Non-occulusive adhesive patch for applying medication to the skin

• US 5,536,263 A
• Filed: 03/30/1994
• Issued: 07/16/1996
• Est. Priority Date: 03/30/1994
• Status: Expired due to Term

• Current Assignee: Endo Pharmaceuticals Incorporated (Endo International PLC)
• Original Assignee: LecTec Corporation
• Inventors: Urmann, Elisabeth K. S., Rolf, David
• Primary Examiner(s): Green, Randall L.
• Assistant Examiner(s): CLARKE, ROBERT A
• Application Number:
  US08/219,982
• Time in Patent Office: 839 Days
• Field of Search: 604/304, 604/307, 602/48-51, 424/447-449, 514/953, 514/964, 514/965
• US Class Current: 604/307
• CPC Class Codes: A61F 13/00995 for mechanical treatments
• CPC Class Codes: A61F 2013/00646 Medication patches, e.g. transcutaneous
• CPC Class Codes: A61K 9/7023 Transdermal patches and similar drug-containing composite devices, e.g. cataplasms galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006
• CPC Class Codes: A61K 9/7061 Polyacrylates

Abstract

A non-occlusive medication patch to be applied to the skin includes a porous self-supporting backing layer to give the patch the required integrity and strength by acting as a supporting framework for other components, and a flexible hydrophilic pressure-sensitive adhesive reservoir comprising a hydrocolloidal gel for the sustained release of medication to be absorbed topically through the skin into the body of a patient. The reservoir has two portions: first, an external coating layer with an exposed lower skin-contacting surface that forms a pressure-sensitive bond with the skin, and second, an upper internal portion which infiltrates the porous backing and becomes solidified therein after being applied so that the reservoir and the backing are unified, enabling the backing itself to act as a storage location for the medication-containing reservoir. The medication within the reservoir migrates over time from within the backing through the lower coating layer and passes through the skin to provide sustained release of the medication into the body of a patient. The reservoir comprises a hydrocolloidal dispersion of a natural or synthetic gel-forming polymer, a hydrophilic adhesive, a hydrophilic humectant and a biomedically active medication, i.e., a medicament, dispersed throughout the reservoir including both the external portion and the internal portion that infiltrates the porous backing.

Claims

1. A non-occlusive medication-containing adhesive patch to be applied to the skin for releasing medication into the body of a patient comprising,

a porous backing layer comprising flexible sheet of water insoluble material to provide support for the patch,

a flexible hydrophilic pressure-sensitive adhesive hydrocolloidal gel matrix including a natural or synthetic polymer and a biomedically active substance, said matrix providing a reservoir for the sustained release of the biomedically active substance to be absorbed through the skin into the body of the patient,

said hydrocolloidal gel matrix penetrates a lower portion of the backing and the backing has an upper portion that is unpenetrated by the gel matrix,

the gel matrix is solidified within the lower portion of the backing and is dimensionally stable whereby the gel matrix partially penetrates the backing and leaves the upper portion of the backing free from the gel,

said gel matrix has two portions including:

a) an external layer with an exposed surface for bonding to the skin and

b) an internal portion infiltrated within only the lower portion of the porous backing layer,

said biomedically active substance is dispersed in a hydrocolloidal gel matrix including said internal portion, and

during use the gel matrix releases the biomedically active substance through an exposed surface thereof that is bonded to the skin of the patient, and

the backing has an upper surface that is spaced apart from the gel matrix.

2. The adhesive patch of claim 1 wherein the porous backing layer is a nonwoven fabric comprising water insoluble polymeric fibers with spaces therebetween.

3. The adhesive patch of claim 1 wherein the nonwoven fabric comprises a mixture of polyester fibers and cotton fibers.

4. The adhesive patch of claim 1 wherein the matrix comprises a natural or synthetic gel-forming polymer comprising a member selected from the group consisting of gum karaya, gum acacia, locust bean gum, guar gum, modified guar gum, maltodextrin, carboxymethyl cellulose, carboxypropyl cellulose, polyacrylamide and its cogeners, and polyacrylic acid.

5. The adhesive patch of claim 1 wherein the gel matrix includes a humectant that comprises a polyhydric alcohol.

6. The adhesive patch of claim 5 wherein the polyhydric alcohol comprises a member selected from the group consisting of glycerol, propylene glycol, ethylene glycol, and sorbitol.

7. The patch of claim 5 wherein the polyhydric alcohol is selected from the group consisting of glycerin and propylene glycol.

8. The adhesive patch of claim 1 wherein said matrix includes a resin emulsion adhesive.

9. The adhesive patch of claim 8 wherein the resin emulsion adhesive comprises a member selected from the group consisting of acrylate emulsion adhesive, an acrylic ester copolymer, a vinyl acetate resin, and copolymer of vinyl acetate and dioctyl maleate.

10. The adhesive patch of claim 1 wherein the substance is a medication comprising a member selected from the group consisting of trolamine salicylate, methyl salicylate, menthol, camphor, eucalyptus oil, spearmint oil, hydrocortisone, benzocaine, lidocaine, ibuprofen, salicylic acid, and capsicum.

11. The non-occlusive medication-containing adhesive patch of claim 1 wherein said biomedically active substance is at least one of the following:

a topical analgesic, an anti-pruritic agent, an anti-inflammatory agent, an anesthetic agent, a keratolytic agent, a rubrefacient agent.

