| 5-Fu多级前体药物在小鼠体内的代谢转化 |
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| 引用本文： | 闫美兴,李德爱,徐文方.5-Fu多级前体药物在小鼠体内的代谢转化[J].中国新药杂志,2007,16(23):1947-1949. |
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| 作者姓名： | 闫美兴 李德爱 徐文方 |
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| 作者单位： | 1. 青岛市市立医院药剂科,青岛,266011
2. 山东大学药学院,济南,250012 |
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| 摘 要： | 目的:研究5-Fu的多级前体药物N1,N3双邻甲苯甲酰基-5-Fu(DTFu)在小鼠体内的代谢转化,分析其代谢途径。方法:给小鼠分别灌胃和腹腔注射DTFu,用高效液相色谱法检测原型药物和代谢产物在血浆中的浓度。结果:2种途径给药后在小鼠血浆中均没有检测到原型药物,但能检测到代谢产物N3-邻甲苯甲酰基-氟尿嘧啶(TFu)及5-Fu。DTFu首先代谢为TFu,TFu又缓慢代谢为5-Fu。结论:DTFu具多级代谢特点,可显著延长5-Fu在体内的滞留时间。
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| 关 键 词： | 多级前体药物 代谢转化 |
| 文章编号： | 1003-3734（2007）23-1947-03 |
| 收稿时间： | 2007-05-08 |
| 修稿时间： | 2007年5月8日 |
Metabolic conversion of multiple-grade prodrugs of 5-fluorouracil in mice |
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| YAN Mei-xing,LI De-ai,XU Wen-fang.Metabolic conversion of multiple-grade prodrugs of 5-fluorouracil in mice[J].Chinese Journal of New Drugs,2007,16(23):1947-1949. |
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| Authors: | YAN Mei-xing LI De-ai XU Wen-fang |
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| Abstract: | Objective: To study metabolic conversion of multiple-grade prodrugs of 5-fluorouracil,N1,N3-double-o-toluyl-Flulorouracil DTFu,in mice in vivo and the metabolic pathways.Methods: After ig and ip administration of DTFu,the plasma concentration of DTFu and its metabolites were determined by high-performance liquid chromatography(HPLC).Results: The prototype of DTFu was not detected in plasma after ig and ip administration;while the metabolites,N3-o-toluyl-Flulorouracil(TFu) and 5-fluorouracil,were detected.DTFu was quickly and firstly metabolized into TFu,and then TFu was slowly metabolized into 5-fluorouracil.Conclusion: The characteristics of multiple-grade metabolism of DTFu in vivo results in a longer retaining time of 5-fluorouracil in the body. |
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| Keywords: | 5-Fu |
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