齐多夫定脂质前药自组装体的制备及其在大鼠血浆中的稳定性  

Self-assemblies of zidovudine lipid prodrugs:preparation and stability in rat plasma

作　　者：邢磊[1] 金义光[1] 陈洪轩[2] 杜丽娜[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850 [2]河南大学药学院,河南开封475004

出　　处：《国际药学研究杂志》2008年第3期161-164,共4页Journal of International Pharmaceutical Research

基　　金：国家自然科学基金资助项目(No.30371700)

摘　　要：目的制备齐多夫定脂质前药自组装体,考察其在大鼠血浆中的稳定性。方法用乙醇注入法制备齐多夫定脂质前药自组装体,透射电子显微镜和激光粒度测定仪观测其形态和粒度,高效液相色谱法测定齐多夫定脂质前药自组装体在大鼠血浆中降解情况。结果齐多夫定脂质前药自组装体是球形囊泡,平均粒径为200nm;在大鼠血浆中降解半衰期为3.68h,降解产物为齐多夫定。结论齐多夫定脂质前药自组装体在体外生物环境中能较快地降解出原药。Objective To prepare self-assemblies of zidovudine （AZT） lipid prodrugs and investigate the in vitro stability in rat plasma. Methods Self-assemblies of AZT lipid prodrugs were prepared by an ethanol injection method. Morphology was observed by transmission electron microscope and particle size was measured by laser particle analyzer. Degradation of the self-assemblies of AZT lipid prodrugs in rat plasma was investigated by high performance liquid chromatography （ HPLC ）. Results Self-assemblies of AZT lipid prodrugs were spherical vesicles whose mean particle size was about 200 nm. t1/2 of the prodrugs in rat plasma was 3.68 h and the degradation product of the prodrugs was AZT. Conclusion Self- assemblies of AZT lipid prodrugs degrade into AZT rapidly in rat plasma.

关 键 词：齐多夫定 脂质前药 自组装 血浆 药物稳定性 

分 类 号：R94[医药卫生—药剂学] R96[医药卫生—药学]