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Pharmacokinetics and tissue distribution study of camellianin A and its major metabolite in rats by liquid chromatography with tandem mass spectrometry
Journal of Chromatography B ( IF 2.8 ) Pub Date : 2015-06-19 , DOI: 10.1016/j.jchromb.2015.06.012
Yunliang Zheng , Xingjiang Hu , You Zhai , Jian Liu , Guolan Wu , Lihua Wu , Jianzhong ShenTu

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 ± 41.4 h and CL of 3.19 ± 0.471 L/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.



中文翻译:

液相色谱-串联质谱法研究山茶素A及其主要代谢产物在大鼠体内的药代动力学和组织分布

Camellianin A是Adinandra nitida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山茶素A及其代谢物(山茶素B),并将其用于药代动力学和组织分布研究。样品在Waters HSS T3色谱柱上分离,流动相由甲醇和水(含0.1%甲酸)组成。MS / MS检测是在三重四极杆质谱仪上以负ESI模式进行的。药代动力学研究表明,t 1/2可以迅速消除山茶素A92.6±41.4 h的CL和3.19±0.471 L / min / kg的CL。此外,山茶素A显示出较低的口服生物利用度,为2.99%,并且组织分布较窄。然而,事实证明,山茶花B具有广泛的组织分布并具有大脑渗透能力。本研究中提供的数据为A. nitida和camellianin A的进一步应用提供了有用的信息。

更新日期:2015-06-19
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