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。
Water-soluble and biodegradable poly[N -(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.
出处
《广州化学》
CAS
2002年第2期1-5,共5页
Guangzhou Chemistry
