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  

Carboxylated 3D ordered macroporous carbon for improvement of the dissolution rate of 10-hydroxycamptothecin

作　　者：王和禹[1] 刚晶[1] 高清河[1] 

机构地区：[1]辽宁中医药大学信息工程学院,辽宁沈阳110847

出　　处：《沈阳药科大学学报》2015年第8期593-597,共5页Journal of Shenyang Pharmaceutical University

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。Objective To prepare carboxylated 3DOM carbon and improve the dissolution of hydroxycampto- thecin. Methods 3 DOM carbon was prepared on the hard-temple method and characterized by SEM. Carbox- ylation was conducted by surface oxidation. The carriers were tested by IR and their Zeta potentials were measured. Drug was loaded on solvent-evaporating method. The drug loading and dispersibility of the drug loaded systems were tested. DSC was used to study the state of drug in carders. The release profiles of the raw drug and the drug loaded in carriers were investigated. Results The prepared 3DOM carbon had a 3D structure with interconnected pores. The diameters of the outer pores and inner pores were 500 nm and 200 nm respectively. The Zeta potential of carboxylated 3DOM carbon reduced to - 16 mV, and an obvious peak could be seen in its IR spectrum. The drug loading was about 24% （w） and the dispersibility of the car- boxylated carrier in water was improved dramatically. The melting peak of crystalline drug was weakened in the DSC spectrum of drug-loaded carboxylated carder. The accumulated release of raw drug in 1 h was only 24. 7%, while the accumulated release of the drug in carboxylated carder rose to 83.6% . Conclusions Tak- ing advantage of the unique structural features and improved dispersibility in water, the prepared carboxyla- ted 3DOM carbon could improve the dissolution of hydroxycamptothecin markedly.

关 键 词：三维有序大孔炭 羟基喜树碱 溶出 羧基化 

分 类 号：R94[医药卫生—药剂学]