Marunaka T, Umeno Y
J Chromatogr. 1978 Sep 21;157:321-30. 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.
1,3-双(四氢-2-呋喃基)-5-氟-2,4-嘧啶二酮已作为一种抗肿瘤药物进入临床开发阶段。已开发出一种高压液相色谱法,用该方法可在血浆中对其进行测定,灵敏度为0.050微克/毫升。其两种代谢物,1-(四氢-2-呋喃基)-5-氟-2,4-嘧啶二酮和3-(四氢-2-呋喃基)-5-氟-2,4-嘧啶二酮,可同时以0.025微克/毫升的灵敏度进行测定。已开发出一种气相色谱-质谱碎片分析法,用于特异性测定第三种代谢物5-氟-2,4-嘧啶二酮,以其硅烷化衍生物形式测定,灵敏度为0.001微克/毫升。该测定方法的精密度和灵敏度对于测定药物的血浆水平似乎是令人满意的。