Pharmaceutical compositions comprising benzyl alcohol

• US 9,999,670 B2
• Filed: 03/13/2013
• Issued: 06/19/2018
• Est. Priority Date: 03/19/2012
• Status: Active Grant

• Current Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Original Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Inventors: Perry, Jason M., Hickey, Magali B., Remenar, Julius F., Vandiver, Jennifer
• Primary Examiner(s): Kim, Jennifer M
• Application Number:
  US13/801,344
• Publication Number:
  US 20130267505A1
• Time in Patent Office: 1,924 Days
• Field of Search: 514220, 51425307, 51425404
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 31/497 containing further heterocyclic rings
• CPC Class Codes: A61K 31/551 having two nitrogen atoms, e.g. dilazep
• CPC Class Codes: A61K 31/5513 1,4-Benzodiazepines, e.g. diazepam or clozapine
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• 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 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• 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
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention relates to a pharmaceutical composition comprising benzyl alcohol and polyoxyethylene derivatives of sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.

Claims

1. A pharmaceutical composition consisting of:

(a) compound A-7;

2. The composition of claim 1, wherein (b) and (c) are present at a ratio that results in flocs comprising component (a) wherein the flocs settle to greater than a predetermined sediment bed height, such that components (a), (b) and (c) can be resuspended for injection.

3. The composition of claim 2, wherein the bed height has at least a 20 to 80% higher sediment height compared to a non-flocculated composition after 24 hours of undisturbed sitting.

4. The composition of claim 2, wherein the ratio of (b) to (c) is such that the composition can be injected using a 20 or greater gauge needle.

5. The composition of claim 2, wherein the ratio of (b) to (c) is approximately 4.5 to 1, by weight.

6. The composition of claim 2, wherein the concentration of (a) is approximately 15-35%.

8. A method for treating disorders of the central nervous system, comprising administering an effective amount of the composition of claim 1 to an individual in need of such treatment.

10. The composition of claim 1, wherein the sterile saline solution is phosphate-buffered saline.

7. An injectable pharmaceutical composition consisting of:

(a) approximately 15-35% compound A-7;

11. The composition of claim 7, wherein the sterile saline solution is phosphate-buffered saline.

9. A pharmaceutical composition consisting of:

(a) 15-35% compound A-7;

12. The composition of claim 9, wherein the sterile saline solution is phosphate-buffered saline.