Nasal Delivery of [14C]Dextromethorphan Hydrochloride in Rats: Levels in Plasma and Brain

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 a...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1992-08, Vol.81 (8), p.750-752
Main Authors: Charx, Hing, Kumar, Saran, Patel, Sunil, Piemontese, David, Iqbal, Khurshid, Malick, A. Waseem, Salvador, Richard A., Behl, Charan R.
Format: Article
Language:English
Subjects:
Absorption
Administration, Intranasal
Animals
Biological and medical sciences
Biological Availability
Brain - metabolism
Carbon Radioisotopes
Dextromethorphan - administration & dosage
Dextromethorphan - blood
Dextromethorphan - pharmacokinetics
Injections, Intravenous
Male
Medical sciences
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
Respiratory system
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Summary: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.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600810806