Granted Patent B2

US 12,653,822 · App. 18/440,388 · Granted Jun 16, 2026

Inventors: Magali B. Hickey (Westwood, MA); Jennifer Vandiver (Arlington, MA)

Assignee: Alkermes Pharma Ireland Limited

A61K31/496A61K9/0019A61K31/00A61K47/26

Abstract

Claims (37)

1 . A method of treating a disorder of the central nervous system in a subject in need thereof comprising intramuscular administration of a therapeutically effective amount of a pharmaceutical composition to the subject at an injection rate greater than or equal to 0.3 mL/s, wherein said pharmaceutical composition comprises:

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

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

the disorder of the central nervous system is selected from the group consisting of schizophrenia, anxiety, depression, bipolar disorder, autism-related irritability, and acute mania.

2 . The method of claim 1 , wherein the said pharmaceutical composition comprises:

(a) about 26.6 weight percent Compound 1:

(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 intramuscular injection rate is greater than 0.3 mL/s.

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

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

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

7 . The method of claim 5 , wherein the needle is a 21 gauge needle.

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

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

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

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

12 . The method of claim 1 , wherein the method does not elicit any injection site reactions in the subject above a normal threshold in the subject.

13 . The method of claim 12 , wherein the symptoms of the injection site reaction include but is not limited to redness, tenderness, warmth, itching, pain at injection site, blistering, nodule formation, and severe skin damage.

14 . The method of claim 1 , wherein approximately 3.4 mL of the pharmaceutical composition is injected within 10 seconds or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.

15 . 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.

16 . A method of treating a disorder of the central nervous system in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically amount of a pharmaceutical composition at an intramuscular injection rate greater than or equal to 0.3 mL/s, wherein said pharmaceutical composition comprises:

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

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

the disorder of the central nervous system is selected from the group consisting of schizophrenia, anxiety, depression, and bipolar disorder.

17 . The method of claim 16 , wherein the disorder is schizophrenia.

18 . The method of claim 16 , wherein the intramuscular injection rate is greater than 0.3 mL/s.

Assignments (3)

Continuity (9)

References Cited (240)