Exendin analog formulations
View Patent ↗Novel formulations containing exendins, exendin agonists and/or exendin analogs are provided.
1. A pharmaceutical formulation which is a liquid dosage form suitable for multi-use administration comprising about 0.005% (w/v) to about 0.4% (w/v) of an exendin, an exendin analog or a combination thereof, a buffer, an iso-osmolality modifier, and about 0.005% to about 1.0% (w/v) of a preservative selected from the group consisting of m-cresol, phenol, benzyl alcohol, methyl-, ethyl-, propyl- and butyl-paraben and any combination thereof, wherein said formulation has a pH of between about 3.0 and about 7.0 and said exendin is not exendin-4.
2. The pharmaceutical formulation of claim 1 , where said exendin is exendin-3.
3. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 41.
4. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 42.
5. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 43.
6. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 44.
7. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 45.
8. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 46.
9. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 47.
10. The pharmaceutical formulation of claim 1 , where said exendin analog comprises SEQ ID NO: 48.
11. The pharmaceutical formulation of claim 1 , where said exendin analog is selected from at least one of the group consisting of SEQ ID NOs: 6-189.
12. The pharmaceutical formulation of claim 1 , wherein said exendin analog is selected from at least one of the group consisting of SEQ ID NOs: 6, 7, 8, 9, 40 and 41.
13. The formulation of claim 1 , said formulation having a pH of between about 4.0 and about 6.0.
14. The formulation of claim 1 , wherein said pH is between about 4.0 and about 5.0.
15. The formulation of claim 1 , wherein said exendin or exendin analog is present at a concentration of between about 0.005% (w/v) and about 0.05% (w/v).
16. The formulation of claim 1 , wherein said buffer is selected from the group consisting of an acetate buffer, a glutamate buffer, a citrate buffer, a phosphate buffer, and any combination thereof.
17. The formulation of claim 1 , wherein said buffer is at a concentration between about 0.02% (w/v) and about 0.5% (w/v).
18. The formulation of claim 1 , wherein said iso-osmolality modifier is a carbohydrate, a polyhydric alcohol, or a combination thereof, and said iso-osmolality modifier is at a concentration between about 1% (w/v) and 10% (w/v).
19. The formulation of claim 18 , wherein said polyhydric alcohol is selected from the group consisting of sorbitol, mannitol, inositol, glycerol, xylitol, polyethylene glycols, and any combination thereof.
20. The formulation of claim 18 , wherein said carbohydrate is selected from the group consisting of galactose, arabinose, lactose, and any combination thereof.
21. The formulation of claim 1 , wherein said iso-osmolality modifier is mannitol, sorbitol, or a combination thereof.
22. The formulation of claim 1 , wherein said preservative is m-cresol, phenol or a combination thereof.
23. The formulation of claim 1 , wherein said formulation is suitable for administration via injection to achieve a dose of from about 0.1 μg/kg to about 0.5 μg/kg of said exendin or exendin analog.
24. The formulation of claim 1 , wherein said formulation is suitable for administration via injection to achieve a dose of from about 0.005 μg/kg to about 0.2 μg/kg of said exendin or exendin analog.
25. The formulation of claim 1 , wherein said formulation is suitable for administration via injection to achieve a dose of from about 1 μg/day to about 1 mg/day of said exendin or exendin analog.
26. A pharmaceutical formulation which is a liquid dosage form suitable for multi-use administration comprising an exendin, an exendin analog or a combination thereof, a buffer, an iso-osmolality modifier, and about 0.005% (w/v) to about 1.0% (w/v) of a preservative selected from the group consisting of m-cresol, phenol, benzyl alcohol, methyl-, ethyl-, propyl- and butyl-paraben and any combination thereof, wherein said formulation has a pH of between about 3.0 and about 6.0 and said exendin is not exendin-4.
27. The formulation of claim 26 , wherein said formulation is suitable for a route of administration selected from the group consisting of:
oral administration to achieve a dose of from about 500 μg/day to about 12,000 μg/day of said exendin or exendin analog in a single or divided dose;
pulmonary administration to achieve a dose from about 100 μg/day to about 12,000 μg/day of said exendin or exendin analog in a single or divided dose;
sublingual administration to achieve a dose from about 10 μg/day to about 8,000 μg/day of said exendin or exendin analog in a single or divided dose;
nasal administration to achieve a dose from about 10 μg/day to about 12,000 μg/day of said exendin or exendin analog in a single or divided dose; and
buccal administration to achieve a dose from about 100 μg/day to about 12,000 μg/day of said exendin or exendin analog in a single or divided dose.
28. The formulation of claim 26 , said formulation having a pH of between about 4.0 and about 6.0.
29. The formulation of claim 26 , wherein said pH is between about 4.0 and about 5.0.
30. The formulation of claim 26 , wherein said buffer is selected from the group consisting of an acetate buffer, a glutamate buffer, a citrate buffer, a phosphate buffer, and any combination thereof.
31. The formulation of claim 26 , wherein said buffer is at a concentration between about 0.02% (w/v) and about 0.5% (w/v).
32. The formulation of claim 26 , wherein said iso-osmolality modifier is a carbohydrate, a polyhydric alcohol, or a combination thereof, and said iso-osmolality modifier is at a concentration between about 1% (w/v) and 10% (w/v).
33. The formulation of claim 26 , wherein said polyhydric alcohol is selected from the group consisting of sorbitol, mannitol, inositol, glycerol, xylitol, polyethylene glycols, and any combination thereof.
34. The formulation of claim 26 , wherein said carbohydrate is selected from the group consisting of galactose, arabinose, lactose, and any combination thereof.
35. The formulation of claim 26 , wherein said iso-osmolality modifier is mannitol, sorbitol, or a combination thereof.
36. The formulation of claim 26 , wherein said preservative is m-cresol, phenol or a combination thereof.