DPP IV INHIBITOR FORMULATIONS
The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.
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 . 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.
13 . The pharmaceutical composition according to claim 12 in the form of a capsule, a tablet, or a film-coated tablet.
14 . The pharmaceutical composition of claim 12 , 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.
15 . The pharmaceutical composition of claim 14 , wherein the film coat comprises a film-forming agent, a plasticizer, a glidant and optionally one or more pigments.
16 . The pharmaceutical composition of claim 15 , wherein the film coat comprises hydroxypropylmethylcellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and iron oxide.
17 . The pharmaceutical composition according to claim 12 , which is an oral dosage form in the form of a tablet.
18 . The pharmaceutical composition according to claim 12 , which is an oral dosage form in form of a film-coated tablet.