Pharmaceutical formulation of apomorphine for buccal administration

• US 20090023766A1
• Filed: 05/08/2006
• Published: 01/22/2009
• Est. Priority Date: 05/06/2005
• Status: Abandoned Application

• Current Assignee: Amarin Pharmaceuticals Ireland Limited (Amarin Corporation plc)
• Original Assignee: Amarin Pharmaceuticals Ireland Limited (Amarin Corporation plc)
• Inventors: Clarke, Anthony
• Application Number:
  US11/919,799
• Publication Number:
  US 20090023766A1
• Time in Patent Office: Days
• US Class Current: 514/284
• CPC Class Codes: A61K 31/435 having six-membered rings with one nitrogen as the only ring hetero atom
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs

Abstract

The present invention provides a kit comprising, in separate compartments of a container, the following components (a) and (b): (a) a combination of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier; and (b) a solution which comprises a diluent and a pH modifying agent; the components being presented such that they can be combined at the point of use into a formulation which is adjusted to a pH ranging from mildly acidic to alkaline and which is suitable for buccal administration. The formulation is useful in treating Parkinson'"'"'s disease and in promoting sexual function.

Claims

1. A kit comprising a container, which comprises separate first and second compartments, wherein the first compartment comprises the following components (a):

(a) a combination of;

(i) apomorphine or a pharmaceutically acceptable acid addition salt thereof, and

(ii) a pharmaceutically acceptable excipient or carrier; and

wherein the second compartment comprises the following component (b);

(b) a solution which comprises a diluent and a pH modifying agent;

wherein the first and second compartments are arranged such that components (a) and (b) can be combined at the point of use of the kit to produce a formulation having a pH ranging from mildly acidic to alkaline, and which is suitable for buccal administration.

2. A kit according to claim 1 wherein the diluent is water.

3. A kit according to claim 1 wherein the pH modifying agent is a buffer and the formulation is buffered to a pH ranging from mildly acidic to alkaline.

4. A kit according to claim 1 wherein component (a) is present in particulate form.

5. A kit according to claim 1 wherein component (a) is present in suspension or liquid form.

6. A kit according to claim 1 wherein component (b) further comprises one or more additional pharmaceutically acceptable agents selected from the group consisting of solubilizers, adhesive agents, antioxidants, flavouring agents, sweeteners, and combinations thereof.

7. A process for producing a pharmaceutical composition, which process comprises combining apomorphine or a pharmaceutically acceptable acid addition salt thereof with a solution which comprises a diluent and a pH modifying agent, such that the resulting formulation is has a pH ranging from mildly acidic to alkaline, and is suitable for buccal administration.

8. A process according to claim 7 wherein the diluent is water.

9. A process according to claim 7 wherein the pH modifying agent is a buffer, such that the formulation is buffered to a pH ranging from mildly acidic to alkaline.

10. (canceled)

11. (canceled)

12. (canceled)

13. (canceled)

14. (canceled)

15. A method of administering an apomorphine composition to a patient in need thereof, comprising:

(a) optionally adjusting the pH of a composition comprising a pharmaceutically effective amount of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier to a pH ranging from mildly acidic to alkaline; and

(b) delivering the composition buccally to a patient in need thereof.

16. The method of claim 15, wherein the diluent comprises water.

17. The method of claim 15, wherein the adjusting of the pH of the composition comprises adding to the composition a pH modifying agent.

18. The method of claim 17, wherein the pH modifying agent comprises a buffer capable of buffering the composition to a pH ranging from mildly acidic to alkaline.

19. The method of claim 15, wherein composition is administered to treat Parkinson'"'"'s disease.

20. The method of claim 15, wherein the composition is administered to promote sexual function, treat sexual dysfunction, enhance libido, reduce impotence, or a combination thereof.