Document Detail


Permeation and systemic absorption of R- and S-baclofen across the nasal mucosa.
MedLine Citation:
PMID:  21283988     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Baclofen, an antispasmodic agent that acts as a GABA(B) agonist, resembles phenylalanine in structure and has been reported to be a substrate of the large amino acid transporter 1 (LAT-1). The objective of this study was to investigate the absorption of baclofen across the nasal mucosa both in vitro and in vivo. Baclofen transport was measured across excised bovine olfactory and respiratory mucosae to investigate site-specific uptake of baclofen, and the intranasal bioavailability of R- and S-baclofen was determined in rats. Increasing flux with increasing baclofen donor concentration and the absence of polarized transport was observed in vitro, and similar distribution profiles were observed for both enantiomers following intranasal administration in rats. The absence of stereospecificity in nasal absorption indicates limited involvement of the amino acid or other transporters in the nasal absorption of baclofen.
Authors:
Hefei Zhang; Mark Schmidt; Daryl J Murry; Maureen D Donovan
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, N.I.H., Extramural     Date:  2011-01-31
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  100     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2011 Jul 
Date Detail:
Created Date:  2011-05-06     Completed Date:  2011-09-12     Revised Date:  2012-10-09    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2717-23     Citation Subset:  IM    
Copyright Information:
Copyright © 2011 Wiley-Liss, Inc. and the American Pharmacists Association
Affiliation:
Division of Pharmaceutics and Translational Therapeutics, College of Pharmacy, University of Iowa, Iowa City, Iowa 52242, USA.
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MeSH Terms
Descriptor/Qualifier:
Absorption
Administration, Intranasal
Animals
Baclofen / blood,  chemistry,  pharmacokinetics*
Biological Availability
Biological Transport
Cattle
Cell Polarity
Electric Impedance
Injections, Intra-Arterial
Isomerism
Male
Models, Biological
Muscle Relaxants, Central / blood,  chemistry,  pharmacokinetics*
Nasal Mucosa / metabolism*
Olfactory Mucosa / metabolism
Permeability
Rats
Rats, Sprague-Dawley
Grant Support
ID/Acronym/Agency:
DC 008374/DC/NIDCD NIH HHS; R01 DC008374/DC/NIDCD NIH HHS
Chemical
Reg. No./Substance:
0/Muscle Relaxants, Central; 1134-47-0/Baclofen

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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