含5-氟尿嘧啶的聚乙二醇酯的制备与表征

Synthesis and characterize of 5-fluorouracil and polyethylene glycol conjugate

采用氯乙酸与不同分子量的聚乙二醇进行酯化反应得到氯乙酸聚乙二醇酯,由于酯中的α-氯具有良好的反应活性,将它再与抗癌药物5-氟尿嘧啶结合制备了不同分子量的高分子前药,并对得到的产物进行表征。产物的体外降解实验表明,该产物具有长效缓释的功效,其中(PEG 2000)-5-FU的载药量为18.6%,随着聚乙二醇分子量的增加,产物水溶性提高,当聚乙二醇相对分子质量为2000时水解速率最大。

A series of novel polyethylene glycol derivates was synthesized by esterification of chloroacetic acid with polyethylene glycol. Because of the good reactive activity of a-chlorin in the esters it can react with 5-fluorouracil, thus the conjugate can be obtained. The conjugate is characterized by IR, ^1H-NMR and UV spectroscopy and it shows a longer duration of activity due to the slow release. The loading content of the （PEG 2000）-5-FU conjugate was 18.6%, and as the molecular weight of polyethylene glycol heightens, the water-solubility was enhanced. When the molecular weight reaches 2000, the hydrolyzation speed is the fastest.