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Simultaneous quantification of 3 ',4 '-dimethoxy flavonol-3-O-glucoside and its major metabolite in human plasma by LC-MS/MS and its application to a clinical pharmacokinetic study

文献类型：期刊论文

作者Wang, Lu2; Shen, Haifeng2; Zhan, Yan2; Zhang, Yifan2; Zhang, Yong1; Chen, Min1; Li, Xiaoju1; Zhong, Dafang2
刊名JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
出版日期2023-02-20
卷号225页码:9
关键词3?4?-Dimethoxy flavonol-3-O-glucoside Aglycone glucuronide LC-MS MS Human pharmacokinetic study
ISSN号0731-7085
DOI10.1016/j.jpba.2022.115203
通讯作者Li, Xiaoju(lixj.81@pharm81.com) ; Zhong, Dafang(dfzhong@simm.ac.cn)
英文摘要Hyperlipidemia is a disease characterized by abnormal blood lipid levels and is the leading risk factor for car-diovascular disease. 3 ',4 '-Dimethoxy flavonol-3-O-glucoside (abbreviated DF3G) is a new lipid-lowering drug created as a flavonoid structural analog. The principal metabolite of DF3G in human plasma is the aglycone glucuronide conjugate M2. The purpose of this study is to use liquid chromatography-tandem mass spectrometry to develop and validate a quantitative analysis method for DF3G and its metabolite M2 in human plasma, and to use the method to investigate the pharmacokinetics of DF3G and M2 in a clinical trial. This method employed DF3G-d6 as the internal standard, and plasma samples were processed by protein precipitation. Isocratic sepa-ration could accurately differentiate DF3G, M2, and DF3G-d6 from endogenous components in the matrix or other components in the samples, and endogenous components in the matrix had little impact on ionization efficiency. Positive electrospray ionization with multiple reaction monitoring (MRM) transitions of m/z 461.2-* 299.0 for DF3G, m/z 475.1-* 299.1 for M2 and m/z 467.1-* 305.1 for DF3G-d6 was used for quantification. The DF3G and M2 linear range for plasma were in the range of 4.00/4.00 ng/mL to 4000/4000 ng/mL. Both the analytes and the internal standard were stable regardless of whether they were in solution or plasma samples. The accuracy of the average concentration of the quality control samples was within 15% of the theoretical value, and the RSD was less than 15%. The method is rapid, accurate, straightforward, and precise. It is appropriate for the determination of DF3G and M2 concentrations in human plasma and has been successfully applied to determine the pharmacokinetic analysis in phase I clinical trials.
WOS关键词HYPERLIPIDEMIA ; FLAVONOIDS ; NARINGENIN ; QUERCETIN ; INSIGHTS
资助项目National Natural Science Foundation of China[81521005] ; Zhongshan Hospital Affiliated with Fudan University (Shanghai, China) ; Eight Plus One Pharmaceutical Co., Ltd (Guilin, China)
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000912343900001
出版者ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/303805]  
专题新药研究国家重点实验室
通讯作者Li, Xiaoju; Zhong, Dafang
作者单位1.Eight Plus One Pharmaceut Co Ltd, Guilin 541000, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Lu,Shen, Haifeng,Zhan, Yan,et al. Simultaneous quantification of 3 ',4 '-dimethoxy flavonol-3-O-glucoside and its major metabolite in human plasma by LC-MS/MS and its application to a clinical pharmacokinetic study[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2023,225:9.
APA Wang, Lu.,Shen, Haifeng.,Zhan, Yan.,Zhang, Yifan.,Zhang, Yong.,...&Zhong, Dafang.(2023).Simultaneous quantification of 3 ',4 '-dimethoxy flavonol-3-O-glucoside and its major metabolite in human plasma by LC-MS/MS and its application to a clinical pharmacokinetic study.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,225,9.
MLA Wang, Lu,et al."Simultaneous quantification of 3 ',4 '-dimethoxy flavonol-3-O-glucoside and its major metabolite in human plasma by LC-MS/MS and its application to a clinical pharmacokinetic study".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 225(2023):9.

入库方式： OAI收割

来源：上海药物研究所

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