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Last Updated: April 24, 2024

Details for Patent: 4,814,168


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Title: Transdermal multipolymer drug delivery system
Abstract:A dermal compositon comprising a drug, a multi-polymer of vinyl acetate, polyethylene and optionally one or more monomers, a natural or synthetic rubber and a tackifying agent. The ratio of the multipolymer to the rubber is, respectively, about 1:1 to about 10:1 and more preferably 1:1 to 5:1 and more preferably 3:1. The dermal composition can optionally contain a crosslinking agent, tackifiers, penetration enhancers and other ingredients known for use in adhesives for the transdermal delivery of drugs. The dermal compositions can be produced by a variety of methods known in the preparation of drug containing adhesive preparations including the homogenous mixing of the multi-polymer, drug and optional crosslinking agent and additional ingredients in aqueous solution followed by removal of excess water.
Inventor(s): Sablotsky; Steven (Miami, FL), Questel; John M. (Cuyahoga Falls, OH), Leeson; Dorothy J. (North Canton, OH)
Assignee: Noven Pharmaceuticals, Inc. (Miami, FL)
Filing Date:Mar 04, 1988
Application Number:07/164,482
Claims:1. An adhesive dermal composition comprising a drug, a multipolymer containing vinyl acetate and ethylene monomers, a natural or synthetic rubber, and a tackifying agent, in which the ratio by weight of the multi-polymer to rubber is about 1:1 to about 10:1.

2. The dermal composition of claim 1, in which the multi-polymer is a carboxylated vinyl acetate/ethylene terpolymer and the rubber is polyisoprene.

3. The dermal composition of claim 1 in which the drug is a solid or liquid at room temperature, is percutaneously absorbable, and is dissolved or dispersed in the composition.

4. The dermal composition of claim 3 in which the weight of the drug is about 1 to 50% by weight based on the weight of the dermal composition.

5. A dermal composition comprising a drug, a crosslinked multipolymer of carboxylated vinyl acetate/ethylene, a natural or synthetic rubber, and a tackifying agent in which the multipolymer and rubber are in a ratio, respectively, of from about 1:1 to about 10:1.

6. The dermal composition according to claim 5 in which the crosslinking agent is selected from the group of agents known for the crosslinking of free carboxyl groups of polymeric substances.

7. The dermal composition according to claim 5 in which the crosslinking agent is selected from the group consisting of melamine formaldehyde resin, urea formaldehyde resn, phenolic resins, epoxy resins, glyoxal, zinc oxide, magnesium oxide and ammonium dichromate.

8. The dermal composition according to claim 5, in which the multipolymer is a terpolymer of ethylene, vinyl acetate and acrylic acid.

9. The dermal composition according to claim 8 in which the percent by weight of ethylene, vinyl acetate and acrylic acid units in the terpolymer are, respectively, roughly 15 to 90;4 to 80 and 0 to 5.

10. The dermal composition according to claim 8 in which the amounts of ethylene, vinyl acetate and acrylic acid are respectively roughly 77%, 20% and 3%.

11. The dermal composition according to claim 5 in which the carboxylated vinyl acetate ethylene copolymer and natural rubber are in a ratio, respectively, of about 3:1.

12. The dermal composition which comprises, as percent by weight, about 20% to about 39% carboxylated vinyl acetate ethylene copolymer about 5% to about 20% natural rubber, about 10% to about 30% of a tackifying agent, about 1% to about 50% of drug, and 0% to about 2% of a crosslinking agent.

13. The composition of claim 12 which comprises about 30% carboxylated vinyl acetate ethylene copolymer, about 11% natural rubber, about 12% tackifier and 41% drug.

14. The composition according to claim 13 in which the drug is nitroglycerin or estradiol.

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