Transdermal Therapeutic System

• US 20070166364A1
• Filed: 03/19/2007
• Published: 07/19/2007
• Est. Priority Date: 12/06/2000
• Status: Abandoned Application

• Current Assignee: Cornelia Beier, Ralf Kibele
• Original Assignee: Cornelia Beier, Ralf Kibele
• Inventors: Kibele, Ralf, Beier, Cornelia
• Application Number:
  US11/687,771
• Publication Number:
  US 20070166364A1
• Time in Patent Office: Days
• US Class Current: 424/449
• 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: Y10S 602/90 Method of making bandage structure
• CPC Class Codes: Y10T 428/14 Layer or component removable to expose adhesive
• CPC Class Codes: Y10T 428/1405 Capsule or particulate matter containing [e.g., sphere, flake, microballoon, etc.]
• CPC Class Codes: Y10T 428/1414 Ceramic, glass, glasslike, vitreous
• CPC Class Codes: Y10T 428/1438 Metal containing
• CPC Class Codes: Y10T 428/1452 Polymer derived only from ethylenically unsaturated monomer
• CPC Class Codes: Y10T 428/1471 Protective layer
• CPC Class Codes: Y10T 428/1486 Ornamental, decorative, pattern, or indicia
• CPC Class Codes: Y10T 428/25 Web or sheet containing structurally defined element or component and including a second component containing structurally defined particles
• CPC Class Codes: Y10T 428/252 Glass or ceramic [i.e., fired or glazed clay, cement, etc.] [porcelain, quartz, etc.]
• CPC Class Codes: Y10T 428/254 Polymeric or resinous material

Abstract

This present invention concerns a cover layer that is impermeable to the active substances and/or a removable protective layer of a transdermal therapeutic system, comprising a thermoplastic film which either directly contains the absorbing agents and channel-forming agents or is coated with a polymer support (thermoplast) containing these substances. The polymer support can either be applied over the entire surface of the film or in patterns, directly during production. The thermoplastic film that is used and the polymer support can be made from either the same or different materials.

Claims

1. A transdermal therapeutic system, wherein such system is a matrix system with

a cover layer that is impermeable to active substances;

one or more active substance-containing self-adhesive matrix layers or one or more active substance-containing layers that have been coated with a pressure-sensitive adhesive; and

a removable protective layer,

wherein the cover layer or the protective layer or both are made from at least one polymer and an embedded absorbing agent and channel-forming agent, or

wherein the cover layer or the protective layer or both are a film that has been coated with a polymer support over the entire surface or in patterns, wherein the polymer support contains a mixture of at least one polymer, channel-forming agent, and absorbing agent.

2. The transdermal therapeutic system of claim 1, wherein the cover layer or the protective layer or both have been coated with a polymer support consisting of at least one thermoplast, at least one channel-forming agent, and at least one absorbing agent.

3. The transdermal therapeutic system of claim 1, wherein the cover layer or the protective layer or both have been coated, whether in a cold or hot state, with a polymer support consisting of

(i) at least one thermally crosslinkable polymer, at least one channel-forming agent, and at least one absorbing agent, or

(ii) at least one polymer which can be crosslinked by means of radiation, at least one channel-forming agent, and at least one absorbing agent, and in either case, the crosslinking has been performed thereinafter.

4. The transdermal therapeutic system of claim 1, wherein the film used for the cover layer that is impermeable to the active substances is coated with the polymer support on its top side or bottom side or on both sides.

5. The transdermal therapeutic system of claim 1, wherein the film that is used for the removable protective layer is coated with the polymer support on its outward-facing side.

6. The transdermal therapeutic system of claim 1, wherein a thermoplast or a crosslinkable or crosslinked polymer is the polymer in the mixture of the polymer, absorbing agent, and channel-forming agent.

7. The transdermal therapeutic system of claim 1, wherein the polymer is selected from the group consisting of a polyolefin, polyisoprene, polybutadiene, polybutene, polysiloxane, polyamide, ethylene vinyl acetate copolymer, ethylene methacrylate copolymer, polystyrene, polyester, polyanhydride, polyacrylate nitrile, polyacryl nitrile, polysulfonate, polyesteramide, polyacrylate ester, polypylene maleic anhydride, polyethylene maleic anhydride, polyethylene urethane, polyethylene ethyl vinyl alcohol, polyethylene nylon, polyurethane and mixtures thereof.

8. The transdermal therapeutic system of claim 7, wherein the polymer is polyethylene or polypropylene or a mixture thereof.

9. The transdermal therapeutic system of claim 1, wherein the channel-forming agent is selected from the group consisting of polyglycols, ethyl vinyl alcohols, glycerin, pentaerythritol, polyvinyl alcohols, polyvinyl pyrrolidone, vinyl pyrrolidone, N-methylpyrrolidone, polysaccharides, saccharides, sugar alcohols and mixtures thereof.

