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 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.
Char
H
H
Pharmaceutical Research and Development, Hoffmann-La Roche Inc., Nutley, NJ 07110.
Kumar
S
S
Patel
S
S
Piemontese
D
D
Iqbal
K
K
Malick
A W
AW
Salvador
R A
RA
Behl
C R
CR
D000042:Absorption; D000281:Administration, Intranasal; D000818:Animals; D001682:Biological Availability; D001921:Brain / Q000378:metabolism*; D002250:Carbon Radioisotopes; D003915:Dextromethorphan / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
D002250:Carbon Radioisotopes; D003915:Dextromethorphan