Matrix for transdermal drug delivery
First Claim
Patent Images
1. A transdermal drug delivery device, comprising:
- (1) a backing;
(2) a matrix adhered to one side of the backing and comprising (a) a copolymer comprising (i) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 10 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 10 carbon atoms in the alkyl group; and
(ii) optionally one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(iii) a macromonomer comprising an ethylenically unsaturated group copolymerizable with the A and B monomers defined above and having a molecular weight in the range 500-500,000;
(b) a softener dissolved in the copolymer; and
, (c) if the softener is not therapeutically effective, a therapeutically effective amount of a drug,
wherein the structure and amount of the comonomers in the copolymer, the inherent viscosity of the copolymer, and the amount and structure of the drug and the softener are such as to provide the matrix with a compliance value in the range of about 2×
10−
6 cm2/dyne to about 4×
10−
3 cm2/dyne.
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Accused Products
Abstract
A transdermal drug delivery device involving a macromonomer-containing acrylate or methacrylate copolymer, a softener, and a drug. Also a pressure sensitive skin adhesive involving a macromonomer containing acrylate or methacrylate copolymer and a softener.
157 Citations
34 Claims
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1. A transdermal drug delivery device, comprising:
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(1) a backing;
(2) a matrix adhered to one side of the backing and comprising (a) a copolymer comprising (i) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 10 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 10 carbon atoms in the alkyl group; and
(ii) optionally one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(iii) a macromonomer comprising an ethylenically unsaturated group copolymerizable with the A and B monomers defined above and having a molecular weight in the range 500-500,000;
(b) a softener dissolved in the copolymer; and
,(c) if the softener is not therapeutically effective, a therapeutically effective amount of a drug,
wherein the structure and amount of the comonomers in the copolymer, the inherent viscosity of the copolymer, and the amount and structure of the drug and the softener are such as to provide the matrix with a compliance value in the range of about 2×
10−
6 cm2/dyne to about 4×
10−
3 cm2/dyne. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 33)
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19. A pressure sensitive skin adhesive comprising:
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(1) a copolymer comprising (a) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 10 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 10 carbon atoms in the alkyl group; and
(b) optionally one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(c) a macromonomer comprising an ethylenically unsaturated group copolymerizable with the A and B monomers defined above and having a molecular weight in the range 500-500,000; and
(2) a softener dissolved in the copolymer,
wherein the structure and amount of the comonomers in the copolymer, the inherent viscosity of the copolymer, and the amount and structure of the softener are such as to provide the pressure sensitive sldn adhesive with a compliance value in the range 2×
10−
6 cm2/dyne to about 4×
10−
3 cm2/dyne. - View Dependent Claims (20)
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- 21. In atransdermal delivery system for administering at least one pharmacologically active agent comprising a flexible backing material impermeable to said active agent and an adhesive layer on said backing material, the improvement wherein said adhesive layer comprises a pressure sensitive adhesive composition comprised of (1) a percutaneous penetration enhancer to increase permeability of skin to transdermally administered pharmacologically active agents in admixture with (2) a macromer reinforced base polymer, said base polymer component comprising a phase separated graft copolymer comprised of copolymerized monomers A and B to form a backbone polymer having polymeric moieties grafted thereto, wherein monomer A is a monomeric acrylic or methacrylic ester of a non-tertiary alcohol having from 4 to 10 carbon atoms, and monomer B is a polar monomer which is copolymerizable with monomer A, said percutaneous penetration enhancer being present in said composition in an amount of up to 40 percent by weight based on the weight of the composition.
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30. A transdermal drug delivery device, comprising:
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(1) a backing;
(2) a matrix adhered to one side of the backing and comprising (a) a copolymer comprising (i) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 10 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 10 carbon atoms in the alkyl group; and
(ii) optionally one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(iii) a macromonomer comprising an ethylenically unsaturated group copolymerizable with the A and B monomers defined above; and
(3) a skin penetration enhancer dissolved in the copolymer.
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31. A pressure sensitive skin adhesive comprising:
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(1) a copolymer comprising (a) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 10 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 10 carbon atoms in the alkyl group; and
(b) optionally one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(c) a macromonomer comprising an ethylenically unsaturated group copolymerizable with the A and B monomers defined above; and
(2) a skin penetration enhancer dissolved in the copolymer.
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32. A transdermal drug delivery device, comprising:
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(1) a backing;
(2) a matrix adhered to one side of the backing and comprising (a) a copolymer comprising (i) one or more A monomers selected from the group consisting of alkyl acrylates containing 4 to 10 carbon atoms in the alkyl group and alkyl methacrylates containing 4 to 10 carbon atoms in the alkyl group; and
(ii) optionally one or more ethylenically unsaturated B monomers copolymerizable with the A monomer; and
(iii) a macromonomer comprising an ethylenically unsaturated group copolymerizable with the A and B monomers defined above; and
(3) a softener dissolved in the copolymer,
wherein the structure and amount of the comonomers in the copolymer, the inherent viscosity of the copolymer, and the amount and structure of the softener are such as to provide the pressure sensitive skin adhesive with a compliance value in the range 2×
10−
6 cm2/dyne to about 1×
10−
3 cm2/dyne.- View Dependent Claims (34)
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Specification