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一种用于定量两种异构苯丙烯的液相色谱-串联质谱法的开发及其在大鼠体内药代动力学研究中的应用。

Development of an LC-MS/MS method for quantification of two isomeric phenylpropenes and the application to pharmacokinetic studies in rats.

作者信息

Yang Qiong, Deng Zhipeng, Zhang Fang, Sun Peilu, Li Jun, Zheng Wanjin

机构信息

Jiaozhou People's Hospital, Qingdao, China.

Institute of Materia Medica, Shandong Academy of Medical Sciences, Jinan, China.

出版信息

Biomed Chromatogr. 2018 Mar;32(3). doi: 10.1002/bmc.4115. Epub 2017 Oct 27.

DOI:10.1002/bmc.4115
PMID:29027249
Abstract

Isomers β-asarone and α-asarone have recently been demonstrated to have differential pharmacological activities. Here, we report an LC-MS/MS method developed using acetonitrile to extract two isomeric phenylpropenes from rat plasma. Separation was achieved using a XDB-C column (100 × 2.1 mm; i.d., 1.8 μm) with a mobile phase of methanol-0.1% formic acid (55:45, v/v) at a flow rate of 0.3 mL/min. Calibration curves ranging from 5.20 to 2080 ng/mL for β-asarone and from 3.68 to 1470 ng/mL for α-asarone were linear (r  ≥ 0.9938) with the lower limits of quantification being 5.20 and 3.68 ng/mL for both isomers. Intravenous administration of β-asarone (2.22 mg/kg) and α-asarone (2.36 mg/kg) in rats yielded half-lives of 13.40 ± 4.11 and 28.88 ± 7.82 min with clearance values of 0.196 ± 0.062 mL/min/kg and 0.112 ± 0.012 mL/min/kg for β-asarone and α-asarone, respectively.

摘要

异构体β-细辛醚和α-细辛醚最近被证明具有不同的药理活性。在此,我们报告一种使用乙腈从大鼠血浆中提取两种异构苯丙烯的LC-MS/MS方法。采用XDB-C柱(100×2.1mm;内径,1.8μm),以甲醇-0.1%甲酸(55:45,v/v)为流动相,流速为0.3mL/min进行分离。β-细辛醚的校准曲线范围为5.20至2080ng/mL,α-细辛醚的校准曲线范围为3.68至1470ng/mL,均呈线性(r≥0.9938),两种异构体的定量下限均为5.20和3.68ng/mL。大鼠静脉注射β-细辛醚(2.22mg/kg)和α-细辛醚(2.36mg/kg)后,β-细辛醚和α-细辛醚的半衰期分别为13.40±4.11和28.88±7.82分钟,清除率分别为0.196±0.062mL/min/kg和0.112±0.012mL/min/kg。

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