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Tissue Distribution and Pharmacodynamics of Rivastigmine after Intranasal and Intravenous Administration in Rats
Yang, Zhen-zhen1; Zhang, Yan-qing2; Wu, Kai1; Wang, Zhan-zhang1; Qi, Xian-rong1
关键词Acetylcholinesterase Alzheimer&prime s disease brain delivery butyrylcholinesterase intranasal administration rivastigmine
刊名CURRENT ALZHEIMER RESEARCH
2012-03-01
9期:3页:315-325
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Clinical Neurology ; Neurosciences
资助者National Basic Research Program of China (973 Program) ; National Basic Research Program of China (973 Program)
研究领域[WOS]Neurosciences & Neurology
关键词[WOS]CENTRAL-NERVOUS-SYSTEM ; ALZHEIMERS-DISEASE ; ACETYLCHOLINESTERASE INHIBITION ; BRAIN ACETYLCHOLINE ; CEREBROSPINAL-FLUID ; DRUG-DELIVERY ; CHOLINESTERASE ; DONEPEZIL ; DOPAMINE
英文摘要

The aim of the study was mainly to investigate the relationship between concentration of rivastigmine and its inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) following intranasal (IN) and intravenous (IV) administration in rats, and to provide a novel nasal delivery route for the brain disease therapy. Rivastigmine was administered to male rats at 2 mg/kg by IN and IV route. Drug concentration, AChE and BuChE activity were measured in the plasma, central nervous system (CNS) regions i.e. olfactory region, hippocampus, cerebrum and cerebellum, and peripheral tissues. It was determined that rivastigmine was characterized by extremely rapid and complete absorption into the systemic circulation followed by a rapid decline in the plasma concentrations, and can also quickly distribute into CNS and peripheral tissues by the two routes. IN administration showed higher concentration in CNS regions and longer action on inhibiting the activity of AChE and BuChE than IV administration. More significant decrease of the two enzymes was observed in CNS regions than in peripheral tissues for both administrations. A close relationship was found between the concentration of rivastigmine and enzyme inhibition in plasma and CNS tissues in rats. Based on these findings, it was concluded that rivastigmine could cause relatively strong inhibition of AChE and BuChE in plasma and brain tissues, especially in hippocampus, cortex and cerebrum. The pharmacodynamics was closely related to its concentration in vivo. The intranasal route can be strategy for delivering the drug into brain.

语种英语
所属项目编号2007CB935801 ; 2009CB930300
资助者National Basic Research Program of China (973 Program) ; National Basic Research Program of China (973 Program)
WOS记录号WOS:000304008800006
引用统计
被引频次:10[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/60138
专题北京大学药学院
作者单位1.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Tianjin Univ Commerce, Dept Pharmaceut Engn, Tianjin 300134, Peoples R China
推荐引用方式
GB/T 7714
Yang, Zhen-zhen,Zhang, Yan-qing,Wu, Kai,et al. Tissue Distribution and Pharmacodynamics of Rivastigmine after Intranasal and Intravenous Administration in Rats[J]. CURRENT ALZHEIMER RESEARCH,2012,9(3):315-325.
APA Yang, Zhen-zhen,Zhang, Yan-qing,Wu, Kai,Wang, Zhan-zhang,&Qi, Xian-rong.(2012).Tissue Distribution and Pharmacodynamics of Rivastigmine after Intranasal and Intravenous Administration in Rats.CURRENT ALZHEIMER RESEARCH,9(3),315-325.
MLA Yang, Zhen-zhen,et al."Tissue Distribution and Pharmacodynamics of Rivastigmine after Intranasal and Intravenous Administration in Rats".CURRENT ALZHEIMER RESEARCH 9.3(2012):315-325.
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