Adhesive transdermal dosage layer
First Claim
1. An adhesive bilayer transdermal dosage system for the sustained release of nitroglycerin to the skin of a human patient, comprising:
- (i) a first component layer formed of a nitroglycerin-containing essentially planar sheet of an at least partially cross-linked acrylic pressure-sensitive adhesive, said essentially planar sheet comprising a flexible self-supporting cross-linked acrylate polymer of sufficient adhesivity, durability and strength whereby intimate diffusional contact with skin of the patient is maintained for a period of at least about 24 hours without destruction of the physical integrity of said sheet, said essentially planar sheet being capable of retaining dispersed therein sufficient nitroglycerin to deliver to the skin a pharmaceutically effective amount of said nitroglycerin over a 24-hour time interval, without dissolution of the at least partially cross-linked acrylic pressure-sensitive adhesive and(ii) a second component layer intimately adhered to one side of said first component layer, said second component layer being resistant to the passage of pharmaceutically active drug from said first component layer;
wherein said first component layer comprises about 40 to about 80% by weight of acrylic adhesive;
wherein said acrylic adhesive comprises about 1 to about 5% by weight of acrylic acid and about 5 to about 20% by weight of a C4 to C12 alkyl acrylate;
about 20 to about 60% by weight of nitroglycerin;
about 0.2 to about 1% of a cross-linking agent and 10% or less of water.
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Accused Products
Abstract
An adhesive bilayer transdermal dosage system capable of sustained release of a pharmaceutically active drug to the skin of a human patient having a first component layer which is a pharmaceutically active drug-containing essentially planar sheet of an at least partially cross-linked acrylic adhesive. The planar sheet is formed of a flexible self-supporting cross-linked acrylate of sufficient adhesivity, durability and strength whereby intimate diffusional contact with the skin of the patient is maintained for a period of at least about 24 hours without destruction of the physical integrity of the sheet. The sheet is capable of retaining, dispersed therein, sufficient pharmaceutically active drug to deliver to the skin a pharmaceutically effective amount of the drug over a 24-hour period without dissolution of the at least partially crosss-linked acrylic adhesive. The system also contains a second component layer intimately adhered to one side of the first component layer. The second component layer is resistant to the passage of the pharmaceutically active drug from the first component layer. Methods for making the first component layer and dosage system are also disclosed.
145 Citations
19 Claims
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1. An adhesive bilayer transdermal dosage system for the sustained release of nitroglycerin to the skin of a human patient, comprising:
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(i) a first component layer formed of a nitroglycerin-containing essentially planar sheet of an at least partially cross-linked acrylic pressure-sensitive adhesive, said essentially planar sheet comprising a flexible self-supporting cross-linked acrylate polymer of sufficient adhesivity, durability and strength whereby intimate diffusional contact with skin of the patient is maintained for a period of at least about 24 hours without destruction of the physical integrity of said sheet, said essentially planar sheet being capable of retaining dispersed therein sufficient nitroglycerin to deliver to the skin a pharmaceutically effective amount of said nitroglycerin over a 24-hour time interval, without dissolution of the at least partially cross-linked acrylic pressure-sensitive adhesive and (ii) a second component layer intimately adhered to one side of said first component layer, said second component layer being resistant to the passage of pharmaceutically active drug from said first component layer; wherein said first component layer comprises about 40 to about 80% by weight of acrylic adhesive;
wherein said acrylic adhesive comprises about 1 to about 5% by weight of acrylic acid and about 5 to about 20% by weight of a C4 to C12 alkyl acrylate;
about 20 to about 60% by weight of nitroglycerin;
about 0.2 to about 1% of a cross-linking agent and 10% or less of water. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 17, 18, 19)
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12. An adhesive transdermal layer for the sustained release of a pharmaceutically active drug to the skin of a human patient, comprising:
a pharmaceutically active drug-containing essentially planar sheet of an at least partially cross-linked acrylic adhesive, said essentially planar sheet comprising a flexible self-supporting cross-linked acrylate polymer of sufficient adhesivity, durability and strength whereby intimate diffusional contact with skin of the patient is maintained for a period of at least about 24 hours without destruction of the physical integrity thereof, said essentially planar sheet being capable of retaining dispersed therein sufficient pharmaceutically active drug to deliver to the skin a pharmaceutically effective amount of said pharmaceutically active drug over a 24-hour time interval, without dissolution of the at least partially cross-linked acrylic pressure-sensitive adhesive. - View Dependent Claims (13, 14, 15)
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16. An adhesive transdermal layer for the sustained release of a pharmaceutically active drug formed by
a) mixing an acrylic adhesive and water to form a homogeneous mixture; -
b) adding a pharmaceutically active drug to said homogeneous mixture; c) forming a smooth homogeneous mix of said pharmaceutically active drug and said homogeneous mixture; d) adding a cross-linking agent for said acrylic adhesive to said smooth homogeneous mix; e) undertaking cross-linking between said cross-linking agent and said acrylic adhesive; and f) removing sufficient water and solvent from the product of step e) to form said adhesive transdermal layer.
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Specification