5-氟尿嘧啶-聚α,β(2-羟乙基)-DL-天冬酰胺的合成及体内释放的研究  

PREPARTION OF 5 FLUOROURACIL POLY α,β(2 HYDROXYETHY1) DL ASPARAMIDE AND IN VIVO RELEASE IN RABBIT

作　　者：朱卡琳[1] 汤谷平[1] 陈启琪[1] 张晓东 周淑青 

机构地区：[1]浙江医科大学药学系

出　　处：《药学学报》1998年第12期906-909,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：以５氟尿嘧啶为模型药物，将药物以共价键的形式键合于生物降解型高分子材料聚α，β（２羟乙基）ＤＬ天冬酰胺上制成高分子载体药物，药物接入率达３７１％（ｗ／ｗ）。用红外和差热分析法对载体药物进行了表征。以纯种大白兔为实验动物，把载体药物制成混悬型和棒状型两种剂型，进行药物体内释放实验。结果表明：以棒状型药物给药在一定程度上可以降低释药初期的“爆释”现象，为进一步临床应用提供了重要依据。A polymer release drug was prepared by poly α,β (2 hydroxyethyl) DL asparamide(PHEA) and 5 fluorouracil. As a model drug 5 fluorouracil was conjugated into the biodegradable polymer by chemical bond. The released drug was determined to be about 37 1% ( w/w ) and it was characterized by IR spectrum and differential scanning calorimetry (DSC). Two forms of drugs, rod and suspension were prepared and in vivo release experiment were carried out in rabbits. The experimental result showed that the rod form of drug can in some degree reduce initial burst.

关 键 词：氟尿嘧啶 天冬酰胺 体内释放 合成 高分子载体 

分 类 号：TQ463.54[化学工程—制药化工] TQ463.26