[关键词]
[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。
[Key word]
[Abstract]
Objective To explore the feasibility of brain-targeting intranasal administration with β-asarone microemulsion by nose-brain pathway. Methods The concentration of β-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/AUCplasma obtained after intranasal administration was significantly higher than that after iv administration. Conclusion 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.
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[基金项目]
国家“重大新药创制”科技重大专项(2009ZX09103-429)