布洛芬-偕二膦酸偶联物的合成及体外靶向性研究  

Synthesis of Ibuprofen-gem-bisphosphonate and study of targeting in vitro

作　　者：程铃[1] 钱珊[1] 樊维[1] 吴勇[1] 海俐[1] 

机构地区：[1]四川大学华西药学院,成都610041

出　　处：《四川大学学报（自然科学版）》2011年第4期891-894,共4页Journal of Sichuan University(Natural Science Edition)

摘　　要：以偕二磷酸为骨靶向载体，设计并合成了一个新型的骨靶向抗炎药布洛芬一偕二磷酸偶联物L，该化合物将抗炎药布洛芬通过酯键与偕二磷酸偶联，其结构经^1HNMR、IR和MS确证，体外吸附性实验显示目标化合物能与羟磷灰石晶体（HPA）发生良好结合，初步验证了其体外骨靶向性．Using gem-bisphosphonate as bone-targeting carrier, we designed and synthesized a new bone targeting anti-inflammatory drugs, Ibuprofen-gem-bisphosphonate conjugation, in which ibuprofen conjugated with gem-bisphosphonate by ester linkage. The chemical structure of the title compound was confirmed by IR, 1 HNMR and MS. The absorption experiment in vitro showed the target compound can efficiently bond with hydroxyapatite （HPA） that proved the good bone targeting of title compound.

关 键 词：抗炎药 布洛芬-偕二磷酸偶联物 骨靶向 合成 

分 类 号：R978[医药卫生—药品]