Estradiol-containing patch for transdermal application of hormones

• US 6,531,149 B1
• Filed: 04/04/2001
• Issued: 03/11/2003
• Est. Priority Date: 07/29/1998
• Status: Expired due to Fees

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: Kirstgen, Elvira, Meconi, Reinhold
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Sheikh, Humera N.
• Application Number:
  US09/744,711
• Time in Patent Office: 706 Days
• Field of Search: 424/402, 424/443, 424/447, 424/448, 424/449, 514/847
• US Class Current: 424/449
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 2800/651 The particulate/core comprising inorganic material
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 8/0208 Tissues; Wipes; Patches
• CPC Class Codes: A61K 8/0241 Containing particulates characterized by their shape and/or structure see also A61K8/04, A61K8/11, and A61K8/14, further aspects are classified in A61K2800/40 and subcodes
• CPC Class Codes: A61K 8/63 Steroids; Derivatives thereof
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin

Abstract

An active substance-containing patch for controlled release of estradiol or its pharmaceutically acceptable derivatives, alone or in combination with gestagens, to the human or animal skin, consisting of a backing layer, an active substance-containing reservoir connected thereto which is suitable for combined active substance release and which has been produced using pressure-sensitive adhesives, and a detachable protective layer, is characterized in that the pressure-sensitive adhesive contains wool wax or components thereof and zinc oxide.

Claims

1. Active substance-containing patch for controlled release of hormonal active substance consisting of at least one of estradiol or its pharmaceutically acceptable derivatives, or at least one of estradiol or its pharmaceutically acceptable derivatives and at least one gestagen in a molar ratio of the former to the latter of 1:

1 to 1;

10, to human or animal skin, comprising a backing layer, an active substance-containing reservoir connected thereto which is suitable for active substance release and which comprises a layer of at least one pressure-sensitive adhesive containing polymer consisting essentially of acrylic polymer, and a detachable protective layer, wherein the acrylic polymer pressure-sensitive adhesive contains said active substance in a concentration of 1-20%-wt. based on the total weight of the reservoir, wool wax or components thereof in a concentration of 1-30%-wt. based on the total weight of the reservoir and zinc oxide in a concentration of 1-30%-wt. based on the total weight of the reservoir.

2. Active substance-containing patch according to claim 1, wherein the reservoir contains at least one component belonging to the group of age-protecting agents, antioxidants and absorption enhancers.

3. Active substance-containing patch according to claim 1, wherein the pressure-sensitive adhesive is a pressure-sensitive solution adhesive, a pressure-sensitive dispersion adhesive or a pressure-sensitive hot-melt adhesive.

4. Active substance-containing patch according to Claim 1, wherein the backing layer is impenneable to the components of the reservoir.

5. Active substance-containing patch according claim 1, wherein the reservoir comprises a plurality of layers including a plurality of active substance-containing pressure-sensitive adhesive layers.

6. Active substance-containing patch according to claim 1, further comprising an active substance release-controlling membrane between the reservoir and the pressure-sensitive adhesive layer.

7. Active substance-containing patch according to claim 1, wherein the reservoir includes a circumferential, pressure-sensitive adhesive margin.

8. Active substance-containing patch according to claim 1, wherein the thickness of the active substance-containing patch is in the range of 0.03-0.6 mm.

9. Active substance-containing patch according to claim 1, wherein said concentration of said active substance is 1.5-15%-wt.

10. Method of treating a human to improve skin of the human cosmetically, comprising applying to said skin said active substance-containing patch according to claim 1.

11. Method of treating skin of a human or an animal therapeutically, comprising applying to said skin said active substance-containing patch according to claim 1.