Adhesive mixture for transdermal delivery of highly plasticizing drugs
View Patent ↗Transdermal drug delivery patches and methods of their production are described. The patches can be made such that the accommodate highly plasticizing drugs such as selegiline and/or the use of protonated forms of various drugs.
1. A therapeutic adhesive formulation comprising:
between about 65% and about 97%, by weight, of an acrylic polymeric adhesive which includes between about 40% and about 90% of a C 4 –C 12 alkyl acrylate, between about 10% and about 40% by weight of a C 1 –C 4 alkyl acrylare hardening monomer; between about 1% and about 20% by weight of a monomer which provides functional groups for crosslinking; and a crosslinking agent; and
between about 3% and about 35% by weight, based on the weight of said mixture, of a highly plasticizing drug.
2. The therapeutic adhesive formulation of claim 1 wherein said C 4 –C 12 alkyl acrylare is selected from the group consisting of 2-ethylhexyl acrylate, butyl acrylate, n-decyl, n-nonyl, 2 ethyoctyl, isooctyl and dodecyl-acrylate.
3. The therapeutic adhesive formulation of claim 1 wherein said C 4 –C 12 alkyl acrylate is provided in an amount of between about 60% and about 80% by weight based on the weight of the adhesive.
4. The therapeutic adhesive formulation of claim 2 wherein said C 1 –C 4 alkyl acrylate hardening monomer is selected from the group consisting of methyl acrylate, methyl methacrylate, ethylacrylate, ethyl methacrylate, hydroxyethyl acrylate and hydroxy propyl methacrylate.
5. The therapeutic adhesive formulation of claim 1 wherein said C 1 –C 4 alkyl acrylate hardening monomer is provided in an amount of between about 15% and about 30% by weight based on the weight of the adhesive.
6. The therapeutic adhesive formulation of claim 1 wherein said functionalizing monomer which facilitates crosslinking is selected from the group consisting of acrylic acid, hydroxy ethylacrylate, methacrylic acid and acrylamide.
7. The therapeutic adhesive formulation of claim 1 wherein said functionalizing monomer which facilitates crosslinking is provided in an amount of between about 3% and about 8% by weight based on the weight of the adhesive.
8. The therapeutic adhesive formulation of claim 1 wherein said highly plasticizing drug is selected from the group consisting of selegiline, fluoxetine, Des-methyl selegiline, tetracaine and chlorpheniramine.
9. The therapeutic adhesive formulation of claim 8 wherein said highly plasticizing drug is selegiline.
10. The therapeutic adhesive formulation of claim 1 wherein said highly plasticizing drug is provided in an amount of between about 3% and about 25% by weight of the finished adhesive& and drug mixture.
11. The therapeutic adhesive formulation of claim 10 wherein said highly plasticizing drug is provided in an amount of between about 3% and about 18% by weight of the finished adhesive and drug mixture.
12. The therapeutic adhesive formulation of claim 11 wherein said crosslinking agent is selected from the group consisting of butyl titinate, polybutyl titinate, aluminum isopropoxide, butyl titinate, aluminum zinc acetate, multivalent metals, methylol ureas and melamines.
13. The therapeutic adhesive formulation of claim 12 wherein said crosslinking agent is provided in an amount of between about 0.005% and about 2.0% based on the weight of the adhesive.
14. The therapeutic adhesive formulation of claim 1 wherein said formulation is anhydrous and substantially free of volatile solvents after drying.
15. A drug containing and releasing adhesive mixture comprising:
between about 65% and about 97%, by weight of an acrylic polymeric adhesive which includes between about 60% and about 80% of a C 4 –C 12 alkyl acrylate selected from the group consisting of 2-ethylhexyl acrylate, butyl acrylate, n-decyl, n-nonyl, 2 ethyoctyl, isooctyl and dodecyl-acrylate; between about 15% and about 30% by weight of a C 1 –C 4 alkyl acrylate hardening monomer selected front the group consisting of methyl acrylate, methyl methacrylate, ethylacrylate, ethyl methacrylate, hydroxyethyl acrylate and hydroxy propyl methacrylate; between about 1% and about 20% by weight of a functionalizing monomer which facilitates crosslinking selected from the group consisting of acrylic acid, hydroxy ethylacrylate, methacrylic acid and acrylamide; and a crosslinking agent provided in an amount of between about 0.005% and about 2.0%; and
between about 3% and about 35% by weight, based on the weight of said mixture, of a highly plasticizing drug selected from the group consisting of selegiline, fluoxetine, des-methyl selegiline, tetracaine and chlorpheniramine.
16. The therapeutic adhesive formulation of claim 15 wherein said highly plasticizing drug is selegiline.
17. The therapeutic adhesive formulation of claim 15 which does not include a solvent after drying.