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Last Updated: October 31, 2020

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Claims for Patent: 10,238,651

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Summary for Patent: 10,238,651
Title:Aripiprazole formulations having increased injection speeds
Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.
Inventor(s): Hickey; Magali B. (Westwood, MA), Vandiver; Jennifer (Arlington, MA)
Assignee: ALKERMES PHARMA IRELAND LIMITED (Dublin, IE)
Application Number:16/116,652
Patent Claims: 1. A method of treating bipolar disorder, depression, or schizophrenia in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically effective amount of a pharmaceutical composition at a rapid and continuous injection rate, wherein said pharmaceutical composition comprises: (a) 24-30 weight percent of a compound of Formula (I): ##STR00048## wherein n is an integer between 4 and 14; (b) 0.3-0.4 weight percent sorbitan laurate; (c) 0.1-0.3 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and wherein the pharmaceutical composition has a total injection volume of about 1.5 mL, about 2 mL, about 2.5 mL, about 3 mL, about 3.5 mL, or about 4 mL.

2. The method of claim 1, wherein the said pharmaceutical composition comprises: (a) about 26.6 weight percent Compound 1: ##STR00049## (b) about 0.37 weight percent sorbitan laurate; (c) about 0.15 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.

3. The method of claim 1, wherein the administration is instantaneous.

4. The method of claim 1, wherein the pharmaceutical composition is injected using a 20 to 23 gauge needle.

5. The method of claim 4, wherein the needle is a 20 gauge needle.

6. The method of claim 4, wherein the needle is a 21 gauge needle.

7. The method of claim 1, wherein the injection is administered to the subject in the dorsal gluteal muscle.

8. The method of claim 1, wherein the injection is administered to the subject in the deltoid muscle.

9. The method of claim 1, wherein the needle does not experience injection failure due to needle clogging.

10. The method of claim 1, wherein the method does not elicit a pain intensity above a normal threshold in the subject.

11. The method of claim 1, wherein the total volume of the pharmaceutical composition is approximately 3.2 mL, 2.4 mL, or 1.6 mL.

12. The method of claim 1, wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.

13. The method of claim 1, wherein the intramuscular injection rate is selected from the group consisting of: 0.3 mL/s, 0.35 mL/s, 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.

14. A method of treating schizophrenia in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically amount of a pharmaceutical composition at a rapid and continuous intramuscular injection rate, wherein said pharmaceutical composition comprises: (a) 24-30 weight percent of a compound of Formula (I): ##STR00050## wherein n is an integer between 4 and 14; (b) 0.3-0.4 weight percent sorbitan laurate; (c) 0.1-0.3 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and wherein the pharmaceutical composition has a total injection volume of about 1.5 mL, about 2 mL, about 2.5 mL, about 3 mL, about 3.5 mL, or about 4 mL.

15. The method of claim 14, wherein the intramuscular injection rate is selected from the group consisting of: 0.3 mL/s, 0.35 mL/s, 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.

16. The method of claim 14, wherein the total volume of the pharmaceutical composition is approximately 3.2 mL, 2.4 mL, or 1.6 mL.

17. The method of claim 14, wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.

18. A kit useful for the treatment of bipolar disorder, depression, or schizophrenia, wherein the kit comprises a therapeutically effective amount of a pharmaceutical composition and further comprises instructions for intramuscular injection, wherein the instructions specify a rapid and continuous intramuscular injection rate, wherein said pharmaceutical composition comprises: (a) 24-30 weight percent Compound 1: ##STR00051## (b) 0.3-0.4 weight percent sorbitan laurate; (c) 0.1-0.3 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and wherein the pharmaceutical composition has a total injection volume of about 1.5 mL, about 2 mL, about 2.5 mL, about 3 mL, about 3.5 mL, or about 4 mL.

19. The kit according to claim 18, wherein the kit is adapted to be associated with a treatment regimen.

20. The kit of claim 18, wherein the said pharmaceutical composition comprises: (a) about 26.6 weight percent Compound 1: ##STR00052## (b) about 0.37 weight percent sorbitan laurate; (c) about 0.15 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.

21. The kit of claim 18, wherein the intramuscular injection rate is selected from the group consisting of: 0.3 mL/s, 0.35 mL/s, 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.

22. The kit of claim 18, wherein the total volume of the pharmaceutical composition is approximately 3.2 mL, 2.4 mL, or 1.6 mL.

23. The kit of claim 18, wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.

24. The method of claim 1, wherein the method comprises treating depression.

25. The method of claim 14, wherein the said pharmaceutical composition comprises: (a) about 26.6 weight percent Compound 1: ##STR00053## (b) about 0.37 weight percent sorbitan laurate; (c) about 0.15 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.

26. The method of claim 25, wherein the total volume of the pharmaceutical composition is approximately 3.2 mL, 2.4 mL, or 1.6 mL.

27. The method of claim 25, wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.

28. The method of claim 25, wherein the intramuscular injection rate is selected from the group consisting of: 0.3 mL/s, 0.35 mL/s, 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.

29. The kit of claim 18, wherein the kit is useful for the treatment of bipolar disorder.

30. The kit of claim 18, wherein the kit is useful for the treatment of depression.

31. The kit of claim 18, wherein the kit is useful for the treatment of schizophrenia.

32. A method of treating bipolar disorder in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically amount of a pharmaceutical composition at a rapid and continuous intramuscular injection rate, wherein said pharmaceutical composition comprises: 24-30 weight percent of a compound of Formula (I): ##STR00054## wherein n is an integer between 4 and 14; (e) 0.3-0.4 weight percent sorbitan laurate; (f) 0.1-0.3 weight percent polysorbate 20; and (g) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and wherein the pharmaceutical composition has a total injection volume of about 1.5 mL, about 2 mL, about 2.5 mL, about 3 mL, about 3.5 mL, or about 4 mL.

33. The method of claim 32, wherein the total volume of the pharmaceutical composition is approximately 3.2 mL, 2.4 mL, or 1.6 mL.

34. The method of claim 32, wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.

35. The method of claim 32, wherein the intramuscular injection rate is selected from the group consisting of: 0.3 mL/s, 0.35 mL/s, 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.

36. The method of claim 32, wherein the said pharmaceutical composition comprises: (a) about 26.6 weight percent Compound 1: ##STR00055## (b) about 0.37 weight percent sorbitan laurate; (c) about 0.15 weight percent polysorbate 20; and (d) an aqueous vehicle wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.

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