核黄素衍生物的合成及其光交联明胶的应用研究

Synthesis of Riboflavin Derivatives and Their Application in Photo-Cross-Linked Gelatin

通过化学合成的方法获得了具有不同化学基团修饰的核黄素衍生物,衍生物的结构中均保留了与核黄素相同的光激发响应基团,并且分别作为光敏剂实现了光诱导明胶交联,验证了核黄素光诱导交联明胶的作用机理。考察了所得交联明胶膜的机械性能,优选水溶性核黄素为光敏剂,使得明胶在载药蒙脱土微粒表面光诱导原位交联,从而实现对微粒的包覆制粒。包覆后的蒙脱土微粒流动性更好,堆密度大,更适合作为制剂粉体进行加工,而且对模型药物(阿奇霉素)具有一定的掩味效果,体现了用交联明胶包覆载药蒙脱土微粒的优势。

Riboflavin derivatives with different group modifications were obtained by chemical synthesis method,in which the structures of the synthesized compounds have the same photo-excitation response group as riboflavin.These compounds acted as photosensitizers,respectively,to carry out the photocross-linked procedure of gelatin,which verified the same mechanism as riboflavin.The mechanical properties of the cross-linked gelatin film were investigated,and hydrophilic riboflavin derivatives were selected as the photosensitizers to make the gelatin in situ photocross-linked on the surface of drug-loaded montmorillonite particles,so as to realize the encapsulation and granulation of the particles.The coated montmorillonite particles have better fluidity,higher bulk density,which are more suitable for processing as preparation powder.Moreover,the coated montmorillonite particles have certain flavor masking effect on the model drug azithromycin,which reflecting the advantages of using cross-linked gelatin to coat the drug-loaded montmorillonite particles.