Estradiol transdermal delivery system

• US 4,906,475 A
• Filed: 02/16/1988
• Issued: 03/06/1990
• Est. Priority Date: 02/16/1988
• Status: Expired due to Fees

• Current Assignee: Paco Pharmaceutical Services, Inc.
• Original Assignee: Paco Pharmaceutical Services, Inc.
• Inventors: Kim, Benjamin K.
• Primary Examiner(s): Robinson, Ellis P.
• Assistant Examiner(s): HORNE, LEON
• Application Number:
  US07/156,266
• Time in Patent Office: 749 Days
• Field of Search: 424/448, 424/449
• US Class Current: 424/449
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 9/7061 Polyacrylates

Abstract

The present invention is directed to a transdermal delivery system for an active substance. The active substance is estrogen or its derivatives and preferably is 17-beta-estradiol. The system comprises an impermeable backing layer and a matrix affixed thereto. The matrix comprises, on a weight percentage basis, from about 60 to about 95% of an adhesive polymer, from about 5 to about 20% of a solvent, from about 0.2 to about 4% of a skin penetration enhancer, and from about 0.5 to about 5% of the active substance. The system is free of any discrete permeable, polymeric, diffusion-controlling membrane.

Claims

1. A transdermal delivery system comprises:

an impermeable backing layer;

a matrix affixed to said backing layer and comprising on a weight percentage basis from about 60 to about 95% of an adhesive vinyl acetate-acrylate multipolymer, from about 5 to about 20% of a solvent, from about 0.2 to about 4% of a skin penetration enhancer, and from about 0.5 to about 5% of an active substance selected from the group consisting of estrogen, derivatives of estrogen and combinations thereof; and

said system being free of any discrete, permeable, polymeric, diffusion-controlling membrane.

2. The system according to claim 1 wherein said active substance is 17-beta-estradiol.

3. The system according to claim 1 wherein said solvent is selected from the group consisting of propylene glycol, propylene glycol derivatives and combinations thereof.

4. The system according to claim 1 wherein said solvent is selected from the group consisting of polyethylene glycol having approximate molecular weights of 200, 300, 400, 500, 600 and 800, and polyethylene glycol ester such as polyethylene glycol monolaurate, mono-oleate, and monolaurate, and combinations thereof.

5. The system according to claim 1 wherein said skin penetration enhancer is a polyoxyethylene ester.

6. The system according to claim 1 wherein said skin penetration enhancer is sorbitan mono-9-octadecenoate poly(oxy-1,2-ethanediyl) and its derivatives.

7. The system according to claim 1 further comprising a release layer, whereby said matrix is sandwiched between said backing layer and said release layer prior to use.

8. A transdermal delivery system comprises:

an impermeable backing layer;

a matrix affixed to said backing layer and comprising on a weight percentage basis from about 60 to about 95% of an adhesive vinyl acetate-acrylate multipolymer, from about 5 to about 20% of a solvent selected from the group consisting of propylene glycol, propylene glycol derivatives and combinations thereof, from about 0.2 to about 4% of a polyoxyethylene ester skin penetration enhancer, and from about 0.5 to about 5% of an active substance selected from the group consisting of estrogen, derivatives of estrogen and combinations thereof; and

said system being free of any discrete, permeable, polymeric, diffusion-controlling membrane.