Compositions containing incretin analogs and their use

Abstract

The present invention provides a composition containing an incretin analog. [Solution] A composition is provided comprising an incretin analog having activity at glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1), and a glucagon (GCG) receptor (i.e., a Tri receptor agonist), and one or more additional agents such as an isotonic agent and a preservative. Methods for treating diseases such as type 2 diabetes, dyslipidemia, metabolic syndrome, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and obesity with the composition are also provided.

Claims

1. Incretin analogs or pharmaceutically acceptable salts thereof, A small number of substances selected from the group consisting of glycerin, mannitol, and propylene glycol At least one isotonic agent, A selective preservative selected from the group consisting of m-cresol and phenol is included. , pharmaceutical composition.

2. The incretin analog or its pharmaceutically acceptable salt is approximately 1 mg / mL to approximately 30 mg The pharmaceutical composition according to claim 1, having a concentration of g / mL.

3. The isotonic agent is glycerin, at a concentration of approximately 5 mg / mL to approximately 50 mg / mL. or the pharmaceutical composition according to claim 1 or 2.

4. The pharmaceutical composition according to claim 3, wherein the glycerin is present at a concentration of 20 mg / mL.

5. The isotonic agent is mannitol, in a concentration of approximately 10 mg / mL to approximately 100 mg / mL. The pharmaceutical composition according to claim 1 or 2, which is a concentration.

6. The pharmaceutical composition according to claim 5, wherein the mannitol is present at a concentration of 48 mg / mL.

7. The isotonic agent is propylene glycol, and is present in a concentration of approximately 5 mg / mL to approximately 50 mg / mL. A pharmaceutical composition according to claim 1 or 2, having a certain concentration.

8. The pharmaceutically acceptable chemical of claim 7, wherein the propylene glycol is present at a concentration of 15 mg / mL. composition.

9. The optional preservative is m-cresol, and is present in concentrations of approximately 1 mg / mL to approximately 10 mg / mL. A pharmaceutical composition according to any one of claims 1 to 8, having a concentration of the above.

10. The pharmaceutical combination according to claim 9, wherein the m-cresol has a concentration of 3.15 mg / mL. A finished product.

11. The aforementioned optional preservative is phenol, in a concentration of approximately 1 mg / mL to approximately 10 mg / mL. A pharmaceutical composition according to any one of claims 1 to 8, having a concentration of [a certain value].

12. The pharmaceutical composition according to claim 11, wherein the phenol is present at a concentration of 5 mg / mL.

13. The incretin analog comprises SEQ ID NO: 1, according to any one of claims 1 to 12. The pharmaceutical composition.

14. The incretin analogs are 1 mg / mL, 2 mg / mL, 3 mg / mL, 4 mg / mL L, 5mg / mL, 6mg / mL, 8mg / mL, 9mg / mL, 12mg / mL, 18 The concentration is selected from the group consisting of mg / mL, 24 mg / mL, and 30 mg / mL. The pharmaceutical composition according to claim 13.

15. Phosphate (PO ４ ) Buffer and Tris(hydroxymethyl)aminomethane (TRIS) The claim according to any one of claims 1 to 14, further comprising a buffer selected from the group consisting of cirrhous fluids. The pharmaceutical composition.

16. The buffer is the TRIS buffer, and has a concentration of 10 mM, as described in claim 15. The pharmaceutical composition.

17. Claim 1 further comprises ethylenediaminetetraacetic acid (EDTA) at a concentration of 0.3 mg / mL. A pharmaceutical composition as described in any one of items 15.

18. An incretin analog containing SEQ ID NO: 1 or a pharmaceutically acceptable salt thereof, wherein the above (i) The concentration of cretin analogs or pharmaceutically acceptable salts thereof is approximately 1 mg / mL to approximately 30 mg / mL. The concentration of the incretin analog or a pharmaceutically acceptable salt thereof, Mannitol at concentrations of approximately 10 mg / mL to approximately 100 mg / mL, Tris(hydroxymethyl)aminomethane (TRI) at concentrations of approximately 10 mM to approximately 100 mM S) The pharmaceutical composition according to claim 1, comprising a buffer.

19. The pharmaceutical composition according to claim 18, wherein the pharmaceutical composition has a pH of about 6.5 to about 7.

5. composition.

20. The pharmaceutically acceptable combination according to claim 18 or 19, wherein the mannitol is present at a concentration of 48 mg / mL. A finished product.

21. The incretin analog or its pharmaceutically acceptable salt is 1 mg / mL, 2 mg / mL L, 3mg / mL, 4mg / mL, 5mg / mL, 6mg / mL, 8mg / mL, 9mg From 12 mg / mL, 18 mg / mL, 24 mg / mL, and 30 mg / mL A pharmaceutical composition according to any one of claims 18 to 20, wherein the concentration is selected from the group. 。

22. The preservative further comprises a preservative selected from the group consisting of m-cresol and phenol, and the preservative The agent has a concentration of approximately 1 mg / mL to approximately 10 mg / mL, any one of claims 18 to 21. The pharmaceutical compositions described in the section.

23. Any of claims 1 to 22 further comprising a pharmaceutically acceptable carrier, diluent, or excipient. The pharmaceutical composition described in item 1.

24. The drug according to any one of claims 1 to 23, wherein the dose of the composition is about 0.5 mL. chemical composition.

25. The pharmaceutical composition according to claim 24 is suitable for administration using an automated injection device. Pharmaceutical composition.

26. The pharmaceutically acceptable salts are sodium salt, trifluoroacetate salt, hydrochloride salt, and acetic acid. A pharmaceutical composition according to any one of claims 1 to 25, selected from salts.

27. Any one of claims 1 to 26, wherein the pharmaceutically acceptable salt is a tetrasodium salt. The pharmaceutical composition described in [reference].

28. A method of treating diabetes, For individuals requiring treatment for diabetes, an effective dose according to any one of claims 1 to 27 A method comprising the step of administering a pharmaceutical composition.

29. The method according to claim 28, wherein the effective dose is administered using an automated injection device.

30. The method according to claim 28 or 29, wherein the effective dose is administered once a week.

31. A method for treating obesity, For individuals requiring treatment for obesity, the drug according to any one of claims 1 to 27 in an effective dose. A method comprising the step of administering a scientific composition.

32. The method according to claim 31, wherein the effective dose is administered using an automated injection device.

33. The method according to claim 31 or 32, wherein the effective dose is administered once a week.

34. Diabetes, dyslipidemia, fatty liver disease, metabolic syndrome, non-alcoholic fat For use in treating diseases selected from the group consisting of hepatitis and obesity, claim A pharmaceutical composition as described in any one of items 1 to 27.

35. A method for use in treating type II diabetes, according to any one of claims 1 to 27 Pharmaceutical composition.

36. A pharmaceutical combination according to any one of claims 1 to 27 for use in treating obesity A finished product.

37. Diabetes, dyslipidemia, fatty liver disease, metabolic syndrome, non-alcoholic fat In the manufacture of drugs for treating diseases selected from the group consisting of hepatitis and obesity, Use of the pharmaceutical composition according to any one of claims 1 to 27.

38. In the manufacture of a drug for treating type II diabetes, any one of claims 1 to 27 Use of the pharmaceutical composition described.

39. A drug according to any one of claims 1 to 27 in the manufacture of a drug for treating obesity. Use of scientific compositions.

40. A product comprising the pharmaceutical composition described in any one of claims 1 to 27, wherein the product is Reusable vials, reusable pen-type syringes, pre-filled disposable pens, auto-injectors Products selected from injectors and pumps.

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