12. A medication-containing adhesive patch for the transdermal delivery of medication into the body of a patient through the skin comprising,

a flexible pressure-sensitive adhesive matrix including a natural or synthetic polymer and a biomedically active substance to be absorbed through the skin into the body of the patient,

a porous backing for supporting the matrix, said backing comprising a sheet of water insoluble material having an upper surface and a lower surface,

said adhesive patch having the following layers proceeding from a lower surface of the adhesive patch to said upper surface of the backing:

a) an external layer of said adhesive matrix that is located below the lower surface of the backing, said external layer having an exposed surface for bonding to the skin of the patient,

b) an internal portion of the matrix partially penetrating the backing so as to be infiltrated within only a lower portion of the porous backing layer,

c) said backing layer includes a lower filled portion as a layer in which the internal portion of the matrix layer is infiltrated, and

d) an upper layer portion of the backing that is free of said matrix,

said biomedically active substance is dispersed in both portions of the matrix whereby the matrix releases the biomedically active substance into the skin through said exposed surface thereof, and

the backing has an upper surface that is spaced apart from the gel matrix.

13. The transdermal medication-containing adhesive patch of claim 12 wherein the matrix comprises a member selected from the group consisting of gum karaya, gum acacia, locust bean gum, guar gum, modified guar gum, maltodextrin, carboxymethylcellulose, carboxypropylcellulose, polyacrylamide and its cogeners, polyacrylic acid, vinyl acetate resin, acrylic ester copolymer, carbohydrate, vinyl acetate/dioctyl maleate copolymer, and acrylic polymer.

14. The medication-containing adhesive patch of claim 12 wherein the patch is coated on said upper surface with a release coating.

15. The medication-containing adhesive patch of claim 14 wherein the release coating is silicone.

16. The medication-containing adhesive patch of claim 12 wherein the porous backing layer is a member selected from the group consisting of nonwoven fabric, woven cloth fabric, and open-cell plastic foam.

17. The medication-containing adhesive patch of claim 12 wherein said matrix includes a hydrophilic hydrocolloid, a humectant, and a polymeric adhesive.

18. The medication-containing adhesive patch of claim 17 wherein the hydrophilic hydrocolloid comprises a member selected from the group consisting of gum karaya, gum acacia, locust bean gum, guar gum, modified guar gum, maltodextrin, carboxymethylcellulose, carboxypropylcellulose, polyacrylamide and its cogeners, and polyacrylic acid.

19. The adhesive patch of claim 17 wherein the humectant comprises a member selected from the group consisting of propylene glycol and glycerin.

20. The adhesive patch of claim 17 wherein the polymeric adhesive comprises an acrylic.

21. The adhesive patch of claim 20 wherein said acrylic is an acrylic ester copolymer.

22. The adhesive patch of claim 20 wherein the biomedically active substance comprises a member selected from the group consisting of trolamine salicylate, methyl salicylate, menthol, camphor, eucalyptus oil, spearmint oil, hydrocortisone, benzocaine, lidocaine, ibuprofen, salicylic acid, capsicum, anti-pruritic agents, anti-inflammatory agents, keratolytic agents, and rubefacient agents.

23. A medication-containing adhesive patch for the transdermal delivery of medication into the body of a patient through the skin comprising,

a flexible pressure-sensitive adhesive hydrocolloidal gel matrix including a natural or synthetic hydrophilic polymer and a biomedically active substance to be absorbed through the skin into the body of the patient,

a polyhydric alcohol selected from the group consisting of glycerin and propylene glycol dispersed in the matrix,

a hydrophilic resin emulsion adhesive dispersed in the matrix,

said biomedically active substance comprises a member selected from the group consisting of capsicum, eucalyptus oil and spearmint,

a porous backing for supporting the matrix, said backing comprising a sheet of water insoluble material having an upper surface and a lower surface,

said adhesive patch having the following layers proceeding from a lower surface of the adhesive patch to said upper surface of the backing:

a) an external layer of said adhesive matrix that is located below the lower surface of the backing, said external layer having an exposed surface for bonding to the skin of the patient,

b) an internal portion of the matrix partially penetrating the backing so as to be infiltrated within only a lower portion of the porous backing layer,

c) said backing layer includes a lower filled portion as a layer in which the internal portion of the matrix layer is infiltrated, and

d) an upper layer portion of the backing that is free of said matrix,

said biomedically active substance is dispersed in both portions of the matrix whereby the matrix releases the biomedically active substance into the skin through said exposed surface thereof, and

the backing has an upper surface that is spaced apart from the gel matrix.

24. A medication-containing adhesive patch for the transdermal delivery of medication into the body of a patient through the skin comprising,

a flexible pressure-sensitive adhesive hydrocolloidal gel matrix including a natural or synthetic hydrophilic polymer and a biomedically active substance to be absorbed through the skin into the body of the patient,

said polymer comprises a natural or synthetic polysaccharide,

a humectant comprising a polyhydric alcohol dispersed in said matrix,

a hydrophilic resin emulsion adhesive dispersed in the matrix,

the biomedically active substance comprises a member selected from the group of methyl salicylate, spearmint oil, camphor, eucalyptus oil, menthol, trolamine salicylate, and capsicum,

a porous backing for supporting the matrix, said backing comprising a sheet of water insoluble material having an upper surface and a lower surface,

said adhesive patch having the following layers proceeding from a lower surface of the adhesive patch to said upper surface of the backing:

a) an external layer of said adhesive matrix that is located below the lower surface of the backing, said external layer having an exposed surface for bonding to the skin of the patient,

b) an internal portion of the matrix partially penetrating the backing so as to be infiltrated within only a lower portion of the porous backing layer,

c) said backing layer includes a lower filled portion as a layer in which the internal portion of the matrix layer is infiltrated, and

d) an upper layer portion of the backing that is free of said matrix,

said biomedically active substance is dispersed in both portions of the matrix whereby the matrix releases the biomedically active substance into the skin through said exposed surface thereof, and

the backing has an upper surface that is spaced apart from the gel matrix.