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三甲基壳聚糖-维生素B₁₂偶联物的制备与表征

Preparation and characterization of N-trimethyl chitosan-Vitamin B₁₂ conjugates

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【Author】 KE Zhi-yang1,CHENG Gang2,ZHU Xi1,HE Shuang1,LEI Ying2,HE Bin2,HUANG Yuan1(1.Key Laboratory of Drug Targeting and Drug Delivery,Ministry of Education,West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China;2.National Engineering Research Center for Biomaterials,Sichuan University,Chengdu,Sichuan,610064 P.R.China)

【机构】四川大学华西药学院靶向药物与释药系统教育部重点实验室；四川大学国家生物医学材料工程技术研究中心；

【摘要】目的合成两种具有肠上皮细胞靶向的三甲基壳聚糖-Vit B12偶联物,并测定Vit B12的修饰度。方法分别以丁二酸和PEG2000为间隔基制备三甲基壳聚糖-Vit B12偶联物。结果与结论合成了两种不同间隔基的三甲基壳聚糖-Vit B12偶联物;目标偶联物及重要中间体经1HNMR、MS和UV确证;两种偶联物中Vit B12的修饰度分别为3.3%、3.1%。更多还原

【Abstract】 OBJECTIVE To synthesize two kinds of intestinal epithelial cells targeting N-trimethyl chitosan-Vit B12 conjugates and determine the level of Vit B12 substitution on the conjugates.METHODS Vit B12 was conjugated with N-trimethyl chitosan via two kinds of spacers:succinic acid and PEG2000.RESULTS and CONCLUSION Two kinds of N-trimethyl chitosan-Vit B12 conjugates were successfully synthesized.The chemical structures of the target conjugations and intermidiates were characterized by 1HNMR,MS and UV.The degree of Vit B12 substitution on the conjugations were 3.3% and 3.1%,respectively.更多还原