Formulation inhibiting effects of low acid environment

1. A formulation comprising:

(a) a dispersion comprising:

(i) a water soluble matrix polymer;

(ii) a compound of Formula I:

 and

(iii) citric acid,

wherein, at least about 70 mole % of said compound of Formula I is in the form of a citrate salt within the dispersion; and

(b) a mixture of at least one acidifying agent and at least one solubilizing agent.

2. A formulation of claim 1 , wherein said water soluble matrix polymer is polyvinylpyrolidone/vinyl acetate (PVP-VA) copolymer.

3. A formulation of claim 1 , wherein at least about 95 mole % of the compound of Formula I present in the dispersion is in the form of amorphous citrate salt.

4. A formulation of claim 2 , wherein about 100 mole % of the compound of Formula I present in the dispersion is in the form of amorphous citrate salt.

5. A formulation of claim 1 , wherein said dispersion comprises:

(a) about 50 wt. % of a 3:2 wt./wt. ratio of a compound of Formula I , including the amount which is converted to a citrate salt, and citric acid, including the amount present in the citrate salt of the compound of Formula I; and

(b) the balance a water-soluble polyvinylpyrolidone/vinyl acetate copolymer.

6. A formulation of claim 1 , wherein said water soluble matrix polymer is a water soluble cellulosic polymer.

7. A formulation of claim 1 , wherein, the acidifying agent in the mixture of at least one acidifying agent and at least one solubilizing agent is citric acid.

8. A formulation of claim 1 , wherein, the solubilizing agent in the mixture of at least one acidifying agent and at least one solubilizing agent is sodium lauryl sulfate.

9. A formulation of claim 1 , wherein, said formulation comprises:

(a) about 40 wt. % of a dispersion comprising:

(i) from about 2.5 wt % of a compound of Formula I to about 12 wt. % of a compound of Formula I wherein at least about 95 mole % of the compound of Formula I is in the form of a citrate salt within the dispersion;

(ii) citric acid; and

(iii) a water soluble matrix polymer;

(b) about 8 wt. % of a mixture of sodium lauryl sulfate and crospovidone which are present in the mixture in a wt. ratio of 2:5 sodium lauryl sulfate:crospovidone;

(c) about 12 wt. % of ex-dispersion anhydrous citric acid;

(d) about 1 wt. % of colloidal silicon dioxide;

(e) about 2 wt. % of stearic acid; and

(f) the balance of the weight of said formulation mannitol.

10. A formulation of claim 1 , wherein the dispersion used in the formulation is prepared by heating a suspension of the compound of Formula I in a suspending solution comprising a mixed water/acetone solvent and citric acid to dissolve the compound of Formula I therein, and spray-drying the resulting heated solution.

11. A formulation of claim 1 , wherein said dispersion is prepared by wet granulating a mixture comprising the compound of Formula I and citric acid with water in the presence of a water soluble matrix polymer.

12. The formulation of claim 11 wherein said compound of Formula I comprises about 30 wt. % of said dispersion, and said dispersion comprises about 40 wt. % of said formulation.

13. A method of providing A2a- antagonist therapy to patients in need thereof who are also receiving proton-pump inhibiting therapy, said method comprising orally administering a therapeutic amount of the formulation of claim 1 to said patient.

14. A method of treating Parkinson's disease by administering a formulation according to claim 9 to a patient in need thereof.

15. A formulation comprising:

(a) a dispersion comprising:

(i) a water soluble matrix polymer;

(ii) a compound of Formula I:

 and

(iii) citric acid,

wherein, at least about 70 mole % of said compound of Formula I is in the form of a citrate salt within the dispersion;

(b) at least one acidifying agent; and

(c) at least one solubilizing agent.

16. A formulation of claim 15 , wherein said dispersion comprises:

(a) about 50 wt. % of a 3:2 wt./wt. ratio of a compound of Formula I, including the amount which is converted to a citrate salt, and citric acid, including the amount present in the citrate salt of the compound of Formula I; and

(b) the balance a water soluble polyvinylpyrolidone/vinyl acetate copolymer.