摘要
目的合成肿瘤靶向药物透明质酸氟尿嘧啶耦联物,并探讨最佳合成条件。方法①以透明质酸(HA)和5-氟尿嘧啶(5-FU)为原料,将5-FU通过4位上的氨基与HA片段上的羧基耦合,得到HA-FU耦联物,测定其产物的紫外光谱。②以HA-FU耦联产物量作为指标,考察反应试剂加入的顺序、反应温度、溶液pH等多个水平,并从中选出最佳实验条件。结果制备HA-FU耦联物的最佳条件是将5-FU滴入HA中,温度为20-30℃,pH为3～4。合成了透明质酸与5-氟尿嘧啶耦合物,呈乳白色粉末。结论通过实验研究,找到合成透明质酸氟脲嘧啶的最佳合成条件。
OBJECTIVE To synthesize a tumor targeting drug 5-fluorouracil coupling of hyaluronic acid,and explore the best of conditions.METHODS ①To hyaluronic acid（HA）and 5-fluorouracil（5-FU）as raw materials,the amidogen of 5-FU couples with the carboxyl of the HA,and then measure the ultraviolet spectrum.②As a product of indicators of coupled with HA-FU,we study the reaction reagents of joining order,temperature,the pH and so on to choose the best experimental conditions.RESULTS The best conditions of preparing HA-FU coupling is puthing 5-FU titrating into HA,and the temperature is 20～30 ℃,pH is 3～4.The production of the hyaluronic acid and 5-fluorouracil conjugate is milky white powder.CONCLUSION Through experimental research,we find the best synthesis condition of hyaluronic acid-fluorouracil.
出处
《海峡药学》
2011年第2期13-16,共4页
Strait Pharmaceutical Journal
