IP Library Granted Patent US 9,193,685
Granted Patent B2
US 9,193,685 · App. 14/031,842 · Granted Nov 24, 2015

Pharmaceutical compositions having improved storage stability

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Quick Facts
Patent No.
US 9,193,685
App. No.
14/031,842
Granted
Nov 24, 2015
Kind
B2
Abstract

The present invention relates to a pharmaceutical composition that provides long-term stability of a hydrolytically labile antipsychotic agent

Claims (27)

1. A pharmaceutical composition comprising:

(a) a hydrolytically labile antipsychotic agent;

(b) a non-ionic water insoluble or immiscible ester co-surfactant;

(c) a water miscible or soluble non-ionic surfactant; and

(d) an aqueous vehicle;

wherein the pharmaceutical composition comprises less than 50 parts per million of the hydrolysis product of the antipsychotic agent.

2. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises less than 30 parts per million of the hydrolyzed antipsychotic agent.

3. The pharmaceutical composition of claim 1 , wherein the non-ionic water insoluble or immiscible ester co-surfactant is a sorbitan ester of a carboxylic acid, wherein the carboxylic acid comprises 4-20 carbon atoms.

4. The pharmaceutical composition of claim 1 , wherein the water miscible or soluble non-ionic surfactant is a polyoxyethylene derivative of a sorbitan ester of a carboxylic acid, wherein the carboxylic acid comprises 8-14 carbon atoms.

5. The pharmaceutical composition of claim 1 , wherein the antipsychotic agent is Compound 1

6. The pharmaceutical composition of claim 5 , wherein the hydrolysis product is of one or more of the following formulas:

7. The pharmaceutical composition of claim 1 , wherein the water miscible or soluble non-ionic surfactant is a polyoxyethylene derivative of a sorbitan ester of a carboxylic acid, wherein the carboxylic acid comprises 8-14 carbon atoms.

8. The pharmaceutical composition of claim 7 , wherein the sorbitan ester is sorbitan laurate.

9. A pharmaceutical composition comprising:

(a) 24-30 weight percent Compound 1:

(b) 0.3-0.4 weight percent sorbitan laurate;

(c) 0.1-0.3 weight percent polysorbate 20; and

(d) an aqueous vehicle.

10. A pharmaceutical composition comprising:

(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.

11. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises less than 50 parts per million of the hydrolysis product of the antipsychotic agent after standing for at least 12 months.

12. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises less than 50 parts per million of the hydrolysis product of the antipsychotic agent after standing for at least 24 months.

13. The pharmaceutical composition of claim 1 , wherein the non-ionic water insoluble or immiscible ester co-surfactant is sorbitan laurate, and wherein the water miscible or soluble non-ionic surfactant is polysorbate 20.

14. A method for treating a disorder of the central nervous system, comprising administering an effective amount of the composition of claim 1 to an individual in need of such treatment, wherein the disorder of the central nervous system is schizophrenia or bipolar disorder.

Assignments (5)
SECURITY INTEREST Recorded Feb 13, 2026
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 074858/0405 →
RELEASE OF SECURITY INTEREST IN PATENTS PREVIOUSLY RECORDED AT REEL/FRAME (073213/0302) Recorded Feb 13, 2026
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 074858/0429 →
SECURITY INTEREST Recorded Oct 23, 2025
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 073213/0302 →
SECURITY INTEREST Recorded May 17, 2016
From: ALKERMES PHARMA IRELAND LIMITED
To: MORGAN STANLEY SENIOR FUNDING, INC.
Reel/Frame 038622/0248 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 10, 2013
From: PERRY, JASON M.; DEAVER, DANIEL R.; HICKEY, MAGALI B.; REMENAR, JULIUS F.; VANDIVER, JENNIFER; PALIMIERI, MICHAEL J., JR.; PAN, ZHENGZHENG
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 031748/0001 →