Transdermal drug patches

• US 4,668,232 A
• Filed: 12/18/1985
• Issued: 05/26/1987
• Est. Priority Date: 12/22/1984
• Status: Expired due to Term

• Current Assignee: Schwartz GmbH
• Original Assignee: Schwartz GmbH
• Inventors: Wolff, Michael, Cordes, G/u/ nter
• Primary Examiner(s): YASKO JR, JOHN D
• Application Number:
  US06/810,212
• Time in Patent Office: 524 Days
• Field of Search: 604/897, 604/896, 604/892, 604/890, 42/28, 42/349, 514/509, 514/964
• US Class Current: 424/448
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7076 the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins
• CPC Class Codes: A61K 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
• CPC Class Codes: A61L 15/585 Mixtures of macromolecular compounds
• CPC Class Codes: A61L 15/60 Liquid-swellable gel-forming materials, e.g. super-absorbents

Abstract

The invention relates to transdermal drug patches for the controlled release of drugs to the human skin, 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 polymer matrix composed of a rubber and an adhesive resin material wherein said therapeutically active agent or agents are wholly or partially soluble and which is permeable to said agent or agents,

(c) an adhesive layer adjacent to, and in close contact with, said reservoir layer and permeable to said therapeutically active agent or agents, and

(d) a protective layer covering and adhearing to said adhesive layer and removeable therefrom for the use of said transdermal drug patch,

the improvement wherein said drug or drugs in the rubber and adhesive resin material of the reservoir layer are present together with a polymer capable of swelling in water and insoluble in the rubber and adhesive resin material of the reservoir layer, the quantity of said polymer being between 3 and 30% by weight of the rubber and adhesive resin mixture.

By the incorporation of this particular water-swellable polymer material in the rubber/adhesive resin mixture together with the drug which polymer material is insoluble in the matrix, in a particular proportion calculated to the weight of the rubber and adhesive resin material in particular the drug release from the patch to the skin is increased to twice or even more is achieved.

Claims

1. In a transdermal drug patch for the controlled release of a drug to the human skin 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 polymer matrix composed of a rubber and an adhesive resin material in which a therapeutically active drug agent is present in wholly or partially soluble form and said material being permeable to said agent or agents,

(c) an adhesive layer adjacent to, and in close contact with, said reservoir layer and permeable to said therapeutically active agent, and

(d) a protective layer covering and adhearing to said adhesive layer and removable therefrom for the use of said transdermal drug patch, the improvement wherein said drug agent in the rubber and adhesive resin material of the reservoir layer is present together with a polymer capable of swelling in water and insoluble in the rubber and adhesive resin material of the reservoir layer, the quantity of said polymer being between 3 and 30 percent by weight of the rubber and adhesive resin mixture.

2. Transdermal drug patch according to claim 1 wherein the drug is a compound selected from the group consisting of the beta blockers, the steroid hormones, the calcium antagonists and the cardiac-acting drugs.

3. Transdermal drug patch according to claim 1 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a polysaccharide or a mixture of polysaccharides.

4. Transdermal drug patch according to claim 2 wherein the polymer capable of swelling in water and insolule in the material of the reservoir layer and/or the adhesive layer is a polysaccharide or a mixture of polysaccharides.

5. Transdermal drug patch according to claim 2 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a membrane selected from the group consisting of a galactomannane, microcrystalline cellulose and tragacanth.

6. Transdermal drug patch according to claim 3 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a membrane selected from the group consisting of a galactomannane, microcrystalline cellulose and tragacanth.

7. Transdermal drug patch according to claim 4 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a membrane selected from the group consisting of a galactomannane, microcrystalline cellulose and tragacanth.

8. Transdermal drug patch for estradiol according to claim 1 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

9. Transdermal drug patch for estadiol according to claim 2 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

10. Transdermal drug patch for estadiol according to claim 3 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

11. Transdermal drug patch for estadiol according to claim 4 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

12. Transdermal drug patch for estadiol according to claim 5 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

13. Transdermal drug patch for estadiol according to claim 6 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

14. Transdermal drug patch for estadiol according to claim 7 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

15. Transdermal drug patch for bupranolol according to claim 1 wherein the polymer capable of swelling in water and insoluble in the material of the adhesive film is microcrystalline cellulose.

16. Transdermal drug patch for bupranolol according to claim 2 wherein the polymer capable of swelling in water and insoluble in the material of the adhesive film is microcrystalline cellulose.

17. Transdermal drug patch for bupranolol according to claim 3 wherein the polymer capable of swelling in water and insoluble in the material of the adhesive film is microcrystalline cellulose.

18. Transdermal drug patch for bupranolol according to claim 4 wherein the polymer capable of swelling in water and insoluble in the material of the adhesive film is microcrystalline cellulose.

19. Transdermal drug patch for bupranolol according to claim 5 wherein the polymer capable of swelling in water and insoluble in the material of the adhesive film is microcrystalline cellulose.

20. Transdermal drug patch for bupranolol according to claim 6 wherein the polymer capable of swelling in water and insoluble in the material of the adhesive film is microcrystalline cellulose.

21. Transdermal drug patch for estadiol according to claim 7 wherein the polymer capable of swelling in water and insoluble in the material of the reservoir layer and/or the adhesive layer is a galactomannane.

22. Transdermal drug patch for nitroglycerin in accordance with claim 1 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

23. Transdermal drug patch for nitroglycerin in accordance with claim 2 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

24. Transdermal drug patch for nitroglycerin in accordance with claim 3 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

25. Transdermal drug patch for nitroglycerin in accordance with claim 4 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

26. Transdermal drug patch for nitroglycerin in accordance with claim 5 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

27. Transdermal drug patch for nitroglycerin in accordance with claim 6 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

28. Transdermal drug patch for nitroglycerin in accordance with claim 7 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film and/or adhesive film is microcrystalline cellulose.

29. Transdermal drug patch for propranolol according to claim 1 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microcrystalline cellulose.

30. Transdermal drug patch for propanolol according to claim 7 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microcrystalline cellulose.

31. Transdermal drug patch for propanolol according to claim 3 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microcrystalline cellulose.

32. Transdermal drug patch for propanolol according to claim 4 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microcrystalline cellulose.

33. Transdermal drug patch for propanolol according to claim 5 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microcrystalline cellulose.

34. Transdermal drug patch for propanolol according to claim 6 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microcrystalline cellulose.

35. Transdermal drug patch for propranolol according to claim 7 wherein the polymer capable of swelling in water and insoluble in the material of the matrix film/adhesive film is microsrystalline cellulose.