文档介绍：去羟肌苷脂质前药药质体的稳定性研究
辛瑞1,2 ,于善江3,金义光1,2作者简介:辛瑞,女,河南开封人,在读硕士, Tel:010-66931220,E-mail:2004xiaorui@
﹡通讯作者: 金义光,男,河南清丰人,副研究员,博士,硕士生导师,主要从事新型药物传递系统的研究,Tel:010-66931220,E-mail:jinyg@
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,北京 100850;,开封 475004;,北京 100081
摘要:目的制备胆固醇基己二酰去羟肌苷(CAD)药质体,考察其物理和化学稳定性。方法用合成的CAD通过四氢呋喃注入法制备药质体,透射电子显微镜和激光粒度分析仪观察其形态和粒径,加热、离心和室温长期放置考察药质体的物理稳定性,HPLC测定药质体在缓冲液、猪肝酯酶、大鼠血浆和肝中的化学稳定性。结果 CAD药质体是类球形囊泡,平均粒径122nm;物理稳定性良好,在上述化学环境中的降解速率较慢,肝中半衰期为23h,降解产物不完全为ddI。结论CAD药质体在生物环境中的降解产物为ddI,可作为抗HIV药物的新型给药系统。
关键词:药剂学;稳定性;去羟肌苷;药质体;自组装
中图分类号:R94 文献标识码:A 文章编号:
The Stability of Pharmacosomes Prepared from Didanosine Lipophilic Prodrug
XIN Rui1,2 , YU Shan-Jiang3, JIN Yi-Guang1,2*
1 Department of Pharmaceutical Chemistry, Beijing Institute of Radiation Medicine, Beijing 100850 ,China; 2 Pharmaceutical College of Henan University, Kaifeng, 475004,China; 3 China National Center for Biotechnology Development, Beijing 100081,China
Abstract: Objective The pharmacosomes of cholesteryl-adipoyl didanosine (CAD) were prepared and investigated on physical and chemical stability. Methods The pharmacosomes were prepared from the previously synthesized lipophilic prodrug of didanosine (CAD) using the THF injection method. The morphology and particle size of pharmacosomes were explored using TEM and laser particle analyzer. The effects of heat, centrifugation and storage on the physical stabi