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Simultaneous determination of forsythin and its major metabolites in human plasma via liquid chromatography-tandem mass spectrometry

文献类型：期刊论文

作者Pan, Lu-lu1,2; Chen, Tao3; Hui, Min4; Wang, Shuo4; Fu, Li4; Li, Cui-yun5; Zhang, Hong5; Ding, Yan-hua5; Yang, Yong3; Zhong, Da-fang1,2
刊名JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
出版日期2021-05-10
卷号198页码:7
关键词LC-MS/MS Forsythin Aglycone glucuronide Aglycone sulfate Pharmacokinetics
ISSN号0731-7085
DOI10.1016/j.jpba.2021.113992
通讯作者Yang, Yong(yong.yang@hq-biosci.com) ; Zhong, Da-fang(dfzhong@simm.ac.cn)
英文摘要Forsythiae suspensa is widely used in China as a traditional Chinese medicine. Forsythin is extracted from Forsythiae Fructus and has undergone phase II clinical trials as an antipyretic drug in China. The main metabolites of forsythin in human plasma are aglycone sulfate (KD-2-SO3H) and aglycone glucuronide (KD-2-Glc). In the present study, a sensitive and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and fully validated for the simultaneous analysis of forsythin, KD-2Glc, and KD-2-SO3H, in human plasma. After precipitating proteins with methanol, these three analytes were separated on a Gemini-C18 column along with teniposide as an internal standard. Mass spectrometry detection, under multiple reaction monitoring, was then carried out in negative mode using the Triple Quad (TM) 6500(+) LC-MS/MS system coupled with an electrospray ionization (ESI) ion source. The transitions of m/z 371.1 -> 356.1 for forsythin, m/z 547.2 -> 356.0 for KD-2-Glc and m/z 451.2 -> 356.2 for KD-2-SO3H were chosen to effectively maintain the balance between selectivity and sensitivity. The developed method was linear over the following concentrations in human plasma samples: 1.00-1000 ng/mL for forsythin, 2.50-2500 ng/mL for KD-2-Glc, and 5.00-5000 ng/mL for KD-2-SO3H. Assays were validated and satisfied the acceptance criteria recommended by the CFDA guidance. Furthermore, this LC-MS/MS method was successfully implemented in a Phase I, first-in-human, dose-escalation pharmacokinetic study among Chinese healthy participants after single oral administration of forsythin tablets. (C) 2021 Elsevier B.V. All rights reserved.
资助项目National Natural Science Foundation of China[81521005] ; Strategic Priority ResearchProgram of the Chinese Academy of Sciences[XDA12050306]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000636654000011
出版者ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/295244]  
专题新药研究国家重点实验室
通讯作者Yang, Yong; Zhong, Da-fang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Suzhou Haike Med Technol Co Ltd, Suzhou 215123, Peoples R China
4.Dalian Fusheng Pharmaceut Co Ltd, Dalian 116000, Peoples R China
5.First Hosp Jilin Univ, Changchun 130021, Peoples R China
推荐引用方式
GB/T 7714		 Pan, Lu-lu,Chen, Tao,Hui, Min,et al. Simultaneous determination of forsythin and its major metabolites in human plasma via liquid chromatography-tandem mass spectrometry[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2021,198:7.
APA Pan, Lu-lu.,Chen, Tao.,Hui, Min.,Wang, Shuo.,Fu, Li.,...&Zhong, Da-fang.(2021).Simultaneous determination of forsythin and its major metabolites in human plasma via liquid chromatography-tandem mass spectrometry.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,198,7.
MLA Pan, Lu-lu,et al."Simultaneous determination of forsythin and its major metabolites in human plasma via liquid chromatography-tandem mass spectrometry".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 198(2021):7.

入库方式： OAI收割

来源：上海药物研究所

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