Recrystallization-free estradiol-containing patch

• US 5,885,612 A
• Filed: 07/08/1997
• Issued: 03/23/1999
• Est. Priority Date: 01/12/1995
• Status: Expired due to Term

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme GmbH
• Inventors: Seibertz, Frank, Meconi, Reinhold
• Primary Examiner(s): BROUILLETTE, D GABRIELLE
• Application Number:
  US08/860,595
• Time in Patent Office: 623 Days
• Field of Search: 424/448, 424/449
• US Class Current: 424/448
• CPC Class Codes: A61K 9/7069 obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 5/30 Oestrogens

Abstract

An active substance-containing patch for the controlled release of estradiol or its pharmaceutically acceptable derivatives alone or combined with gestagens, comprising a backing layer, an active substance-containing reservoir which is bonded thereto and produced by using pressure-sensitive adhesives, and a removable protective layer, is characterized by the fact that the pressure-sensitive adhesive comprises ethylcellulose, esters of non-hydrogenated and/or hydrogenated colophony, and lauric acid.

Claims

1. A recrystallization-free estradiol-containing patch for the controlled release of estradiol or its pharmaceutically acceptable derivatives alone or in combination with at least one gestagen, comprising a backing layer, an active substance-containing reservoir, and a removable protective layer wherein said reservoir is bonded to said backing layer and contains a pressure-sensitive adhesive comprising 5-25%-wt. ethylcellulose, 50-90%-wt. of esters of non-hydrogenated and/or hydrogenated colophony, and 1-20%-wt. lauric acid.

2. The active substance-containing patch according to claim 1 wherein the pressure-sensitive adhesive comprises lauric acid in a proportion of 2-15%-wt.

3. The active substance-containing patch according to claim 1 wherein the pressure-sensitive adhesive comprises 8-14%-wt. of ethylcellulose.

4. The active substance-containing patch according to claim 1 wherein the pressure-sensitive adhesive comprises esters of colophony in a proportion of 60-80%-wt.

5. The active substance-containing patch according to claim 1 wherein the pressure-sensitive adhesive comprises estradiol or its pharmaceutically acceptable derivatives alone or in combination with at least one gestagen in a proportion of 1-15%-wt.

6. The active substance-containing patch according to claim 4 wherein the pressure-sensitive adhesive comprises estradiol or its pharmaceutically acceptable derivatives alone or in combination with at least one gestagen at a proportion of 1.5-5.0%-wt.

7. The active substance-containing patch according to claim 1 wherein the pressure sensitive adhesive comprises 2-15%-wt. lauric acid, 8-14%-wt. ethylcellulose and 60-80%-wt. colophony.

8. The active substance-containing patch according to claim 1 wherein the backing layer is impermeable to the components of the reservoir.

9. The active substance-containing patch according to claim 1 wherein the esters of colophony are selected from the group consisting of methyl ester, glycerol ester, pentaerythritol ester, pentaerythritol ester modified with maleic acid, glycerol ester modified with maleic acid, and triethylene glycol ester.

10. The active substance-containing patch according to claim 1 wherein the reservoir comprises estradiol or its pharmaceutically acceptable derivatives in combination with at least one gestagen in a molar ratio of 1:

1 to 1;

10.

11. The active substance-containing patch according to claim 1 wherein the reservoir comprises at least one component of the group consisting of anti-aging agents, plasticizers, antioxidants, and absorption improvers.

12. The active substance-containing patch according to claim 1 wherein the pressure-sensitive adhesive is a solvent-based pressure-sensitive adhesive or a hot-melt pressure-sensitive adhesive.

13. The active substance-containing patch according to claim 1 wherein the reservoir consists of several layers and has an additional pressure-sensitive adhesive layer which is free from active substances.

14. The active substance-containing patch according to claim 13 wherein a membrane which controls the active substance release and is located between the reservoir and the pressure-sensitive adhesive layer.

15. The active substance-containing patch according to claim 1 wherein the reservoir is provided with a circumferential pressure-sensitive adhesive edge.

16. The 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.

18. A method of using the active substance-containing patch according to claim 1 or 17 for therapeutic purposes in human and veterinary medicine or in cosmetics comprising removing the said removable protective layer from the patch and placing the patch on the skin of a human or animal.

17. A recrystallization-free estradiol-containing patch for the controlled release of estradiol or its pharmaceutically acceptable derivatives alone or in combination with at least one gestagen, comprising a backing layer, an active substance-containing reservoir, and a removable protective layer, wherein said reservoir is bonded to said backing layer and contains a pressure-sensitive adhesive consisting essentially of 5-75% wt. ethylcellulose, 50-90% wt. esters of non-hydrogenated and/or hydrogenated colophony and 1-20% wt. lauric acid.