ARIPIPRAZOLE FORMULATIONS HAVING INCREASED INJECTION SPEEDS

• US 20190167673A1
• Filed: 02/08/2019
• Published: 06/06/2019
• Est. Priority Date: 03/20/2014
• Status: Active Grant

• Current Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Original Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Inventors: Hickey, Magali B., Vandiver, Jennifer
• Granted Patent: US 10,813,928 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants

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.

Claims

1-21. -21. (canceled)

22. A method of treating 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 rate, wherein said pharmaceutical composition comprises:

(a) 24-30 weight percent of a compound of Formula (I);

23. The method of claim 22, wherein the said pharmaceutical composition comprises:

(a) about 26.6 weight percent Compound 1;

24. The method of claim 22, wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.

25. The method of claim 22, 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.

26. The method of claim 22, wherein the intramuscular injection rate is selected from the group consisting of:

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.

27. A method of treating bipolar disorder 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 rate, wherein said pharmaceutical composition comprises:

(a) 24-30 weight percent of a compound of Formula (I);

28. The method of claim 27, wherein the said pharmaceutical composition comprises:

(a) about 26.6 weight percent Compound 1;

29. The method of claim 27, wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.

30. The method of claim 27, 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.

31. The method of claim 27, wherein the intramuscular injection rate is selected from the group consisting of:

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.

32. A method of treating depression 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 rate, wherein said pharmaceutical composition comprises:

(a) 24-30 weight percent of a compound of Formula (I);

33. The method of claim 32, wherein the said pharmaceutical composition comprises:

(a) about 26.6 weight percent Compound 1;

34. The method of claim 32, wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.

35. 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.

36. The method of claim 32, wherein the intramuscular injection rate is selected from the group consisting of:

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.

37. A kit for the treatment of schizophrenia in a subject in need thereof, 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, wherein said pharmaceutical composition comprises:

(a) 24-30 weight percent of a compound of Formula (I);

38. The kit of claim 37, wherein the said pharmaceutical composition comprises:

(e) about 26.6 weight percent Compound 1;

39. The kit of claim 37, wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.

40. The kit of claim 37, 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.

41. The kit of claim 37, wherein the intramuscular injection rate is selected from the group consisting of:

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.