Oral pharmaceutical formulation of omarigliptin
View Patent ↗The present invention is directed to stable, oral pharmaceutical formulations of dipeptidyl peptidase-4 inhibitors, such as omarigliptin. Such pharmaceutical formulations comprise omarigliptin; and neutral excipients, wherein the neutral excipient is present in the amount of at least 75% by weight of the pharmaceutical formulation and comprises at least one non-reducible sugar diluent or a mixture of non-reducible sugar diluents.
1. A tablet composition comprising, by weight of the composition:
15-16% omarigliptin; and
77-82% mixture of non-reducible sugar diluents.
2. The tablet of claim 1 , wherein the amount of omarigliptin is 12.5 mg or 25 mg.
3. The tablet of claim 1 , wherein the mixture of non-reducible sugar diluents comprises microcrystalline cellulose and mannitol.
4. The tablet of claim 1 , wherein the tablet further comprises a lubricant.
5. The tablet of claim 4 , wherein the lubricant is magnesium stearate.
6. The tablet of claim 4 , wherein the lubricant is present in the amount of 2.5% by weight of the tablet.
7. The tablet of claim 1 , wherein the tablet further comprises a disintegrant.
8. The tablet of claim 7 , wherein the disintegrant is croscarmellose sodium.
9. The tablet of claim 7 , wherein the tablet further comprises a coating.
10. A method of treating diabetes comprising administering the tablet of claim 1 , to a subject in need thereof.
11. The method of claim 10 , wherein the tablet of claim 1 is administered once weekly.
12. A stable oral pharmaceutical formulation consisting essentially of:
Omarigliptin
15.6%
Mannitol
59.9%
Microcrystalline Cellulose
20%
Croscarmellose sodium
2%
Magnesium stearate
2.5%.