肝靶向前药胆酸拉米夫定酰胺的合成及其稳定性初步研究  

Synthesis and stability of bile acid conjugate lamivudine as a liver target prodrug

作　　者：胡平[1] 侯世祥[1] 金辉[1] 张继芬[1] 王立[1] 

机构地区：[1]四川大学华西药学院中药制剂研究室,成都610041

出　　处：《中南药学》2005年第1期13-15,共3页Central South Pharmacy

摘　　要：目的　设计合成具有人体胆酸转运体结合活性的肝靶向前体药物。方法　运用活泼酯法原理, 设计合成新化合物胆酸拉米夫定酰胺, 使用1H NMR、13 C NMR、IR、MS确认其结构, 并对其稳定性进行初步研究。结果　合成了目标产物, 初步稳定性结果显示其在各种溶剂中较稳定。结论　得到了稳定的目标化合物胆酸 拉米夫定酰胺,为进一步体内肝脏靶向性研究奠定了基础。OBJECTIVE To design and synthesize a liver target lamivudine prodrug that would utilizes the human apical sodium dependent bile acid transporter and enhance lamivudine oral bioavailability METHODS Using deoxy cholate and lamivudine,the new prodrug was designed and synthesized,and the structure of the compound was determined by elemental analysis,IR, 1H NMR, 13 C NMR and MS RESULTS The ideal compound was synthesized,and its methods of concentration testing by UV and HPLC were established and it was stable in several resolves CONCLUSIONS The conjugate is stable in several resolves Stable bile acid lamivudine conjugate is obtained to ensure the further liver target study in vivo

关 键 词：前药 合成 胆酸转运体 拉米夫定 去氧胆酸 

分 类 号：R978.7[医药卫生—药品] R927.11[医药卫生—药学]