Adhesive mixture for transdermal delivery of highly plasticizing drugs

Abstract

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 transdermal delivery system comprising a blend of
 (a) one or more hydrophobic adhesive polymers;   (b) a therapeutically effective amount of one or more drugs, at least one of which is of low molecular weight and liquid at or about room temperature; and   (c) a solvent system including at least one solvent, said solvent system being free of low volatility solvents which are not driven off during drying of said transdermal delivery system at temperatures of from about 100° F. to 200° F.   
     
     
         2 . The transdermal delivery system of  claim 1  wherein said low volatility solvents are not driven off during drying of said transdermal delivery system at temperatures between about 100° F. and 140° F. 
     
     
         3 . The transdermal delivery system of  claim 1  wherein said one or more drugs comprise one or more highly plasticizing drugs. 
     
     
         4 . The transdermal delivery system of  claim 3  wherein said highly plasticizing drugs are selected from the group consisting of selegiline, fluoxetine, des-methyl selegiline, tetracaine and chlorpheniramine. 
     
     
         5 . The transdermal delivery system of  claim 1  wherein said one or more hydrophobic adhesive polymers comprise one or more acrylic polymers. 
     
     
         6 . The transdermal delivery system of  claim 1  including from about 3% to 35% by weight of said therapeutically effective amount of one or more drugs. 
     
     
         7 . The transdermal delivery system of  claim 4  wherein said highly plasticizing drug comprises selegiline. 
     
     
         8 . The transdermal delivery system of  claim 7  including from about 3% to 18% by weight of said selegiline. 
     
     
         9 . A transdermal delivery system comprising a blend of
 (a) one or more hydrophobic adhesive polymers; and   (b) a therapeutically effective amount of one or more drugs, at least one of which is of low molecular weight and liquid at or about room temperatures,   said system comprising solvents consisting essentially of at least one solvent which volatilizes during drying at a temperature of between about 100° F. and 200° F.   
     
     
         10 . The transdermal delivery system of  claim 9  wherein said solvents volatilize during drying at a temperature of between about 100° F. and 140° F. 
     
     
         11 . The transdermal delivery system of  claim 9  wherein said one or more drugs comprises one or more highly plasticizing drugs. 
     
     
         12 . The transdermal delivery system of  claim 1  wherein said highly plasticizing drugs are selected from the group consisting of selegiline, fluoxetine, des-methyl selegiline, tetracaine and chlorpheniramine. 
     
     
         13 . The transdermal delivery system of  claim 9  wherein said one or more hydrophobic adhesive polymers comprises acrylic polymers. 
     
     
         14 . The transdermal delivery system of  claim 9  comprising from about 3% to 35% by weight of said therapeutically effective amount of one or more drugs. 
     
     
         15 . The transdermal delivery system of  claim 12  wherein said drug comprises selegiline. 
     
     
         16 . The transdermal delivery system of  claim 15  including from about 3% to 18% by weight of said selegiline. 
     
     
         17 . A transdermal delivery system comprising a blend of
 (a) one or more hydrophobic acrylic adhesive polymers and one or more secondary adhesive polymers;   (b) a therapeutically effective amount of one or more drugs, at least one of which is of low molecular weight and liquid at or about room temperature; and   (c) a solvent system including at least one solvent,   said solvent system being free of low volatility solvents which are not driven off during drying of said transdermal delivery system at temperatures of from about 100° F. to 200° F.   
     
     
         18 . The transdermal delivery system of  claim 17  wherein said one or more secondary adhesive polymers is selected from the group consisting of silicones, polyisoalkylenes, rubbers, vinyl acetates, polyisobutylenes, polybutadiene, styrene-butadiene (or isoprene)-styrene block copolymer rubber, acrylic rubber, natural rubber, vinyl-based high molecular weight materials, polyvinyl acetate, polyvinyl alcohol, polyvinyl pyrrolidone; cellulose derivatives, polysaccharides, polyurethane elastomers and polyester elastomers. 
     
     
         19 . The transdermal delivery system of  claim 18  wherein said one or more secondary adhesive polymers are selected from the group consisting of polyisobutylenes and silicones. 
     
     
         20 . The transdermal delivery system of  claim 18  including from about 65% to 97% by weight of said one or more hydrophobic acrylic adhesive polymers. 
     
     
         21 . The transdermal delivery system of  claim 20  wherein said one or more hydrophobic acrylic polymeric adhesive polymers 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 3  alkyl acrylate hardening monomer. 
     
     
         22 . The transdermal delivery system of  claim 21  including between about 1% and about 20% by weight of a monomer which provides functional groups for crosslinking and a crosslinking agent. 
     
     
         23 . A transdermal delivery system comprising a blend of
 (a) one or more hydrophobic acrylic adhesive polymers and one or more secondary adhesive polymers; and   (b) a therapeutically effective amount of one or more drugs, at least one of which is of low molecular weight and liquid at or about room temperature,   said system comprising a solvent system consisting essentially of at least one solvent which volatilizes during drying of said transdermal delivery system at temperatures of from about 100° F. to 200° F.   
     
     
         24 . The transdermal delivery system of  claim 23  wherein said one or more secondary adhesive polymers is selected from the group consisting of silicones, polyisoalkylenes, rubbers, vinyl acetates, polyisobutylenes, polybutadiene, styrene-butadiene (or isoprene)-styrene block copolymer rubber, acrylic rubber, natural rubber, vinyl-based high molecular weight materials, polyvinyl acetate, polyvinyl alcohol, polyvinyl pyrrolidone; cellulose derivatives, polysaccharides, polyurethane elastomers and polyester elastomers. 
     
     
         25 . The transdermal delivery system of  claim 24  wherein said one or more secondary adhesive polymers is selected from the group consisting of polyisobutylenes and silicones.