中国中药杂志

2014, v.39(17) 3306-3310

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HPLC-MS同时测定小鼠血浆中青蒿素、青蒿乙素、青蒿酸和东莨菪内酯的含量
Simultaneous quantitation of artemisinin,arteannuin B,artemisic acid,and scopoletin in mice plasma by HPLC-MS

闵青;卢炜;王满元;张东;周田彦;李良;
MIN Qing;LU Wei;WANG Man-yuan;ZHANG Dong;ZHOU Tian-yan;LI Liang;School of Pharmaceutical Science,Peking University;School of Traditional Chinese Medicine,Capital Medical University;Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences;

摘要(Abstract):

青蒿素是一种常用的抗疟药,但青蒿中其他组分的药效作用很少被考察。研究发现,当青蒿中的青蒿乙素、青蒿酸、东莨菪内酯3种组分与青蒿素按照质量比为1:1:1:1的比例在小鼠体内考察药效时,与等剂量青蒿素单用组相比可以起到显著的抗疟增效作用。建立血浆中同时检测青蒿素、青蒿乙素、青蒿酸和东莨菪内酯4种组分含量的HPLC-MS方法,有助于这种增效现象在药动学层面研究的进一步开展。采用Agilent公司1200-6130液质联用系统,电喷雾电离源,正离子和负离子检测方式,SIM模式;色谱分离采用Agilent Zorbax SB-C_(18)色谱柱(2.1 mm×150 mm,5μm),流动相乙腈-0.5%乙酸水溶液(60:40),流速0.3 mL·min~(-1),柱温为40.0℃,进样量5μL。结果显示,4组分血浆浓度在5~3 000μg·L~(-1)呈现良好线性关系,方法专属性、准确度、精密度良好,无基质效应。该方法适用于小鼠血浆中青蒿素、青蒿乙素、青蒿酸和东莨菪内酯的含量测定,可用于开展4组分小鼠体内药物动力学研究。
The objective of this study is to develop a sensitive and reliable high-performance liquid chromatography mass spectrometry(LC-MS) method for simultaneous determination of artemisinin,arteannuin B,artemisic acid,and scopoletin,and study the pharmacokinetics of the four constituents in mouse serum after oral administration of the four components to mice.The analytical column used was Agilent Zorbax SB-C_(18)(2.1 mm × 150 mm,5 mm).The mobile phase was acetonitrile:0.5%acetic acid(60:40) and the flow rate was 0.3 mL : min~(-1).The temperature of the column was 40.0℃.In this condition,we established an analysis method to simultaneously determine the four components.A sensitive and specific liquid chromatography-mass spectrometric(LC-MS) method was developed and validated for the determination of artemisin in derivatives in mice plasma.The method we established has a linear range of 5-3 000 μg : L~(-1) with a good sensitivity and specificity for all of the four components.This method is simple,rapid,accurate and suitable for the determination of the content of the four compounds.

关键词(KeyWords): 青蒿素;青蒿乙素;青蒿酸;东莨菪内酯;液质联用
artemisinin;arteannuin B;arteannuic acid;scopoletin;HPLC-MS

Abstract:

Keywords:

基金项目(Foundation): 北京市自然科学基金项目(2112010);; 国家自然科学基金项目(81102752);; 中国中医科学院中药研究所自主选题项目(ZZ03068);; 北京市属高等学校高层次人才引进与培养计划项目(CIT&TCD201304184)

作者(Author): 闵青;卢炜;王满元;张东;周田彦;李良;
MIN Qing;LU Wei;WANG Man-yuan;ZHANG Dong;ZHOU Tian-yan;LI Liang;School of Pharmaceutical Science,Peking University;School of Traditional Chinese Medicine,Capital Medical University;Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences;

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