Claims for Patent: 12,383,493

Summary for Patent: 12,383,493

Title:	Drug delivery formulations
Abstract:	The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
Inventor(s):	Anthony RECH, Christophe Roberge, Eran HARARY
Assignee:	MedinCell SA , Teva Pharmaceutical Industries Ltd
Application Number:	US17/642,410
Patent Claims:	1. A method of treating a psychiatric disease or disorder in a subject, comprising subcutaneously administering to the subject with a frequency of no more than once every 21 days: 1 mL or less of a pharmaceutical formulation comprising: a) risperidone, or a pharmaceutically acceptable salt thereof, at a concentration of about 250-400 mg/mL, equivalent to risperidone; b) a biodegradable triblock copolymer having the formula: poly(lactic acid)v-poly(ethylene glycol)w,-poly(lactic acid)x wherein v and x are the number of repeat units ranging from 24 to 682 and w is the number of repeat units ranging from 4 to 273 and v=x or v≠x; c) a biodegradable diblock copolymer having the formula: methoxy poly(ethylene glycol)y-poly(lactic acid)z, wherein y and z are the number of repeat units, wherein y is the number of repeat units ranging from 3 to 45 and z is the number of units ranging from 7 to 327; and wherein the ratio of the biodegradable triblock copolymer of (b) and the biodegradable diblock copolymer of (c) is 1:3 to 1:8 or 1:1 to 1:19 or 3:2 to 1:19, in said formulation, which is insoluble in an aqueous environment. 2. The method of claim 1, wherein the risperidone is risperidone base. 3. The method of claim 1, wherein the concentration of the risperidone or the pharmaceutically acceptable salt thereof, is 300 mg/mL to 400 mg/mL, equivalent to risperidone. 4. The method of claim 1, wherein the triblock copolymer is present in an amount of about 3% to 20% (w/w %) of the total weight of the formulation. 5. The method of claim 4, wherein the triblock copolymer is present in an amount of about 5% to 15% (w/w %) of the total weight of the formulation. 6. The method of claim 1, wherein the diblock copolymer is present in an amount of about 8% to 25% (w/w %) of the total weight of the formulation. 7. The method of claim 6, wherein the diblock copolymer is present in an amount of about 10% to 20% (w/w %) of the total weight of the formulation. 8. The method of claim 1, wherein the triblock and diblock copolymers are present in a total amount of about 20% to about 50% (w/w %) of the total weight of the formulation. 9. The method of claim 8, wherein the triblock and diblock copolymers are present in a total amount of about 20% to 30% (w/w %) of the total weight of the formulation. 10. The method of claim 1, wherein the formulation further comprises a water soluble organic solvent that is DMSO. 11. The method of claim 10, wherein the formulation further comprises triacetin, tripropionin, or a mixture thereof. 12. The method of claim 10, wherein the organic solvent is present in an amount of about 35% to about 55% (w/w %) of the total weight of the formulation. 13. The method of claim 1, wherein the administration is effective in treating the subject's psychiatric disease or disorder for 21 days to 90 days. 14. The method of claim 1, wherein the administration is effective in treating the subject's psychiatric disease or disorder for 28 days to 90 days. 15. The method of claim 1, wherein the administration is effective in treating the subject's psychiatric disease or disorder for 28 days to 56 days. 16. The method of claim 1, wherein less than about 15 w % of the risperidone in the formulation is cumulatively released at 24 hours post administration. 17. The method of claim 16, wherein about 7 w % to about 15 w % of the risperidone in the formulation is cumulatively released at 24 hours post administration. 18. The method of claim 13, wherein about 50 w % to about 80 w % of the risperidone in the formulation is cumulatively released at 30 days post administration. 19. The method of claim 13, wherein about 70 w % to about 98% w % of the risperidone in the formulation is cumulatively released at 60 days administration. 20. The method of claim 13, wherein the cumulative release is determined by in vitro release (IVR) method disclosed herein. 21. The method of claim 1, wherein the psychiatric disease or disorder is schizophrenia or bipolar disorder. 22. The method of claim 1, wherein the method is implemented in the absence of a loading dose or supplemental oral risperidone. 23. The method of claim 1 which comprises treating the subject over a period of at least 6 months. 24. The method of claim 23, which comprises treating the subject over a period of at least 15 months. 25. The method of claim 1, wherein the formulation is presented in a single prefilled syringe (PFS). 26. The method of claim 25, wherein the volume in the prefilled syringe is between 0.1 mL and 0.8 mL. 27. The method of claim 1, wherein the administration is subcutaneous into the abdomen. 28. The method of claim 1, wherein the administration is subcutaneous into the upper arm. 29. The method of claim 1, wherein the formulation is excisable following administration into the subject. 30. A pharmaceutical formulation comprising 1 mL or less of: a) risperidone, or a pharmaceutically acceptable salt thereof, at a concentration of about 250-400 mg/mL, equivalent to risperidone; b) a biodegradable triblock copolymer having the formula: poly(lactic acid)v-poly(ethylene glycol)w,-poly(lactic acid)x wherein v and x are the number of repeat units ranging from 24 to 682 and w is the number of repeat units ranging from 4 to 273 and v=x or v≠x; c) a biodegradable diblock copolymer having the formula: methoxy poly(ethylene glycol)y-poly(lactic acid)z, wherein y and z are the number of repeat units, wherein y is the number of repeat units ranging from 3 to 45 and z is the number of units ranging from 7 to 327; and wherein the ratio of the biodegradable triblock copolymer of (b) and the biodegradable diblock copolymer of (c) is 1:3 to 1:8 or 1:1 to 1:19 or 3:2 to 1:19, in said formulation, which is insoluble in an aqueous environment, for use in treating a psychiatric disease or disorder.