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  • Title: Determination of tegafur, 5-fluorouracil, gimeracil and oxonic acid in human plasma using liquid chromatography-tandem mass spectrometry.
    Author: Liu K, Zhong D, Zou H, Chen X.
    Journal: J Pharm Biomed Anal; 2010 Aug 01; 52(4):550-6. PubMed ID: 20138454.
    Abstract:
    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. FT, 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 12.0-3000ng/mL for FT, and 2.00-500ng/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 [(13)C(2),(15)N(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 2.00-150ng/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 60mg S-1 tablets to patients with solid gastrointestinal tract tumors.
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