Transdermal composition containing donepezil as active ingredient
AssigneeIcure Pharmaceutical Inc.
InventorsYoung Kweon Choi, Dong Hyun Hong, Seong Soo Kim
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Abstract
The present invention relates to a transdermal composition for dementia treatment containing donepezil as an active ingredient. The transdermal composition according to the present invention contains highly concentrated donepezil in a hydrophobic matrix, can continuously release the drug for a long time by having excellent long-term adhesion to the skin, and further exhibits consistently effective therapeutic effects over a long period of time by having a significantly improved skin penetration rate in comparison with conventional donepezil patches.
Claims19
A transdermal composition containing donepezil as an active ingredient, the transdermal composition comprising:
- (a) a backing layer;
- (b) a drug-containing matrix layer comprising, based on a total weight of the drug-containing matrix layer,
- (b-1) 15-55 wt % of donepezil or a pharmaceutically acceptable salt thereof,
- (b-2) 25-70 wt % of an EVA-based adhesive,
- (b-3) 5-20 wt % of at least one selected from the group consisting of a pyrrolidone derivative and a C8-18 aliphatic derivative, and
- (b-4) 1-10 wt % of triacetin or a citric acid derivative,
- (c) a polymer adhesive matrix layer comprising, based on a total weight of the polymer adhesive matrix layer, 60 wt % or more of an acrylic adhesive;
- and
- (d) a release layer.
A method for administering donepezil into a subject, the method comprising:
- (1) attaching, to the skin of a subject, a transdermal composition comprising donepezil as an active ingredient, wherein the transdermal composition comprises:
- (a) a backing layer;
- (b) a drug-containing matrix layer comprising, based on a total weight of the drug-containing matrix layer,
- (b-1) 15-55 wt % of donepezil or a pharmaceutically acceptable salt thereof,
- (b-2) 25-70 wt % of an EVA-based adhesive,
- (b-3) 5-20 wt % of at least one selected from the group consisting of a pyrrolidone derivative and a C8-18 aliphatic derivative, and
- (b-4) 1-10 wt % of triacetin or a citric acid derivative;
- (c) a polymer adhesive matrix layer comprising, based on a total weight of polymer adhesive matrix layer, 60 wt % or more of an acrylic adhesive;
- and
- (d) a release layer;
- and
- (2) maintaining the transdermal composition attached to the skin of the subject for a time sufficient to deliver donepezil to the subject.
A kit comprising a transdermal composition, wherein the transdermal composition comprises:
- (a) a backing layer;
- (b) a drug-containing matrix layer comprising, based on a total weight of the drug-containing matrix layer,
- (b-1) 15-55 wt % of donepezil or a pharmaceutically acceptable salt thereof,
- (b-2) 25-70 wt % of an EVA-based adhesive,
- (b-3) 5-20 wt % of at least one selected from the group consisting of a pyrrolidone derivative and a C8-18 aliphatic derivative, and
- (b-4) 1-10 wt % of triacetin or a citric acid derivative;
- (c) a polymer adhesive matrix layer comprising, based on a total weight of polymer adhesive matrix layer, 60 wt % or more of an acrylic adhesive;
- and
- (d) a release layer.
Dependencies are inferred from the claim text.