羧基化三维有序大孔炭载体用于提高羟基喜树碱的溶出度

发布时间：2018-11-20 04:36

【摘要】：目的制备羧基化三维有序大孔炭载体,提高水难溶性药物羟基喜树碱的溶出度。方法采用硬模板法制备三维有序大孔炭载体,以扫描电子显微镜(scanning electron microscopy,SEM)进行表征。采用表面氧化法进行羧基化修饰,对修饰前后的载体进行IR表征及Zeta电位测定。采用溶剂挥发法载药,测定载药量并对载药体系的水分散性进行考察。以DSC考察药物于载体中的存在状态,对原料药及羧基化修饰前后的载药体系的药物溶出度进行测定。结果制得的三维有序大孔炭载体孔道呈互相连通的三维结构,外孔孔径为500nm,内孔孔径为200nm。羧基化修饰后载体的Zeta电位显著降至-16mV,IR谱图中可见明显的羧基吸收峰。羟基喜树碱的载药量质量分数约为24%,羧基化修饰的载药体系水分散性显著提高,DSC显示其中所载药物的结晶峰明显减弱。原料药1h累计释放度仅为24.7%,羧基化修饰的载药体系药物累计释放度升至83.6%。结论制备的羧基化三维有序大孔炭载体可利用其独特的结构特征及改善的水分散性显著提高羟基喜树碱的溶出度。
[Abstract]:Objective to prepare carboxylation three dimensional ordered macroporous carbon carrier and improve the dissolution of hydroxy camptothecin. Methods three dimensional ordered macroporous carbon carriers were prepared by hard template method and characterized by scanning electron microscopy (scanning electron microscopy,SEM). Carboxylation modification was carried out by surface oxidation method. The carrier before and after modification was characterized by IR and Zeta potential was measured. The solvent volatilization method was used to determine the amount of drug loaded and the water dispersion of the drug loading system was investigated. The drug dissolution of the drug carrier system before and after carboxylation modification was determined by DSC. Results the three dimensional ordered macroporous carbon carrier channels were interlinked with each other with an external pore diameter of 500 nm and an internal pore diameter of 200 nm. After carboxylation modification, the Zeta potential of the carrier decreased significantly to -16mV ~ (-1) IR spectrum with obvious carboxyl absorption peak. The mass fraction of hydroxy camptothecin was about 24%, the water dispersion of carboxylated modified drug carrier system was improved significantly, and the crystallization peak of the drug was obviously weakened by DSC. The cumulative release rate was only 24.7in 1 h, and the cumulative release rate of carboxylated drug delivery system increased to 83.6%. Conclusion the carboxylated three-dimensional ordered macroporous carbon carrier can significantly improve the dissolution of hydroxycamptothecin with its unique structural characteristics and improved water dispersion.
【作者单位】：辽宁中医药大学信息工程学院;
【分类号】：R943

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