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Int J Pharm ; 436(1-2): 32-40, 2012 Oct 15.
Article in English | MEDLINE | ID: mdl-22771734

ABSTRACT

Because of low treatment compliance with the Alzheimer disease patients, there have been clinical needs for the alternative administration route to effective and well-tolerated approaches of galantamine (Small and Dubois, 2007). In this study, drug-in-adhesive transdermal patches with galantamine were prepared and evaluated in vitro and in vivo. The in vitro permeation studies indicated that DT-2510 was the most suitable pressure-sensitive-adhesive and oleic acid was the most promising enhancer for galantamine drug-in-adhesive patch. The optimized galantamine drug-in-adhesive patch could be physicochemically stable for 28 days at 40 °C/75% RH. The in vivo studies of the optimized galantamine drug-in-adhesive patch showed high absolute bioavailability of around 80% and sustained effect on the drug plasma levels for 24 h. The in vitro and in vivo studies of galantamine drug-in-adhesive patches with different pressure-sensitive-adhesive functional groups showed a strong correlation between the skin permeation rate and the area under the curve. The results suggest that the transdermal application of galantamine drug-in-adhesive patches might be the alternative dosage form to have good efficacy and tolerability for the treatment of Alzheimer disease.


Subject(s)
Adhesives/chemistry , Cholinesterase Inhibitors/chemistry , Galantamine/chemistry , Oleic Acid/chemistry , Transdermal Patch , Adhesives/administration & dosage , Administration, Cutaneous , Animals , Chemistry, Pharmaceutical , Cholinesterase Inhibitors/administration & dosage , Cholinesterase Inhibitors/pharmacokinetics , Galantamine/administration & dosage , Galantamine/pharmacokinetics , In Vitro Techniques , Male , Oleic Acid/administration & dosage , Oleic Acid/pharmacokinetics , Rabbits , Rats , Rats, Sprague-Dawley , Skin Absorption
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