摘要
用氰基丙烯酸正丁酯制备了毫微型胶囊——抗癌药物新剂型。以5-氟尿嘧啶为模型药物所制得的毫微囊最大粒子直径为338nm。建立了凝胶色谱法测定包封率的新方法,5-氟尿嘧啶的包封率达40.9%。通过小鼠尾静脉注射,测得氰基丙烯酸正丁酯的LD_(50_=267.7 mg/kg。制成毫微囊后,5-氟尿嘧啶对S_(180),Hep S以及EAC的抗癌活性明显提高。
In this study, a new dosage form for antitumor agents—— nanocapsules was prepared from biodegradable butylcyanoacrylate (BCA). Using 5- fluorouracil (5-Fu )as the model drug, scanning electron microscope pictrues show that the maximun diameter of nanocapsules particles is about 338 nm. A new gel chromatography method is established for the determination of encapsulation efficiency in nanocapsules. The encapsulation efficiency of 5 - Fu is 40.9%. LD_(50) of BCA is 267.7 mg/kg for intravenous injection in mice. The antitumor activities of 5- Fu nanocapsules on S_(180), HepS and EAC were found to be higher than that of free 5- Fu.
出处
《药学学报》
CAS
CSCD
北大核心
1991年第4期280-285,共6页
Acta Pharmaceutica Sinica
关键词
氟尿嘧啶
毫微型胶囊
抗癌活性
5-Fluorouracil
Nanocapsules
Butylcyanoacrylate
Antitumor activities
