title: Investigation of formulation factors affecting in vitro and in vivo characteristics of a galantamine transdermal system.
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.
authors: School of Pharmacy, Sungkyunkwan University, Republic of Korea.
authors: Chun-Woong
authors: CW
authors: Park
authors: Dao-Danh
authors: DD
authors: Son
authors: Ju-Young
authors: JY
authors: Kim
authors: Tack-Oon
authors: TO
authors: Oh
authors: Jung-Myung
authors: JM
authors: Ha
authors: Yun-Seok
authors: YS
authors: Rhee
authors: Eun-Seok
authors: ES
authors: Park
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000737:chemistry*; D000279:Administration, Cutaneous; D000818:Animals; D002626:Chemistry, Pharmaceutical; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D005702:Galantamine / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008297:Male; D019301:Oleic Acid / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D057968:Transdermal Patch
chemical_list: D000269:Adhesives; D002800:Cholinesterase Inhibitors; D005702:Galantamine; D019301:Oleic Acid