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３７１％（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.
出处
《药学学报》
CAS
CSCD
北大核心
1998年第12期906-909,共4页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
氟尿嘧啶
天冬酰胺
体内释放
合成
高分子载体
Fluorouracil
Poly α,β(hydroxyalkyl) DL asparamide
In vivo release
Initial burst
