鼻内给予乙酰胆碱酯酶抑制剂。
Intranasal administration of acetylcholinesterase inhibitors.
作者信息
Costantino Henry R, Leonard Alexis Kays, Brandt Gordon, Johnson Paul H, Quay Steven C
机构信息
Nastech Pharmaceutical Company Inc, 3830 Monte Villa Parkway, Bothell, WA 98021, USA.
出版信息
BMC Neurosci. 2008 Dec 10;9 Suppl 3(Suppl 3):S6. doi: 10.1186/1471-2202-9-S3-S6.
Abstract
This short review outlines the rationale, challenges, and opportunities for intranasal acetylcholinesterases, in particular galantamine. An in vitro screening model facilitated the development of a therapeutically viable formulation. In vivo testing confirmed achievement of therapeutically relevant drug levels that matched or exceeded those for oral dosing, with a dramatic reduction in undesired emetic responses. Intranasal drug delivery is an effective option for the treatment of Alzheimer's disease and other central nervous system disorders.
摘要
这篇简短的综述概述了鼻内给予乙酰胆碱酯酶，尤其是加兰他敏的基本原理、挑战和机遇。体外筛选模型推动了一种具有治疗可行性的制剂的研发。体内试验证实达到了与口服给药相当或更高的治疗相关药物水平，且意外的催吐反应显著减少。鼻内给药是治疗阿尔茨海默病和其他中枢神经系统疾病的有效选择。
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本文引用的文献
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2
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J Clin Psychiatry. 2006 Nov;67(11):1784-800. doi: 10.4088/jcp.v67n1118.
3
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4
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J Nutr Health Aging. 2006 Sep-Oct;10(5):417-29.
5
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Brain. 2006 Nov;129(Pt 11):2840-55. doi: 10.1093/brain/awl280. Epub 2006 Oct 3.
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