5-氟尿嘧啶-花生凝集素结合物的反应条件优化及性质研究  

Optimization of the Preparation and the Properties of Conjugate of 5-Fluorouracil and Peanut Agglutinin

作　　者：蔡勤[1] 张志荣[1] 

机构地区：[1]四川大学华西药学院药剂学教研室,成都610041

出　　处：《四川大学学报（医学版）》2005年第3期408-410,共3页Journal of Sichuan University(Medical Sciences)

基　　金：国家杰出青年科学基金 (批准号 3 992 5 0 3 9)资助

摘　　要：目的　优化5 -氟尿嘧啶(5 - Fu) -花生凝集素(PNA)结合物的反应条件,以期制备得到既有生物活性又有较高药物结合率的结合物。方法　采用单因素法优化反应条件,考察结合物稳定性,以药物结合率和体外活性为判断指标。结果　以优化条件:5 - Fu∶EDC∶NHS=1∶5∶2 ,D-半乳糖∶PNA (w/ w) =2 .5∶1,连接反应时间12 h制备得到了既有生物活性又有较高药物结合率的结合物。结论　D-半乳糖能保护花生凝集素的活性中心,在D-半乳糖保护下可以制备出既有生物活性又有较高药物结合率的结合物。结合物性质比较稳定。Objective This study was aimed at optimizing the preparation of 5-Fluorouracil and peanut agglutinin conjugates so as to obtain a conjugate with high activity and high drug ratio, and to choose a suitable dosage form in the light of its properties. Methods Every single factor was tested. The drug ratio and activity were chosen according to the criteria for judgement. The stability of the conjugate was tested after treatment. Results A conjugate with high activity and drug ratio was obtained under the condition of 5-Fu∶EDC∶NHS= 1∶5∶2 for 12 h with the protection of D-galactose〔D-galactose∶PNA(w/w)=2.5∶1〕. Conclusion The addition of D-galactose could protect the activity of PNA. The conjugate is stable.

关 键 词：5-氟尿嘧啶-花生凝集素结合物 D-半乳糖 稳定性 

分 类 号：TQ460.1[化学工程—制药化工]