Claims for Patent: 10,130,589

Summary for Patent: 10,130,589

Title:	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 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. 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.
Inventor(s):	Wolff; Hans-Michael (Monheim, DE), Arth; Christoph (Monheim, DE), Quere; Luc (Braine-l'Alleud, BE), Muller; Walter (Andernach, DE)
Assignee:	UCB Pharma GmbH (Monheim, DE) LTS Lohmann Therapie-Systeme AG (Andernach, DE)
Application Number:	15/884,587
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,130,589
Patent Claims:	1. A method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine free base, wherein the weight ratio of rotigotine free base to polyvinylpyrrolidone is in a range from about 9:4 to about 9:6. 2. A solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine free base and polyvinylpyrrolidone, wherein the weight ratio of rotigotine free base to polyvinylpyrrolidone is in a range from about 9:4 to about 9:6. 3. The solid dispersion of claim 2, wherein the solubility of rotigotine free base in the dispersing agent is below 1 wt-%. 4. The solid dispersion of claim 2, wherein the dispersing agent comprises at least one silicone pressure sensitive adhesive. 5. The solid dispersion of claim 2, wherein the dispersing agent comprises a mixture of a first silicone pressure sensitive adhesive and a second silicone pressure sensitive adhesive and wherein the solid dispersion has a complex viscosity between 5 and 15 MP. 6. The solid dispersion of claim 2, wherein rotigotine free base and polyvinylpyrrolidone are in a multitude of microreservoirs. 7. A pharmaceutical composition comprising a solid dispersion according to claim 2. 8. A transdermal therapeutic system comprising at least one amine-compatible silicone pressure sensitive adhesive, about 0.1 to about 3.15 mg/cm' of rotigotine free base, and polyvinylpyrrolidone, wherein the weight ratio of rotigotine free base to polyvinylpyrrolidone is in a range from about 9:4 to about 9:6. 9. The transdermal therapeutic system of claim 8, wherein rotigotine free base and polyvinylpyrrolidone are contained in a multitude of microreservoirs. 10. A transdermal therapeutic system comprising a solid dispersion of claim 2. 11. 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 free base and polyvinylpyrrolidone, wherein the weight ratio of rotigotine free base to polyvinylpyrrolidone is in a range from about 9:4 to about 9:6. 12. The method of claim 1, wherein the solid dispersion further comprises a dispersing agent. 13. The method of claim 12, wherein the dispersing agent comprises at least a first adhesive having a complex viscosity between 40 and 250 MP. 14. The method of claim 13, wherein the dispersing agent comprises at least a second adhesive having a complex viscosity between 1 and 10 MP. 15. The method of claim 14, wherein the dispersing agent has a complex viscosity between 5 and 25 MP. 16. The method of claim 12, 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. 17. The method of claim 12, 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.sup.2 and/or a peel adhesion between 14 and 26 N/50 mm at a thickness of 150 g/m.sup.2. 18. The method of claim 12, 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. 19. The solid dispersion of claim 2, wherein the dispersing agent comprises at least a first adhesive having a complex viscosity between 40 and 250 MP. 20. The solid dispersion of claim 2, wherein the dispersing agent comprises at least a second adhesive having a complex viscosity between 1 and 10 MP. 21. The solid dispersion of claim 20, wherein the dispersing agent has a complex viscosity between 5 and 25 MP. 22. The solid dispersion of claim 2, 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. 23. The solid dispersion of claim 2, 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.sup.2 and/or a peel adhesion between 14 and 26 N/50 mm at a thickness of 150 g/m.sup.2. 24. The solid dispersion of claim 2, 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.