Polyvinylpyrrolidone For The Stabilization Of A Solid Dispersion Of The Non-Crystalline Form Of Rotigotine

Abstract

The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a nom-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

1 . A method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. 
     
     
         2 . The method of  claim 1 , wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:4.5. 
     
     
         3 - 13 . (canceled) 
     
     
         14 . A method for preparing a transdermal therapeutic system, the method comprising preparing a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone (PVP), wherein the weight ratio of rotigotine to PVP is in a range from about 9:3.5 to about 9:6. 
     
     
         15 . The method of  claim 14 , wherein the weight ratio of rotigotine to (PVP) is in a range from about 9:3.5 to about 9:4.5. 
     
     
         16 . The method of  claim 14 , wherein the rotigotine is rotigotine free base. 
     
     
         17 . The method of  claim 16 , further comprising mixing rotigotine free base and the PVP in a solution to obtain the dispersed phase. 
     
     
         18 . The method of  claim 14 , wherein the PVP has a molecular weight of 1,000,000 to 1,500,000 g/mol. 
     
     
         19 . The method of  claim 14 , wherein the dispersing agent comprises at least one silicone pressure sensitive adhesive. 
     
     
         20 . The method of  claim 19 , wherein the dispersing agent comprises a mixture of at least two silicone pressure sensitive adhesives. 
     
     
         21 . The method of  claim 20 , wherein the mixture of at least two silicone pressure sensitive adhesives comprises BIO-PSA® Q7 4301 and BIO-PSA® Q7 4201. 
     
     
         22 . The method of  claim 14 , wherein the dispersing agent comprises at least a first adhesive having a complex viscosity between 40 and 250 MP. 
     
     
         23 . The method of  claim 14 , wherein the dispersing agent comprises at least a second adhesive having a complex viscosity between 1 and 10 MP. 
     
     
         24 . The method of  claim 14 , wherein the dispersing agent has a complex viscosity between 5 and 25 MP. 
     
     
         25 . The method of  claim 14 , wherein the dispersing agent comprises at least a first adhesive and a second adhesive and the solid dispersion has a complex viscosity between 5 and 15 MP. 
     
     
         26 . The method of  claim 14 , wherein the dispersing agent comprises at least a first adhesive and a second adhesive and the solid dispersion has a peel adhesion between 3 and 16 N/50 mm at a thickness of 50 g/m 2  and/or a peel adhesion between 14 and 26 N/50 mm at a thickness of 150 g/m 2 . 
     
     
         27 . The method of  claim 14 , wherein the dispersing agent comprises at least a first adhesive and a second adhesive and the solid dispersion has a static shear adhesion between 20 and 150 min.