Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 436, Issue 1-2, Pages 32-40Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2012.06.057
Keywords
Galantamine; Transdermal patch; Skin permeation rate; Bioavailability; In vitro and in vivo characteristics
Categories
Funding
- Korean Health Technology R&D Project, for Health, Welfare & Family Affairs, Republic of Korea [A092018]
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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 degrees 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. (c) 2012 Elsevier B.V. All rights reserved.
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