10. The transdermal therapeutic system of claim 9, wherein the channel-forming agent is a mixture of at least one polyglycol, saccharide, and sugar alcohol, wherein

the polyglycol is polyethylene glycol or polypropylene glycol or a mixture thereof;

the saccharide is glucose, mannose, galactose or fructose or a mixture thereof; and

the sugar alcohol is mannitol, sorbitol, hexitol, dulcitol, xylitol, ribitol, or erythrol or a mixture thereof.

11. The transdermal therapeutic system of claim 1, wherein the absorbing agent is a substance for the absorption of humidity, oxygen or of substances which are released by a transdermal therapeutic system during storage.

12. The transdermal therapeutic system of claim 1, wherein the absorbing agent is selected from the group consisting of a drying agent, a metal, an alloy, a metal-coated particle, an inorganic substance, an ion-exchange resin, a substance based on carbon, an elastomer, a semi-metal, a ceramic material and mixtures thereof.

13. The transdermal therapeutic system of claim 12, wherein

the drying agent is selected from the group consisting of molecular sieves, silicon gels, earths, synthetic polymers, starches or mixtures thereof;

the metal is selected from the group consisting of nickel, copper, aluminum, gold and alloys thereof;

the metal-coated particle is selected from the group consisting of silver-coated copper, silver-coated nickel, silver-coated glass microspheres and mixtures thereof;

the inorganic substance is selected from the group consisting of barium titanium trioxide, strontium titanium trioxide, silicon dioxide, aluminum oxide, zinc oxide, titanium dioxide, manganese oxide, copper oxide, antimony oxide, molten or melted silicon, amorphous molten or amorphous melted silicon, ion-exchange resins, lithium-containing metal oxides, hollow glass microspheres, silicon sol-gel, titanium sol-gel, mixed titanium and mixtures thereof;

the carbon-based substance is selected from the group consisting of carbon, activated charcoal, diamond powder, and mixtures thereof; and

the elastomer is polybutadiene or polysiloxane or a mixture thereof.

14. The transdermal therapeutic system of claim 13, wherein montmorrillonite earth or montmorrillonite earth polymers with a pore size of 3 to 15 Å

or silicon dioxide gel with a pore size of approximately 24 Å

are used as drying agents.

15. The transdermal therapeutic system of claim 1, wherein the thickness of the cover layer or protective layer is 5 to 100 μ

m.

16. The transdermal therapeutic system of claim 1, wherein the cover layer, the protective layer or both have a polymer content of 10 to 90 percent by weight, based on the total weight of the mixture of the polymer, channel-forming agent, and absorbing agent.

17. The transdermal therapeutic system of claim 1, wherein the channel-forming agent is a hydrophilic substance, wherein the content of the channel-forming agent is 10 to 40 percent by weight based on the total weight of the mixture of the polymer, channel-forming agent and absorbing agent.

18. The transdermal therapeutic system of claim 1, wherein the content of the absorbing agent is from 10 to 70 percent by weight based on the total weight of the mixture of the polymer, channel-forming agent and absorbing agent.

19. The transdermal therapeutic system of claim 3, wherein the radiation is UV radiation.

20. The transdermal therapeutic system of claim 10, wherein substances released by the transdermal system during storage are highly odorous substances.

21. The transdermal therapeutic system of claim 20, wherein the highly odorous substances are amines or polymers monomers.

22. The transdermal therapeutic system of claim 15, wherein the thickness of the cover layer or the protective layer is 15 to 40 μ

m.

23. The transdermal therapeutic system of claim 22. wherein the thickness of the cover layer or the protective layer is 15 μ

m.

24. The transdermal therapeutic system of claim 12, wherein the substance based on carbon is based on elemental carbon.

25. The transdermal therapeutic system of claim 1, further comprising a pressure-sensitive adhesive layer.

26. A method for producing a transdermal therapeutic system of claim 1, wherein said system is a matrix system comprising applying to a removable protective layer or a layer that is impermeable to active substances,

a polymer support containing an absorbing agent and a channel-forming agent thereby producing a transdermal therapeutic system wherein said system is a matrix system, wherein the polymer support is applied either over the entire surface or in patterns.

27. The method of claim 26, wherein the top side or bottom side or both sides of the layer that is impermeable to active substances is coated with the polymer support.

28. The method of claim 26, wherein the outside of the removable protective layer is coated with the polymer support.

29. The method of claim 26, further comprising applying one or several self-adhesive matrix layers.

30. The method of claim 26, further comprising coating the matrix system with a pressure-sensitive adhesive.

31. A method for producing a transdermal therapeutic system of claim 1, wherein said system is a matrix system comprising incorporating into a layer that is impermeable to active substances or a removable protective layer or both,

an absorbing agent and channel-forming agent thereby producing a transdermal therapeutic system wherein said system is a matrix system.