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大鼠鼻腔给予盐酸右美沙芬[¹⁴C]的血浆和脑内浓度

Nasal delivery of [14C]dextromethorphan hydrochloride in rats: levels in plasma and brain.

作者信息

Char H, Kumar S, Patel S, Piemontese D, Iqbal K, Malick A W, Salvador R A, Behl C R

机构信息

Pharmaceutical Research and Development, Hoffmann-La Roche Inc., Nutley, NJ 07110.

出版信息

J Pharm Sci. 1992 Aug;81(8):750-2. doi: 10.1002/jps.2600810806.

Abstract

Dextromethorphan (DM) is a neuroprotective agent. The mechanism of action is believed to be by N-methyl-D-aspartate receptor blockade. The concentration of DM in the brain is believed to be dose and route dependent. Delivery by the nasal route has received a lot of attention recently, because drug absorption from this route follows intravenous profiles with no first-pass effect. The uptake of DM in the brain from the nasal route was 65.9% compared with the intravenous route, whereas the plasma bioavailability from the nasal route was 78.8%. The nasal route is a viable alternative to the parenteral route for DM administration.

摘要

右美沙芬(DM)是一种神经保护剂。其作用机制被认为是通过阻断N-甲基-D-天冬氨酸受体。据信,DM在大脑中的浓度取决于剂量和给药途径。经鼻给药途径最近受到了广泛关注,因为该途径的药物吸收呈现静脉给药特征且无首过效应。与静脉给药途径相比,经鼻途径给药后DM在大脑中的摄取率为65.9%,而经鼻途径给药后的血浆生物利用度为78.8%。经鼻给药途径是DM给药替代胃肠外给药途径的一种可行选择。

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