Composition For Transdermal Delivery Of Fentanyl
A transdermal drug delivery composition comprises an acrylate copolymer and from about 8% to about 30% by weight fentanyl. A transdermal fentanyl delivery composition comprising methyl laurate or tetraglycol as a permeation enhancer is also provided. The transdermal drug delivery compositions can be used to make a transdermal drug delivery device for the delivery of fentanyl.
1 . A transdermal drug delivery composition consisting of:
(a) a copolymer comprising the reaction product of:
(i) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 12 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 12 carbon atoms in the alkyl group; and
(ii) one or more ethylenically unsaturated B monomers copolymerizable with the A monomer;
(b) about 8% to about 30% by weight fentanyl based on the total weight of the composition; and, optionally,
(c) a component selected from the group consisting of delivery enhancing adjuvants, tackifiers, plasticizers, and combinations thereof,
wherein the composition is free of undissolved fentanyl.
2 . The composition of claim 1 wherein the A monomer is selected from the group consisting of isooctyl acrylate, 2-ethylhexyl acrylate, butyl acrylate, cyclohexyl acrylate, and combinations thereof.
3 . The composition of claim 1 wherein the A monomer includes isooctyl acrylate.
4 . The composition of claim 1 wherein the B monomer is selected from the group consisting of 2-hydroxyethyl acrylate, 2-hydroxyethyl methacrylate, glyceryl acrylate, N,N-diethylacrylamide, 2-ethoxyethoxyethyl acrylate, 2-ethoxyethyl acrylate, tetrahydrofurfuryl acrylate, acrylic acid, acrylamide, vinyl acetate, N-vinyl pyrrolidone, and combinations thereof.
5 . The composition of claim 1 wherein the B monomer includes 2-hydroxyethyl acrylate.
6 . The composition of claim 1 wherein the copolymer comprises the reaction product of:
(i) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 12 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 12 carbon atoms in the alkyl group;
(ii) one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(iii) a macromonomer.
7 . The composition of claim 1 wherein the concentration of fentanyl in the composition is about 8% by weight.
8 . A device for the transdermal delivery of fentanyl comprising a backing and a composition according to claim 1 , said composition being adhered to one surface of the backing.
9 . A method of providing analgesia to a mammal comprising:
(a) placing the composition of claim 1 on the skin of a mammal; and
(b) allowing the composition to remain on the skin for a time sufficient to establish or maintain an analgesically effective blood level of fentanyl in the mammal.