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Last Updated: November 28, 2020

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Claims for Patent: 10,010,612

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Summary for Patent: 10,010,612
Title:Sustained delivery formulations of risperidone compounds
Abstract: The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating 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 the 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 (Furlong, PA), Li; Qi (Slough, GB), Lindemann; Christopher (Slough, GB)
Assignee: Indivior UK Limited (Slough, GB)
Application Number:12/602,058
Patent Claims: 1. A flowable composition comprising: 10 wt % to 20 wt % of risperidone base in a solution comprising (i) 40 wt % to 50 wt % of an 80/20 poly(DL-lactide-co-glycolide) with a carboxylic acid end group, and (ii) 50 wt % to 60 wt % of N-methyl-2-pyrrolidone.

2. The composition of claim 1, comprising about 60 mg of risperidone base.

3. The composition of claim 1, comprising about 90 mg of risperidone base.

4. The composition of claim 1, comprising about 120 mg of risperidone base.

5. The composition of claim 1, wherein the composition produces a maximum plasma concentration (C.sub.max) of risperidone and/or 9-hydroxyrisperidone within about 2 hours after injection into a patient.

6. The composition of claim 1, wherein the composition produces a steady state plasma level of risperidone and/or 9-hydroxyrisperidone within about three days after injection into a patient.

7. The composition of claim 1, wherein the composition produces a risperidone and/or 9-hydroxyrisperidone concentration of at least 15.8 ng/mL for about 28 days after injection into a patient.

8. The composition of claim 1, wherein the composition produces a linear sustained release of risperidone and/or 9-hydroxyrisperidone for at least 28 days.

9. The composition of claim 1, consisting of the risperidone base, the 80/20 poly(DL-lactide-co-glycolide) with the carboxylic acid end group, and the N-methyl-2-pyrrolidone.

10. The composition of claim 1, consisting of the risperidone base, the 80/20 poly(DL-lactide-co-glycolide) with the carboxylic acid end group, and the N-methyl-2-pyrrolidone.

11. The composition of claim 1, wherein the composition produces a steady state plasma level of risperidone and/or 9-hydroxyrisperidone from about three days to about forty-two days after injection into a patient.

12. The composition of claim 11, wherein the steady state plasma level of risperidone and/or 9-hydroxyrisperidone is from about 28.9 ng/ml to about 50.7 ng/ml.

13. The composition of claim 1, wherein the composition provides an AUC.sub.Dayo-1 of risperidone and/or 9-hydroxyrisperidone from about 63.1 ngday/ml to about 111.7 ngday/ml.

14. The composition of claim 1, wherein the composition provides an AUC.sub.Day0-42 of risperidone and/or 9-hydroxyrisperidone from about 1243.3 ngday/ml to about 2238.9 ngday/ml.

15. The composition of claim 1, wherein the composition provides an AUC.sub.Day0-56 of risperidone and/or 9-hydroxyrisperidone from about 1417.6 ngday/ml to about 3049.2 ngday/ml.

16. The composition of claim 1, wherein a dose normalized AUC.sub.Day0-42 of risperidone and/or 9-hydroxyrisperidone from about 15.9 ngday/mlmg to about 20.9 ngday/mlmg.

17. The composition of claim 1 having a volume from about 0.75 ml to about 1.0 ml.

18. A flowable composition comprising: (i) 1 wt % to 30 wt % of risperidone base; (ii) 20 wt % to 60 wt % of an 80/20 poly(DL-lactide-co-glycolide) with a carboxylic acid end group; and (iii) 30 wt % to 70 wt % of N-methyl-2-pyrrolidone.

19. The composition of claim 18, wherein the composition provides a linear sustained release of risperidone and/or 9-hydroxyrisperidone for at least 28 days.

20. The composition of claim 18, comprising about 60 mg to about 120 mg of risperidone base.

21. The composition of claim 18, wherein the composition provides (i) a maximum plasma concentration (C.sub.max) of risperidone and/or 9-hydroxyrisperidone occurs within about 2 hours after injection into a patient and (ii) a linear sustained release of risperidone and/or 9-hydroxyrisperidone for at least 28 days after injection into a patient.

22. The composition of claim 18, wherein the composition provides a risperidone and/or 9-hydroxyrisperidone concentration of at least 15.8 ng/mL for at least 28 days after injection into a patient.

23. The composition of claim 18, wherein the composition produces a steady state plasma level of risperidone and/or 9-hydroxyrisperidone about three days after injection into a patient.

24. The composition of claim 18, wherein the composition produces a risperidone or 9-hydroxyrisperidone concentration of at least 15.8 ng/mL for at least 28 days after injection into a patient.

25. The composition of claim 18, consisting of the risperidone base, the 80/20 poly(DL-lactide-co-glycolide) with the carboxylic acid end group, and the N-methyl-2-pyrrolidone.

26. The composition of claim 18 having a volume from about 0.75 ml to about 1.0 ml.

27. A method of forming a biodegradable implant in situ in a patient in need thereof comprising the steps of: (a) injecting the flowable composition of claim 1 into the body of the patient; and (b) allowing the N-methyl-2-pyrrolidone to dissipate to produce the implant in the body of the patient.

28. A composition comprising about 15 wt % of risperidone base in a solution comprising: (i) about 45 wt % of an 80/20 poly(DL-lactide-co-glycolide) with a carboxylic acid end group; and (ii) about 55 wt % of N-methyl-2-pyrrolidone.

29. The composition of claim 28, comprising about 60 mg of risperidone base.

30. The composition of claim 28, comprising about 90 mg of risperidone base.

31. The composition of claim 28, comprising about 120 mg of risperidone base.

32. The composition of claim 28 having a volume from about 0.75 ml to about 1.0 ml.

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