羟基喜树碱-聚乙二醇固体分散体的稳定性  

Stabilization of solid dispersions of 10-hydroxycampothecin in polyethylene glycol

作　　者：严鸿飞[1] 蒋国强[1] 孙佳丽[1] 丁富新[1] 

机构地区：[1]清华大学化学工程系,北京100084

出　　处：《清华大学学报（自然科学版）》2008年第12期2126-2129,共4页Journal of Tsinghua University(Science and Technology)

基　　金：国家自然科学基金资助项目(20576057);北京市科技计划项目(GYYKW05070002)

摘　　要：为提高难溶药物羟基喜树碱(HCPT)的溶出度,研究了以聚乙二醇(PET)为载体的HCPT-PET固体分散体的稳定性。采用溶剂-熔融法制备了HCPT-PEG固体分散体。在相对湿度75%、温度25℃下,测定了溶出度、吸湿增重和晶体形态。结果表明:HCPT在快速冷却时以无定型态,缓慢冷却时以微晶态存在于载体中。相对分子质量6 000的PEG 6000的固体分散体的稳定性,比PEG 2000更好;高的载体/药物质量比也可提高稳定性。The solid dispersion stability of 10-hydroxycampothecin （HCPT）, a drug with low dissolution, in polyethylene glycol （PEG） was investigated to improve the HCPT water solubility. The melting solvent method was used to prepare the HCPT-PEG solid dispersion. The dissolution, bygroscope, and crystallinity were measured for a the humidity of 75% at 25℃. The results show that fast cooling rates during preparation result in amorphous HCPT in the solid dispersion while normal cooling rates lead to crystalline HCPT in the solid dispersion. The carrier PEG 6000, with a relative molecular mass of 6 000, provides better solid dispersion stabilization than PEG 2000. High carrier-drug mass ratio can improve HCPT-PEG stability.

关 键 词：固体分散体 羟基喜树碱 溶出度 稳定性 

分 类 号：R944[医药卫生—药剂学]