DPP IV INHIBITOR FORMULATIONS

1 . A pharmaceutical composition comprising as an active ingredient a DPP IV inhibitor compound of formula

in an amount of 0.5 mg, 1 mg, 2.5 mg, 5 mg or 10 mg, or a salt thereof, a first diluent, a second diluent, a binder, a disintegrant and a lubricant, wherein the first diluent is mannitol, the second diluent is pregelatinized starch, the binder is copovidone, the disintegrant is corn starch, and the lubricant is magnesium stearate; and wherein the DPP IV inhibitor compound is present in an amount 0.5-20% based on the total weight of DPP IV inhibitor compound, first diluent, second diluent, binder, disintegrant and lubricant.

2 . The pharmaceutical composition of claim 1 further comprising an additional disintegrant.

3 . The pharmaceutical composition of claim 2 , wherein the additional disintegrant is crospovidone.

4 . The pharmaceutical composition of claim 1 further comprising a glidant.

5 . The pharmaceutical composition of claim 4 , wherein the glidant is colloidal silicon dioxide.

6 . The pharmaceutical composition of claim 1 comprising

40-88%

diluent 1,

 3-40%

diluent 2,

1-5%

binder,

 5-15%

disintegrant, and

0.1-4%  

lubricant

7 . The pharmaceutical composition of claim 1 comprising

0.5-7%  

active ingredient

50-75%

diluent 1,

 5-15%

diluent 2,

2-4%

binder,

 8-12%

disintegrant, and

0.5-2%  

lubricant

8 . The pharmaceutical composition according to claim 1 in the dosage form of a capsule, a tablet, or a film-coated tablet.

9 . The pharmaceutical composition of claim 8 comprising 2-4% film coat.

10 . The pharmaceutical composition of claim 9 , wherein the film coat comprises a film-forming agent, a plasticizer, a glidant and optionally one or more pigments.

11 . The pharmaceutical composition of claim 10 , wherein the film coat comprises hydroxypropylmethylcellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and iron oxide.

12 . A process for the preparation of a pharmaceutical composition according to claim 1 comprising

a. dissolving the binder in a solvent to produce a granulation liquid;

b. blending the DPP-IV inhibitor, a diluent, and the disintegrant to produce a pre-mix;

c. moistening the pre-mix with the granulation liquid and subsequently granulating the moistened pre-mix;

d. optionally sieving the granulated pre-mix through a sieve with a mesh size of at least 1.0 mm;

e. drying the granulate at about 40-75° C. until the desired loss on drying value in the range of 1-5% is obtained;

f. sieving the dried granulate through a sieve with a mesh size of at least 0.6 mm;

g. adding the lubricant to the granulate for final blending.

13 . The process according to claim 12 further comprising

h. compressing the final blend into tablet cores;

i. preparing a coating suspension;

j. coating the tablet cores with the coating suspension to a weight gain of about 2-4% to produce film-coated tablets.

14 . The process according to claim 12 , wherein part of the excipients are added extragranular prior to the final blending of step g.

15 . The process according to claim 12 , wherein the granulate produced in steps a-e is produced in a one pot high shear granulation process and subsequent drying in a one pot granulator.

16 . The pharmaceutical composition according to claim 1 , wherein 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is comprised in an amount of 5 mg.

17 . The pharmaceutical composition according to claim 16 in the form of a capsule, a tablet, or a film-coated tablet.

18 . The pharmaceutical composition of claim 16 , wherein the composition is in the form of a film-coated tablet, and wherein the film coat comprise 2-4% wt % based the weight of the uncoated tablet.

19 . The pharmaceutical composition of claim 18 , wherein the film coat comprises a film-forming agent, a plasticizer, a glidant and optionally one or more pigments.

20 . The pharmaceutical composition of claim 19 , wherein the film coat comprises hydroxypropylmethylcellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and iron oxide.

21 . The pharmaceutical composition according to claim 16 , which is an oral dosage form in the form of a tablet.

22 . The pharmaceutical composition according to claim 16 , which is an oral dosage form in form of a film-coated tablet.