Aripiprazole oral solution

• US 6,977,257 B2
• Filed: 04/24/2002
• Issued: 12/20/2005
• Est. Priority Date: 04/25/2001
• Status: Expired due to Term

• Current Assignee: Otsuka Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
• Original Assignee: Bristol-Myers Squibb Company
• Inventors: Parab, Prakash V., Chou, Joyc Tianw i
• Primary Examiner(s): Spivack, Phyllis G.
• Application Number:
  US10/131,304
• Publication Number:
  US 20020193438A1
• Time in Patent Office: 1,336 Days
• Field of Search: 514/253.07
• US Class Current: 514/253.07
• 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 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Abstract

The present invention provides for a pharmaceutical solution suitable for oral administration comprising aripiprazole, a pharmaceutically suitable solvent system, one or more taste-enhancing/masking agents and one or more agents selected from the group consisting of lactic acid, acetic acid, tartaric acid and citric acid, wherein said solution has a pH from 2.5 to 4.5.

Claims

1. A pharmaceutical solution suitable for oral administration comprising aripiprazole, a pharmaceutically suitable solvent system comprised of one or more agents selected from the group consisting of water, ethanol, glycerin, propylene glycol and sorbitol, one or more taste-enhancing/masking agents and one or more other agents selected from the group consisting of lactic acid, acetic acid, tartaric acid and citric acid, wherein said solution has a pH from 2.5 to 4.0.

2. A pharmaceutical solution according to claim 1 wherein said other agent is lactic acid.

3. A pharmaceutical solution according to claim 2 wherein said lactic acid is present at concentrations selected from the group of ranges consisting of 0.7 mg/ml to 18 mg/ml, 3.5 mg/ml to 14.5 mg/ml and 5.4 mg/ml to 9 mg.

4. A pharmaceutical solution according to claim 1 wherein aripiprazole is present at concentrations selected from the group of ranges consisting of 0.05 mg/ml to 6 mg/ml, 0.1 mg/ml to 3 mg/ml, 0.25 mg/ml to 2 mg/ml and 0.75 mg/ml to 1.5 mg/ml.

5. A pharmaceutical solution according to claim 1 wherein said pharmaceutically suitable solvent system is comprised of propylene glycol, glycerin and water each being present in ratios of 0.8-1.2:

2.4-3.6;

6.4-9.6 w/w respectively.

6. A pharmaceutical solution according to claim 1 wherein said pharmaceutically suitable solvent system is comprised of glycerin, propylene glycol and water each being present in ratios of 0.8-1.2:

2.4-3.6;

6.4-9.6 w/w respectively.

7. A pharmaceutical solution according to claim 1 wherein said pharmaceutically suitable solvent system is comprised of glycerin and water each being present in ratios of 0.8-1.2:

6.4-8.6 w/w respectively.

8. A pharmaceutical solution according to claim 1 wherein said pharmaceutically suitable solvent system is comprised of glycerin and water each being present in ratios of about 1:

3 w/w respectively.

9. A pharmaceutical solution according to claim 1 further comprising disodium EDTA.

10. A pharmaceutical solution suitable for oral administration comprising aripiprazole, a pharmaceutically suitable solvent system, one or more taste-enhancing/masking agents and lactic acid, wherein said solution has a pH from 2.5 to 4.5.

11. A pharmaceutical solution according to claim 10 wherein said pharmaceutically suitable solvent system is comprised of one or more agents selected from the group consisting of water, ethanol, glycerin, propylene glycol and sorbitol and wherein said solution has a pH from 2.5 to 4.0.

12. A pharmaceutical solution according to claim 11 wherein one or more of said taste-enhancing/masking agents are selected from the group consisting of flavoring agents, sucrose, fructose, dextrose, maltose, glucose, maltitol, xylitol, sorbitol and mannitol.

13. A pharmaceutical solution suitable for oral administration comprising aripiprazole, glycerin, lactic acid, propylene glycol, methylparaben, propylparaben, sucrose, fructose and water.