采用液相色谱-串联质谱法对大鼠体内茶黄素A及其主要代谢产物进行药代动力学和组织分布研究。

Pharmacokinetics and tissue distribution study of camellianin A and its major metabolite in rats by liquid chromatography with tandem mass spectrometry.

作者信息

Zheng Yunliang, Hu Xingjiang, Zhai You, Liu Jian, Wu Guolan, Wu Lihua, ShenTu Jianzhong

机构信息

Research Center for Clinical Pharmacy, State Key Laboratory for Diagnosis and Treatment of Infectious Diseases, First Affiliated Hospital, Zhejiang University, Hangzhou 310003, China.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Aug 1;997:200-9. doi: 10.1016/j.jchromb.2015.06.012. Epub 2015 Jun 19.

DOI:10.1016/j.jchromb.2015.06.012

PMID:26117310

Abstract

Camellianin A is a major active constituent of Adinandra nitida. A LC-MS/MS method for the determination of camellianin A and its metabolite (camellianin B) in rat plasma and tissues was developed and applied to a pharmacokinetics and tissue distribution study. Samples were separated on a Waters HSS T3 column with a mobile phase consisted of methanol and water (containing 0.1% formic acid). MS/MS detection was carried out on a triple-quadruple mass spectrometer under negative ESI mode. Pharmacokinetics study showed that camellianin A was rapidly eliminated with a t1/2 of 92.6±41.4h and CL of 3.19±0.471L/min/kg. Additionally, camellianin A showed a low oral bioavailability of 2.99% and a narrow tissue distribution; however, camellianin B was proved to have a wide tissue distribution with brain penetration. The data presented in this study provides useful information for the further applications of A. nitida and camellianin A.

摘要

茶连素A是亮叶杨桐的主要活性成分。建立了一种LC-MS/MS方法，用于测定大鼠血浆和组织中的茶连素A及其代谢产物（茶连素B），并将其应用于药代动力学和组织分布研究。样品在Waters HSS T3柱上分离，流动相由甲醇和水（含0.1%甲酸）组成。在三重四极杆质谱仪上于负离子电喷雾电离模式下进行MS/MS检测。药代动力学研究表明，茶连素A迅速消除，半衰期为92.6±41.4小时，清除率为3.19±0.471升/分钟/千克。此外，茶连素A的口服生物利用度较低，为2.99%，组织分布较窄；然而，茶连素B被证明具有广泛的组织分布且可穿透血脑屏障。本研究提供的数据为亮叶杨桐和茶连素A的进一步应用提供了有用信息。