β-细辛醚微乳鼻腔给药脑内靶向性评价  

Evaluation of brain-targeting of β-asarone microemulsion by intranasal administration

作　　者：张龙开[1] 许日鑫[1] 蒋梅[1] 严慕贤[1] 陈志辉[1] 欧斯健[1] 魏刚[1] 

机构地区：[1]广州中医药大学新药开发研究中心,广东广州510006

出　　处：《中草药》2014年第1期86-89,共4页Chinese Traditional and Herbal Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09103-429)

摘　　要：目的探索β-细辛醚微乳利用鼻腔的鼻-脑通道实现鼻脑靶向给药的可行性。方法按0.42 mL/kg剂量鼻腔给予β-细辛醚微乳后用HPLC法测定药物在血浆中及脑中的浓度,并以iv自制微乳注射液为对照,以AUC脑/AUC血浆指标考察β-细辛醚微乳鼻腔给药的脑靶向性。结果β-细辛醚微乳鼻腔给药后得到的AUC脑/AUC血浆值均高于iv给药。结论鼻腔给予含药微乳系统后脑靶向性良好,有望成为治疗阿尔茨海默病的新型给药途径。Objective To explore the feasibility of brain-targeting intranasal administration with β-asarone microemulsion by nose-brain pathway. Methods The concentration ofβ-asarone in plasma and brain following nasal administration of β-asarone microemulsion （0.42 mL/kg） was measured by HPLC, taking the iv administration of self microemulsion injection as control. And the brain-targeting was evaluated by ratio of AUCbrain/AUCplasma. Results The ratio of AUCbrain/AUCplasrna obtained after intranasal administration was significantly higher than that after iv administration. Condusion The brain-targeting of β-asarone is better after intranasal administration which could become a new drug delivery system for the treatment of Alzheimer＇s disease.

关 键 词：Β-细辛醚 微乳 鼻腔给药 脑靶向 阿尔茨海默病 

分 类 号：R285.5[医药卫生—中药学]