| 5-氟尿嘧啶-聚[N-(2-羟乙基)-L-谷酰胺]的合成及缓释性能研究 |
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| 引用本文： | 张静夏,潘仕荣,王琴梅,冯敏,吴伟荣.5-氟尿嘧啶-聚[N-(2-羟乙基)-L-谷酰胺]的合成及缓释性能研究[J].广州化学,2002,27(2):1-5. |
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| 作者姓名： | 张静夏 潘仕荣 王琴梅 冯敏 吴伟荣 |
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| 作者单位： | 1. 中山大学中山医学院化学教研室,广东,广州,510089
2. 中山大学附属第一医院人工心研究室,广东,广州,510089 |
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| 摘 要： | 以聚谷氨酸苄酯为原料,用乙醇胺进行胺解得水溶性的可生物降解的聚N-(2-羟乙基)-L-谷酰胺];用光气/甲苯液活化5-氟尿嘧啶,将其以共价键形式键合在高分子上,得5-氟尿嘧啶的高分子前药。用IR、UV、1HNMR及DSC对其结构进行表征,用紫外光谱测定其药物含量,载药高分子的接药率约为38.4%,高分子前药在pH=7.2的磷酸盐介质中42天内的药物累积释放量为57.53%。实验结果表明,5-氟尿嘧啶以共价键的形式键合在聚N-(2-羟乙基)-L-谷酰胺]之上,在体外有明显的缓释效果。
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| 关 键 词： | 聚[N-(2-羟乙基)-L-谷酰胺] 5-氟尿嘧啶-聚[N-(2-羟乙基)-L-谷酰胺] 高分子前药 缓释 |
| 文章编号： | 1009-220(2002)02-0001-05 |
| 修稿时间： | 2002年1月22日 |
Synthesis of 5-Fluorouracil-Poly[N(2-Hydroxyethyl)- L-Glutamine] and Its Sustained Release Effect |
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| ZHANG Jing-xia,PAN Shi-rong,WANG Qin-mei,FENG Min,WU Wei-rong.Synthesis of 5-Fluorouracil-Poly[N(2-Hydroxyethyl)- L-Glutamine] and Its Sustained Release Effect[J].Guangzhou Chemistry,2002,27(2):1-5. |
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| Authors: | ZHANG Jing-xia PAN Shi-rong WANG Qin-mei FENG Min WU Wei-rong |
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| Institution: | ZHANG Jing-xia1,PAN Shi-rong2,WANG Qin-mei2,FENG Min2,WU Wei-rong2 |
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| Abstract: | Water-soluble and biodegradable polyN -(2-hydroxyethyl)-L-glutamine](PHEG) was synthesized by poly-(γ-benzyl)-L-glutamine] with 2-aminoethanol first, then 5- fluorouracil was activated by the solution of phosgene/toluene and conjugated to PHEG. The conjugated compound was characterized by IR,UV,1HNMR and DSC. The content of 5- fluorouracil was detected by UV method and was about 38.4%. The accumulated released amounts was 57.53% in phosphorus salt buffer solution (pH=7.2) during 6w.The results showed that 5-fluorouracil was conjugated to PHEG and the conjugated compound had obvious sustained- release effects. |
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| Keywords: | poly[N-(2-hydroxyethyl)-L-glutamine] 5-fluorouracil- poly[N-(2-hydroxyethyl) - L - glutamine] prodrug sustained-release |
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