Quantitative determination of 1,3-bis(tetrahydro-2- furanyl)-5-fluoro-2,4-pyrimidinedione and its metabolites in plasma by high-pressure liquid chromatography and gas chromatography-mass fragmentography

• Published in: Journal of chromatography Vol. 157; p. 321
• Main Authors: Marunaka, T, Umeno, Y
• Format: Journal Article
• Language: English
• Published: Netherlands 21-09-1978
• Subjects: Antineoplastic Agents - blood; Chromatography, Gas; Chromatography, High Pressure Liquid; Furans - blood; Gas Chromatography-Mass Spectrometry; Humans; Pyrimidinones - blood
• DOI: 10.1016/S0021-9673(00)92349-5

1,3-Bis(tetrahydro-2-furanyl)-5-fluoro-2,4-pyrimidinedione has been developed clinically as an antitumor agent. A high-pressure liquid chromatographic method was developed with which it could be measured in plasma with a sensitivity of 0.050 microgram/ml. Two of its metabolites, 1-(tetrahydro-2-furanyl)-5-fluoro-2,4-pyrimidinedione and 3-(tetrahydro-2-furanyl)-5-fluoro-2,4-pyrimidinedione, could be determined at the same time with a sensitivity of 0.025 microgram/ml. A gas chromatographic-mass fragmentographic method was developed for the specific determination of the third metabolite, 5-fluoro-2,4-pyrimidinedione, as its silylated derivative with a sensitivity of 0.001 microgram/ml. The precision and sensitivity of the assay appear to be satisfactory for determination of the plasma level of the drug.