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 solid-form pharmaceutical composition comprising as an active ingredient 5 mg of a DPP IV inhibitor compound of formula
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 0.5-7.0% 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
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 of claim 1 , 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.
13. The pharmaceutical composition of claim 1 , wherein the film coat comprises a film-forming agent, a plasticizer, a glidant and optionally one or more pigments.
14. The pharmaceutical composition of claim 1 , wherein the film coat comprises hydroxypropylmethylcellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and iron oxide.
15. The pharmaceutical composition according to claim 1 , which is an oral dosage form in the form of a tablet.
16. The pharmaceutical composition according to claim 1 , which is an oral dosage form in form of a film-coated tablet.