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应用体内１９ＦＮＭＲ谱观察并定量评价了５－氟尿嘧啶（５－ＦＵ）在荷Ｓ１８０瘤和Ｂ１６瘤小鼠肿瘤内的摄取和代谢动力学过程．５－ＦＵ２００ｍｇ·ｋｇ－１ｉｖ后，药物在Ｓ１８０和Ｂ１６瘤内的主要产物为其活性产物氟代核苷／核苷酸（ＦＮＵＣ），同时可检测到少量的降解产物α－氟－β－丙氨酸（ＦＢＡＬ）和α－氟－β－脲基丙酸（ＦＵＰＡ）．在Ｓ１８０瘤内，５－ＦＵ摄取，消除以及ＦＮＵＣ的生成有较大的个体变异，５－ＦＵ的消除半衰期ｔ１／２ｋｅ为４１．５－８４．８ｍｉｎ，ＦＮＵＣ生成ｔ１／２ｒ为２６．０－９１．９ｍｉｎ．当甲氨蝶呤（ＭＴＸ）与５－ＦＵ合用时，５－ＦＵ在Ｓ１８０瘤内的活化代谢过程明显加快，ｔ１／２ｋｅ缩短为２９．９－４３．４ｍｉｎ，ＦＮＵＣ的生成速率显著提高，生成量增加．５－ＦＵ在Ｂ１６瘤内的摄取及代谢过程的个体波动较小，其ｔ１／２ｋｅ为３９±５ｍｉｎ，ＦＮＵＣ的生成ｔ１／２ｒ为６０±７ｍｉｎ，在Ｂ１６瘤内，ＭＴＸ的合用不能明显加快５－ＦＵ转化为ＦＮＵＣ的反应，也不改变５－ＦＵ在瘤内的消除模式．上述结果表明，５－ＦＵ对肿瘤的化疗作用与肿瘤灌注５－ＦＵ在瘤组织内的摄取和活化代谢过程密切相关，亦可受到合用药物的影响．
In vivo 19F NMR spectroscopy was used to observe and quantitatively evaluate the uptake and kinetics of 5-fluorouracil (5-FU) in tumors of S180 and B16 tumor-bearing mice. The main products of the drug in S180 and B16 tumors after 5-FU administration of 200 mg · kg-1iv were the active products of FNUC, and a small amount of degradation products α-fluoro-β-C (FBAL) and α-fluoro-β-ureido propionic acid (FUPA). In S180 tumor, 5-FU uptake and elimination and FNUC production had larger individual variation, the elimination half-life t1 / 2ke of 5-FU was 41.5-84.8min, the FNUC generation t1 / 2r was 26.0- 91.9min. When methotrexate (MTX) was used in combination with 5-FU, the activation and metabolism of 5-FU in S180 tumor significantly accelerated, the t1 / 2ke shortened to 29.9-43.4min, FNUC generation rate was significantly increased, generated Increase in volume. The uptake of 5-FU and the individual fluctuation of metabolism in B16 tumor were small with the t1 / 2ke of 39 ± 5min and the generation of FNUC of t1 / 2r of 60 ± 7min. The combination of MTX in B16 tumor could not be obviously accelerated 5 -FU conversion to FNUC does not alter 5-FU elimination patterns in the tumor. The above results show that 5-FU on tumor chemotherapy and tumor perfusion of 5-FU in the tumor tissue uptake and activation of metabolic processes are closely related, may also be affected by the combination of drugs.