Heier M S, Heintz R, Fosså S D
Acta Neurol Scand. 1986 Sep;74(3):240-4. doi: 10.1111/j.1600-0404.1986.tb07862.x.
Lumbar puncture was performed on eight patients in a clinical Phase 1 study of doxifluridine (5'-dFDrd). 5'-dFUrd, 5'FU, and 5-FUH2 were shown to cross the blood-brain barrier to CSF. The maximal concentrations of 5'-dFUrd and 5-FUH2 were about 1-3% of the maximal concentrations in plasma, and were reached within 1-4 h after the end of iv infusion of 5'-dFUrd. 5-FUH2 showed a marked increase in CSF between 3 and 4 h to about 40-60% of the maximal plasma concentration in 5 of the patients, indicating a possible further increase after 4 h. The relationship between the concentrations of 5'-dFUrd and its metabolites in the CSF, and CNS toxicity is discussed.
在一项多西氟尿苷（5'-dFDrd）的临床1期研究中，对8名患者进行了腰椎穿刺。结果显示，5'-dFUrd、5'FU和5-FUH2可穿过血脑屏障进入脑脊液。5'-dFUrd和5-FUH2的最大浓度约为血浆中最大浓度的1%-3%，在静脉输注5'-dFUrd结束后1-4小时内达到。在5名患者中，5-FUH2在3至4小时之间脑脊液中的浓度显著增加，达到最大血浆浓度的约40%-60%，这表明4小时后可能会进一步增加。文中讨论了脑脊液中5'-dFUrd及其代谢物的浓度与中枢神经系统毒性之间的关系。
