透明质酸接枝双氯芬酸的制备、表征和体外释放  

Preparation,characterization and in vitro release of diclofenac grafted with hyaluronic acid

作　　者：宋琳琪 郑枫[1] SONG Linqi;ZHENG Feng(School of Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学药学院,南京211198

出　　处：《中国药科大学学报》2025年第1期49-55,共7页Journal of China Pharmaceutical University

摘　　要：参照原研药双氯芬酸透明质酸钠(DF-HA)采用共价键合的方式合成了一种DF-HA接枝共聚物。通过核磁共振氢谱、紫外分光光度法、傅里叶变换红外光谱对其进行了结构表征,结果显示DF-HA成功合成,同时1H NMR和紫外分光光度法确定其接枝率约为17%。利用HPLC对DF-HA接枝共聚物进行了体外释放研究,考察其在磷酸缓冲盐溶液(pH 7.4)中对双氯芬酸(DF)的释放情况。游离DF在6h后药物释放率达到83.6%,DF-HA在1d内的释放率为4.8%,在21d内的释放率为17.7%,与参比制剂释放行为基本一致,DF-HA能显著实现对DF的缓释效果,且高分子量透明质酸本身具有治疗骨关节炎的作用,DF-HA可以结合两者的优点,具有较好的应用价值。In reference to the original drug diclofenac etalhyaluronate sodium(DF-HA),a graft copolymer was synthesized by covalent bonding.The structure of DF-HA was characterized by 1H NMR,UV-Vis spectrophotometry and FT-IR.The results showed that DF-HA was successfully synthesized,and the grafting rate was determined to be approximately 17%by 1H NMR and UV-Vis spectrophotometry.The in vitro release of DFHA graft copolymer was studied by HPLC,and its release of diclofenac(DF)in phosphate buffered saline(PBS,pH 7.4)was investigated.The drug release rate of free DF was 83.6% after 6 h,and that of DF-HA was 4.8% within 1 d and 17.7% within 21 d,which were basically consistent with the release behavior of the reference listed drug.DF-HA could significantly achieve the sustained release of DF,and high molecular weight hyaluronic acid itself had the effect of treating osteoarthritis.With both advantages,DF-HA could have good application value.

关 键 词：透明质酸 双氯芬酸钠 接枝共聚物 表征 体外释放 

分 类 号：R917[医药卫生—药物分析学]