Aripiprazole, olanzapine and haloperidol pamoate salts

• US 20060040922A1
• Filed: 10/18/2005
• Published: 02/23/2006
• Est. Priority Date: 08/06/2003
• Status: Abandoned Application

• Current Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Original Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Inventors: Wright, James, Greco, Kristyn
• Application Number:
  US11/252,862
• Publication Number:
  US 20060040922A1
• Time in Patent Office: Days
• US Class Current: 514/220
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: C07D 211/52 having an aryl radical as the second substituent in position 4

Abstract

The invention relates to the discovery that pamoate salts of haloperidol and aripiprazole result in a good to superior long acting and/or extended release profile. Thus, in one aspect of the invention, the invention includes pamoate salts of haloperidol or aripiprazole. Preferably, the pamoate salt is characterized by a ratio of haloperidol to pamoate of 1:1 or 2:1. The pamoate salt can be crystalline, such as a needle or a dense crystal, such as described in the Figures. The invention further relates to methods of treating an individual in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of haloperidol and aripiprazole.

Claims

1. A pamoate salt of haloperidol.

2. The pamoate salt of claim 1, wherein the ratio of haloperidol to pamoate is 1:

1 or 2;

1.

3. The pamoate salt of claim 1, wherein the salt is a needle.

4. The pamoate salt of claim 1, wherein the salt is crystalline.

6. The pamoate salt of claim 4, wherein the ratio of aripiprazole to pamoate is 1:

1 or 2;

1.

5. A pamoate salt of aripiprazole.

7. The pamoate salt of claim 5, wherein the salt is crystalline.

8. A method of treating an individual in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of an active agent selected from the group consisting of haloperidol and aripiprazole.

9. The method of claim 8, wherein the composition is administered by injection.

10. The method of claim 8, wherein the composition is administered intramuscularly or subcutaneously.

11. The method of claim 8, wherein the composition releases an effective amount of the active agent over a period of at least about 24 hours.

12. The method of claim 8, wherein the composition releases an effective amount of the active agent over a period of at least about 48 hours.

13. The method of claim 8, wherein said composition consists essentially of the pamoate salt and a viscous aqueous carrier.

14. The method of claim 8, wherein said composition is an extended release formulation comprising a biodegradable polymer and the pamoate salt.

15. The method of claim 14, wherein the extended release formulation comprises a polylactide and the pamoate salt.

16. The method of claim 14, wherein the extended release formulation comprises a polylactide-co-glycolide and the pamoate salt.