Claims for Patent: 10,376,590

Summary for Patent: 10,376,590

Title:	Sustained delivery formulations of risperidone compound
Abstract:	The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating to delusional psychosis, schizophrenia, bipolar disorder, psychotic depression, obsessive-compulsion disorder, Tourette syndrome, and autistic spectrum disorders. The sustained release delivery system includes a flowable composition containing risperidone, a metabolite, or a prodrug thereof and an implant containing risperidone, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become a solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite or a prodrug thereof.
Inventor(s):	Dadey; Eric (Sevierville, TN), Li; Qi (Fort Collins, CO), Lindemann; Christopher (Fort Collins, CO)
Assignee:	INDIVIOR UK LIMITED (Hull, GB)
Application Number:	15/858,525
Patent Claims:	1. A method of treating schizophrenia in a subject in need thereof, the method comprising subcutaneously injecting the subject with a composition comprising risperidone base in a solution comprising: (i) an 80/20 poly(DL-lactide-co-glycolide) copolymer having a carboxy terminal group, and (ii) N-methyl-2-pyrrolidone; to treat the schizophrenia. 2. The method of claim 1, comprising subcutaneously injecting the subject with the composition once every twenty-eight days. 3. The method of claim 1, comprising subcutaneously injecting the subject with the composition once per month. 4. The method of claim 1, wherein the composition comprises about 10 wt % to about 50 wt % of the risperidone base. 5. The method of claim 1, wherein the composition comprises about 10 wt % to about 30 wt % of the risperidone base. 6. The method of claim 1, wherein the composition comprises about 10 wt % to about 20 wt % of the risperidone base. 7. The method of claim 1, wherein the solution comprises: (i) about 10 wt % to about 70 wt % of the 80/20 poly(DL-lactide-co-glycolide) copolymer having a carboxy terminal group, and (ii) about 10 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 8. The method of claim 1, wherein the solution comprises: (i) about 20 wt % to about 70 wt % of the 80/20 poly(DL-lactide-co-glycolide) copolymer having a carboxy terminal group, and (ii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 9. The method of claim 1, wherein the solution comprises: (i) about 40 wt % to about 50 wt % of the 80/20 poly(DL-lactide-co-glycolide) copolymer, and (ii) about 50 wt % to about 60 wt % of N-methyl-2-pyrrolidone. 10. The method of claim 1, wherein the copolymer has an average molecular weight from about 10,000 Daltons to about 45,000 Daltons. 11. The method of claim 1, wherein the copolymer has an average molecular weight from about 15,000 Daltons to about 40,000 Daltons. 12. The method of claim 1, wherein the composition comprises about 90 mg of risperidone base. 13. The method of claim 1, wherein the composition comprises about 120 mg of risperidone base. 14. The method of claim 1, wherein the subject is not administered a supplemental daily oral dose of risperidone. 15. The method of claim 1, wherein the subject is not administered a supplemental daily oral dose of risperidone for the first twenty-one days of the method of treating schizophrenia. 16. The method of claim 1, wherein the method provides therapeutic plasma risperidone levels immediately after injection. 17. The method of claim 1, wherein the method provides steady-state risperidone plasma levels from four to six weeks. 18. The method of claim 1, wherein the composition comprises about 30 mg of risperidone base. 19. The method of claim 1, wherein the composition comprises about 60 mg of risperidone base. 20. The method of claim 1, wherein the composition comprises about 180 mg of risperidone base. 21. The method of claim 1, wherein the composition comprises from about 3 mg to about 300 mg of risperidone base. 22. The method of claim 1, wherein the composition comprises from about 9 mg to about 900 mg of risperidone base. 23. The method of claim 1, wherein the composition comprises about 15 wt % of the risperidone base in a solution comprising: (i) about 45 wt % of the 80/20 poly(DL-lactide-co-glycolide) copolymer, and (ii) about 55 wt % of N-methyl-2-pyrrolidone. 24. The method of claim 23, wherein the subject is not administered a supplemental daily oral dose of risperidone. 25. The method of claim 23, wherein the subject is not administered a supplemental daily oral dose of risperidone for the first twenty-one days of the method of treating schizophrenia. 26. The method of claim 23, wherein the method provides therapeutic plasma risperidone levels immediately after injection. 27. The method of claim 23, wherein the method provides steady-state risperidone plasma levels from four to six weeks. 28. The method of claim 23, wherein the composition comprises about 30 mg of risperidone base. 29. The method of claim 23, wherein the composition comprises about 60 mg of risperidone base. 30. The method of claim 23, wherein the composition comprises about 180 mg of risperidone base. 31. The method of claim 23, wherein the composition comprises from about 3 mg to about 300 mg of risperidone base. 32. The method of claim 23, wherein the composition comprises from about 9 mg to about 900 mg of risperidone base. 33. A method of treating schizophrenia in a subject in need thereof, the method comprising subcutaneously injecting the subject with a composition comprising about 10 wt % to about 30 wt % risperidone base in a solution comprising: (i) about 10 wt % to about 70 wt % of an 80/20 poly(DL-lactide-co-glycolide) copolymer having a carboxy terminal group, and (ii) about 10 wt % to about 70 wt % of N-methyl-2-pyrrolidone; to treat the schizophrenia. 34. The method of claim 33, comprising subcutaneously injecting the subject with the composition once per month. 35. The method of claim 33, wherein the composition comprises about 90 mg of risperidone base. 36. The method of claim 33, wherein the composition comprises about 120 mg of risperidone base. 37. The method of claim 33, wherein the subject is not administered a supplemental daily oral dose of risperidone. 38. The method of claim 33, wherein the subject is not administered a supplemental daily oral dose risperidone for the first twenty-one days of the method of treating schizophrenia. 39. The method of claim 33, wherein the method provides therapeutic plasma risperidone levels immediately after injection. 40. The method of claim 33, wherein the method provides steady-state risperidone plasma levels from four to six weeks. 41. The method of claim 33, wherein the composition comprises about 30 mg of risperidone base. 42. The method of claim 33, wherein the composition comprises about 60 mg of risperidone base. 43. The method of claim 33, wherein the composition comprises about 180 mg of risperidone base. 44. The method of claim 33, wherein the composition comprises from about 3 mg to about 300 mg of risperidone base. 45. The method of claim 33, wherein the composition comprises from about 9 mg to about 900 mg of risperidone base.