You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 6,902,744


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 6,902,744
Title: Exendin agonist formulations and methods of administration thereof
Abstract:Novel exendin and exendin agonist compound formulations and dosages and methods of administration thereof are provided. These compositions and methods are useful in treating diabetes and conditions that would be benefited by lowering plasma glucose or delaying and/or slowing gastric emptying or inhibiting food intake.
Inventor(s): Kolterman; Orville G. (Poway, CA), Young; Andrew A. (La Jolla, CA)
Assignee: Amylin Pharmaceuticals, Inc. (San Diego, CA)
Application Number:09/889,330
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,902,744
Patent Claims: 1. A pharmaceutical formulation which is a liquid dosage form suitable for multi-use administration comprising about 0.005% to about 0.4% (w/v) of exendin-4, 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, 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.

2. The formulation of claim 1, said formulation having a pH of between about 4.0 and about 6.0.

3. The formulation of claim 1, wherein said exendin-4 is present at a concentration of between about 0.005% and about 0.05% (w/v).

4. 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.

5. The formulation of claim 1, wherein said buffer comprises an acetate buffer.

6. The formulation of claim 1, wherein said buffer comprises a glutamate buffer.

7. The formulation of claim 1, wherein said buffer comprises a citrate buffer.

8. The formulation of claim 1, wherein said buffer is at a concentration between about 0.002% and about 0.5% (w/v).

9. The formulation of claim 1, wherein said pH is between about 4.0 and about 5.0.

10. 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% and 10% (w/v).

11. The formulation of claim 10, wherein said polyhydric alcohol is selected from the group consisting of sorbitol, mannitol, inositol, glycerol, xylitol, polyethylene glycols, and any combination thereof.

12. The formulation of claim 10, wherein said carbohydrate is selected from the group consisting of galactose, arabinose, lactose, and any combination thereof.

13. The formulation of claim 1, wherein said iso-osmolality modifier is mannitol, sorbitol, or a combination thereof.

14. The formulation of claim 1, wherein said iso-osmolality modifier comprises mannitol.

15. The formulation of claim 1, wherein said iso-osmolality modifier comprises sorbitol.

16. The formulation of claim 1, wherein said preservative comprises m-cresol.

17. The formulation of claim 1, wherein said preservative comprises phenol.

18. The formulation of claim 1, wherein said formulation is suitable for administration via injection to achieve a dose of from about 0.1 .mu.g/kg to about 0.5 .mu.g/kg of said exendin-4.

19. The formulation of claim 1, wherein said formulation is suitable for administration via injection to achieve a dose of from about 0.005 .mu.g/kg to about 0.2 .mu.g/kg of said exendin-4.

20. The formulation of claim 1, wherein said formulation is suitable for administration via injection to achieve a dose of from about 1 .mu.g/day to about 1 mg/day of said exendin-4.

21. A pharmaceutical formulation which is a liquid dosage form suitable for multi-use administration comprising 0.025% (w/v) of exendin-4, 0.159% (w/v) of an acetate buffer, 4.3% (w/v) mannitol, and 0.22% (w/v) m-cresol, wherein said formulation has a pH of 4.5.

22. A pharmaceutical formulation which is a liquid dosage form suitable for multi-use administration comprising exendin-4, 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, 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.

23. The formulation of claim 22, wherein said formulation is suitable for oral administration to achieve a dose of from about 500 .mu.g/day to about 12,000 .mu.g/day of said exendin-4 in a single or divided dose.

24. The formulation of claim 22, wherein said formulation is suitable for pulmonary administration to achieve a dose from about 100 .mu.g/day to about 12,000 .mu.g/day of said exendin-4 in a single or divided dose.

25. The formulation of claim 22, wherein said formulation is suitable for nasal administration to achieve a dose from about 10 .mu.g/day to about 12,000 .mu.g/day of said exendin-4 in a single or divided dose.

26. The formulation of claim 22, wherein said formulation is suitable for buccal administration to achieve a dose from about 100 .mu.g/day to about 12,000 .mu.g/day of said exendin-4 in a single or divided dose.

27. The formulation of claim 22, wherein said formulation is suitable for sublingual administration to achieve a dose from about 10 .mu.g/day to about 8,000 .mu.g/day of said exendin-4 in a single or divided dose.

28. The formulation of claim 22, said formulation having a pH of between about 4.0 and about 6.0.

29. The formulation of claim 22, wherein said pH is between about 4.0 and about 5.0.

30. The formulation of claim 22, 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 22, wherein said buffer comprises an acetate buffer.

32. The formulation of claim 22, wherein said buffer comprises a glutamate buffer.

33. The formulation of claim 22, wherein said buffer comprises a citrate buffer.

34. The formulation of claim 22, wherein said buffer is at a concentration between about 0.02% and about 0.5% (w/v).

35. The formulation of claim 22, 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% and 10% (w/v).

36. The formulation of claim 35, wherein said polyhydric alcohol is selected from the group consisting of sorbitol, mannitol, inositol, glycerol, xylitol, polyethylene glycols, and any combination thereof.

37. The formulation of claim 35, wherein said carbohydrate is selected from the group consisting of galactose, arabinose, lactose, and any combination thereof.

38. The formulation of claim 22, wherein said iso-osmolality modifier is mannitol, sorbitol, or a combination thereof.

39. The formulation of claim 22, wherein said iso-osmolality modifier comprises mannitol.

40. The formulation of claim 22, wherein said iso-osmolality modifier comprises sorbitol.

41. The formulation of claim 22, wherein said preservative comprises m-cresol.

42. The formulation of claim 22, wherein said preservative comprises phenol.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.