物。结论所建立的连翘脂素在人肝微粒体中的UPLC-Q-TOF-MS测定法方便快捷,可应用于连翘脂素在人肝微粒中的代谢研究,同时为连翘脂素的药物代谢动力学提供了依据。
OBJECTIVE To establish an in vitro human liver microsomal incubation system, the metabolites of forsythiaside in human liver microsomes were identified for the first time by UPLC-Q-TOF-MS. Methods A gradient elution was carried out on a Phenomenex Kinetex C_ (18) column (2.1 mm × 100 mm, 2.6 μm) using 0.1% formic acid in water as mobile phase. The flow rate was 400 μL · min -1. 5 μL. Using positive ion mode for detection, electrospray ionization source, the source temperature is 550 ℃, the mass scanning range m / z 100 ~ 1 000. Results The possible cleavage pathway of forsythiaside in ESI-MS positive mode was presumed, and eight metabolites of forsythiaside in liver microsome were identified. Conclusion The UPLC-Q-TOF-MS method for the determination of forsythiaside in human liver microsomes is rapid and convenient and can be applied to the metabolism study of forsythiaside in human liver micro-particles. Pharmacokinetics provides the basis.