Determination of tegafur, 5-fluorouracil, gimeracil and oxonic acid in human plasma using liquid chromatography-tandem mass spectrometry
文献类型：期刊论文
| 作者 | Liu, Ke; Zhong, Dafang ; Zou, Huiyu; Chen, Xiaoyan
|
| 刊名 | JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 |
| 出版日期 | 2010-08-01 |
| 卷号 | 52期号:4页码:550-556 |
| 关键词 | Tegafur Gimeracil Oxonic acid 5-Fluorouracil LC-MS/MS |
| ISSN号 | 0731-7085 |
| DOI | 10.1016/j.jpba.2010.01.026 |
| 文献子类 | Article |
| 英文摘要 | S-1 is an oral anticancer drug, which Consists of tegafur (FT), gimeracil (CDHP) and potassium oxonate (Oxo) at a molar ratio of 1:0.4:1. Among these, tegafur is a prodrug, and is rapidly metabolized to the active drug, 5-fluorouracil (5-FU), in vivo. To evaluate the pharmacokinetics of S-1 in patients, LC-MS/MS methods were developed and validated for determination of FT, 5-FU, CDHP and Oxo in human plasma. 5-FU and CDHP were extracted from plasma following protein precipitation, separated on a Synergi Hydro-RP column and simultaneously quantified by LC-MS/MS. The mobile phase consisted of methanol-water-ammonia-acetic acid (27:73:0.0018:0.018, v/v/v/v). The mass spectrometer was operated in negative mode using electrospray ionization. The calibration curves were linear in the range of 12.0-3000 ng/mL for FT, and 2.00-500 ng/mL for 5-FU and CDHP. The accuracy ranged from 93.1% to 110.7% and the precision ranged from 2.4% to 14.6% for each analyte. To determine Oxo in human plasma, an LC-MS/MS method employing pre-column derivatization was developed and validated. 4-Bromomethyl-7-methoxycoumarin was chosen as the derivatization reagent and [C-13(2), N-15(3)]-Oxo was used as the internal standard. The MS/MS detection was operated in positive mode using an APCI source. The calibration range was 2.00-150 ng/mL. The accuracy and precision were within 95.9-99.1% and 4.4-10.0%, respectively. The validated methods were successfully applied to characterize the pharmacokinetic profiles of FT, 5-FU, CDHP and Oxo following oral administration of 60 mg S-1 tablets to patients with solid gastrointestinal tract tumors. (C) 2010 Elsevier B.V. All rights reserved. |
| WOS关键词 | POTASSIUM OXONATE ; RAT-LIVER ; DERIVATIZATION ; URINE ; ASSAY ; S-1 ; 4-BROMOMETHYL-7-METHOXYCOUMARIN ; METABOLITES ; DERIVATIVES ; VALIDATION |
| 资助项目 | National Science & Technology Major Project, China[2009ZX09301-001] ; Science and Technology Commission of Shanghai Municipality[08DZ1980200] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000276057300016 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278818]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Chen, Xiaoyan |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Ke,Zhong, Dafang,Zou, Huiyu,et al. Determination of tegafur, 5-fluorouracil, gimeracil and oxonic acid in human plasma using liquid chromatography-tandem mass spectrometry[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2010,52(4):550-556. |
| APA | Liu, Ke,Zhong, Dafang,Zou, Huiyu,&Chen, Xiaoyan.(2010).Determination of tegafur, 5-fluorouracil, gimeracil and oxonic acid in human plasma using liquid chromatography-tandem mass spectrometry.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,52(4),550-556. |
| MLA | Liu, Ke,et al."Determination of tegafur, 5-fluorouracil, gimeracil and oxonic acid in human plasma using liquid chromatography-tandem mass spectrometry".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 52.4(2010):550-556. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。