Estrogen-containing active substance plaster

• US 5,393,529 A
• Filed: 06/08/1993
• Issued: 02/28/1995
• Est. Priority Date: 10/06/1989
• Status: Expired due to Term

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG, Schwarz Pharma Ag (Schwarz Pharma)
• Inventors: Cordes, Gunter, Wolff, Hans M., Hoffmann, Hans-Rainer, Meconi, Reinhold, Klein, Robert P.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Benston, Jr., William E.
• Application Number:
  US08/074,698
• Time in Patent Office: 630 Days
• Field of Search: 424/444, 424/445, 424/446, 424/447, 424/448, 424/449, 428/40
• US Class Current: 424/445
• 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
• CPC Class Codes: A61L 15/58 Adhesives
• CPC Class Codes: C08L 33/06 of esters containing only carbon, hydrogen and oxygen, which oxygen atoms are present only as part of the carboxyl radical

Abstract

The present invention relates to active substance plasters for the controlled release of active substances to the skin consisting of a backing layer, an adhesive film connected therewith which film is water-soluble and consists of pressure-sensitive adhesive which comprises water-swellable polymers and in which the active substance is at least partially soluble, and of a removable protective layer covering the adhesive film, in which plasters the pressure-sensitive adhesive is based on homo and/or copolymers with at least one derivative of the acrylic or methacrylic acid, and which comprise as active substances, partially or completely dissolved in the adhesive, at a concentration of 0.5 to 10.0%-wt estrogens and their pharmaceutically acceptable derivatives alone or in combination with gestagens.

Claims

1. In a plaster for the controlled release of an estrogen to the skin and comprising

A) an impermeable backing or covering layer,

B) a reservoir layer adjacent to, and in close contact with said backing or covering layer, said reservoir layer comprising a water-insoluble pressure-sensitive adhesive polymer layer containing the estrogen in a concentration of about 0.5 to 10 by weight, in combination with at least one water-swellable polymer in 0.01 to 10% wt, and

C) a protective layer covering and adhering to said adhesive polymer layer and removable therefrom for the use of said transdemal drug patch, the improvement wherein the pressure-sensitive adhesive polymer of B is a polymer of acrylic or methacrylic acid or an ester thereof, and contains a 0.1 to 20%-wt of at least one substance delaying or preventing the crystallization of the active substance,

the water-swellable polymer being selected from the group consisting of galactomannans, cellulose products, tragacanth, polyglycosides, polyvinylpyrrolidones, finely pulverized polyamides, water-soluble polyacrylamide, carboxyvinyl polymers, agar, copolymers of methylvinyl ether and maleic acid anhydride, guar gum, hydroxypropyl guar gum or guar flour, gum arabic, dextrin and dextran, polysaccharide gum, hydroxymethylpropyl cellulose, pectin and pectinamide, and

the crystallization delaying or preventing substance being selected from the group consisting of phthalic acid esters, adipic acid esters, monoglycerides, diglycerides, and triglycerides, ester of higher fatty acids, long-chain alcohols, nonylphenol, octylphenol, fatty acids, sorbitol, mannitol, non-ionogenic surfactants, polyoxyethylene alkyl esters, castor oil, sitosterine and polyvinylpyrrolidone.

2. A plaster according to claim 1, wherein the polymer of B is cross-linkable.

3. A plaster according to claim 1, wherein the polymer of B is a solvent-based pressure-sensitive adhesive.

4. A plaster according to claim 1, wherein the polymer of B is a dispersion-based pressure-sensitive adhesive.

5. A plaster according to claim 1, wherein the polymer of C is a hot-melt-pressure-sensitive adhesive.

6. A plaster according to claim 1, wherein the pressure-sensitive adhesive comprises at least one tackifying resin in an amount of 0.5 to 50%-wt.

7. A plaster according to claim 1, wherein the therapeutic substance-containing adhesive film has a thickness of 0.01 to 0.3 mm.

8. A plaster according to claim 1, wherein the additionally water-swellable polymer of layer C is selected from the group consisting of galactomannan, microcrystalline cellulose and tragacanth.