Transdermal drug delivery system containing donepezil
The present invention provides a transdermal drug delivery system comprising a drug-containing matrix layer comprising: (a) donepezil or a pharmaceutically acceptable salt thereof as an active ingredient; and (b) an acrylate-rubber hybrid as an adhesive.
1. A transdermal drug delivery system comprising:
a backing layer;
a drug-containing matrix layer; and
a release layer,
wherein the drug-containing matrix layer comprises:
(a) donepezil or a pharmaceutically acceptable salt thereof as an active ingredient;
(b) an acrylate-rubber hybrid as an adhesive;
(c) an absorption enhancer; and
(d) a crystallization-inhibiting agent,
wherein:
the transdermal drug delivery system has an increased skin penetration rate;
donepezil or its pharmaceutically acceptable salt is in an amount of 10 to 20% by weight of the total weight of the drug-containing matrix layer;
the absorption enhancer is in an amount of 5 to 15% by weight of the total weight of the drug-containing matrix layer; and
the crystallization-inhibiting agent is in an amount of 1 to 10% by weight of the total weight of the drug-containing matrix layer.
2. The transdermal drug delivery system of claim 1 , wherein the acrylate-rubber hybrid is an acrylic polymer comprising a C 4 ˜C 18 alkyl acrylate monomer grafted with a rubber macromer having a glass transition temperature of not more than −30° C.
3. The transdermal drug delivery system of claim 1 , wherein the acrylate-rubber hybrid is present in an amount ranging from 60 to 90% by weight, based on the total weight of the drug-containing matrix layer.
4. The transdermal drug delivery system of claim 1 , wherein the crystallization-inhibiting agent is an acrylate polymer or a methacrylate polymer.
5. The transdermal drug delivery system of claim 1 , wherein the crystallization-inhibiting agent is a copolymer of butyl methacrylate, 2-dimethylaminoethyl methacrylate, and methyl methacrylate in a weight ratio of 1:2:1.
6. The transdermal drug delivery system of claim 1 , wherein the absorption enhancer is selected from the group consisting of terpenes, surfactants, polyoxyethylene alkyl ethers, fatty alcohols, sugar esters, glycerols, alkyl 2-ethyl hexanates, and diethoxylethyl succinates.
7. The transdermal drug delivery system of claim 1 , wherein the absorption enhancer is present in an amount of 5% by weight, based on the total weight of the drug-containing matrix layer.
8. The transdermal drug delivery system of claim 1 , wherein the absorption enhancer is polyethylene glycol palm kernel glyceride, polyoxyethylene lauryl ether, polyglyceryl-3 oleate, lauryl alcohol, oleyl alcohol, or a mixture thereof.