Composition and method for the treatment of eye disease

• US 7,960,350 B2
• Filed: 10/21/2004
• Issued: 06/14/2011
• Est. Priority Date: 10/24/2003
• Status: Active Grant

• Current Assignee: Ader Enterprises, Inc.
• Original Assignee: Ader Enterprises, Inc.
• Inventors: Robledo, Emilio
• Primary Examiner(s): Lundgren; Jeffrey S.
• Assistant Examiner(s): BASQUILL, SEAN M
• Application Number:
  US10/971,922
• Publication Number:
  US 20050113311A1
• Time in Patent Office: 2,427 Days
• Field of Search: 514/21.91, 514/400
• US Class Current: 514/21.91
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/12 for cataracts

Abstract

Embodiments of the invention disclosed herein relate to methods of preventing and/or ameliorating one or more symptoms associated with an eye disease such as dry eye syndrome, cataracts of the eye and nuclear sclerosis of the eye lens by administering to a subject a therapeutically effective amount of Nα-acetyl-L-histidine. Additionally, provided herein are pharmaceutical compositions comprising Nα-acetyl-L-histidine. Kits for preventing and/or ameliorating one or more symptoms associated with an eye disease by administering a pharmaceutical composition comprising Nα-acetyl-L-histidine are also disclosed.

Claims

1. A method of treating an eye disease, said method comprising ophthalmically administering to a subject in need of treatment of said eye disease a therapeutically effective amount of Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine), wherein said eye disease is selected from the group consisting of cataracts, nuclear sclerosis and dry eyes.

2. The method of claim 1, wherein said Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) are administered simultaneously to said subject.

3. The method of claim 2, wherein both Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) are administered by providing to said subject a composition which comprises Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) each in a concentration from about 0.1% (w/v) to about 30% (w/v).

4. The method of claim 2, wherein both Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) are administered by providing to said subject a composition which comprises Nα

-acetyl-L-histidine in a concentration of about 1.2% (w/v) and β

-alanyl-L-histidine (L-carnosine) in a concentration of about 1% (w/v).

5. The method of claim 2, wherein both Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) are administered by providing to said subject a composition which comprises Nα

-acetyl-L-histidine in a concentration of about 7.2% (w/v) and β

-alanyl-L-histidine (L-carnosine) in a concentration of about 6% (w/v).

6. The method of claim 1, wherein said eye disease is eye cataracts.

7. The method of claim 1, wherein said eye disease is nuclear sclerosis of the eye lens.

8. The method of claim 1, wherein said eye disease is dry eye syndrome.

9. The method of claim 1, wherein said subject is selected from the group consisting of amphibians, reptiles, avians and mammals.

10. The method of claim 9, wherein said mammal is selected from the group consisting of rodents, cats, dogs, pigs, horses and humans.

11. The method of claim 9, wherein said mammal is a human.

12. The method of claim 1, wherein said Nα

-acetyl-L-histidine and said L-carnosine are administered at least one time per day.

13. The method of claim 1, wherein said Nα

-acetyl-L-histidine and said L-carnosine are administered more than one time per day.

14. The method of claim 1, wherein said therapeutically effective amount of Nα

-acetyl-L-histidine ranges from at least about 0.1 mg to at least about 3000 mg.

15. The method of claim 1, wherein said therapeutically effective amount of Nα

-acetyl-L-histidine ranges from at least about 1 mg to at least about 2000 mg.

16. The method of claim 1, wherein said therapeutically effective amount of Nα

-acetyl-L-histidine is at least about 1200 mg.

17. The method of claim 1, wherein said therapeutically effective amount of Nα

-acetyl-L-histidine is at least about 80 mg.

18. The method of claim 1, wherein said Nα

-acetyl-L-histidine and said L-carnosine are formulated together in a solution.

19. The method of claim 18, wherein said solution is ophthalmic solution.

20. The method of claim 1, wherein said Nα

-acetyl-L-histidine and said L-carnosine are formulated together in an ointment.

21. The method of claim 1, wherein said Nα

-acetyl-L-histidine and said L-carnosine are formulated together in a gel.

22. A method of treating an eye disease, said method comprising ophthalmically administering to a subject in need of treatment of said eye disease a therapeutically effective amount of a composition comprising Nα

-acetyl-L-histidine, β

-alanyl-L-histidine (L-carnosine) and a lubricating agent, wherein said eye disease is selected from the group consisting of cataracts, nuclear sclerosis and dry eyes.

23. The method of claim 22, wherein said composition comprises Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) each in a concentration from about 0.1% (w/v) to about 30% (w/v).

24. The method of claim 22, wherein said composition comprises Nα

-acetyl-L-histidine in a concentration of about 1.2% (w/v) and β

-alanyl-L-histidine (L-carnosine) in a concentration of about 1% (w/v).

25. The method of claim 22, wherein said composition comprises carboxymethylcellulose in a concentration of about 0.5% (w/v), Nα

-acetyl-L-histidine in a concentration of about 1.2% (w/v) and 13-alanyl-L-histidine (L-carnosine) in a concentration of about 1% (w/v).

26. The method of claim 22, wherein said composition comprises carboxymethylcellulose in a concentration of about 1% (w/v), Nα

-acetyl-L-histidine in a concentration of about 7.2% (w/v) and β

-alanyl-L-histidine (L-carnosine) in a concentration of about 6% (w/v).

27. The method of claim 22, wherein said eye disease is eye cataracts.

28. The method of claim 22, wherein said eye disease is nuclear sclerosis of the eye lens.

29. The method of claim 22, wherein said eye disease is dry eye syndrome.

30. The method of claim 22, wherein said subject is selected from the group consisting of amphibians, reptiles, avians and mammals.

31. The method of claim 30, wherein said mammal is selected from the group consisting of rodents, cats, dogs, pigs, horses and humans.

32. The method of claim 30, wherein said mammal is a human.

33. The method of claim 22, wherein said composition is administered at least one time per day.

34. The method of claim 22, wherein said composition is administered more than one time per day.

35. The method of claim 22, wherein said composition is formulated as a solution.

36. The method of claim 35, wherein said solution is an ophthalmic solution.

37. The method of claim 22, wherein said composition is formulated as an ointment.

38. The method of claim 22, wherein said composition is formulated as a gel.

48. The method of claim 22, wherein said composition further comprises a preservative.

49. The method of claim 48, wherein said preservative is benzalkonium chloride.

50. The method of claim 22, wherein said lubricating agent comprises carboxymethylcellulose.

39. A kit for treating an eye disease, said kit comprising a container comprising Nα

-acetyl-L-histidine and β

-alanyl-L-histidine (L-carnosine) in a pharmaceutically acceptable carrier and instructions for administering said Nα

-acetyl-L-histidine and said L-carnosine to a subject in need of treatment of said eye disease, wherein said eye disease is selected from the group consisting of cataracts, nuclear sclerosis and dry eyes.

40. The kit of claim 39, wherein said Nα

-acetyl-L-histidine is present in a concentration from about 0.1% (w/v) to about 30% (w/v).

41. The kit of claim 39, wherein said Nα

-acetyl-L-histidine is present in a concentration of about 1.2% (w/v).

42. The kit of claim 39, wherein said eye disease is eye cataracts.

43. The kit of claim 39, wherein said eye disease is nuclear sclerosis of the eye lens.

44. The kit of claim 39, further comprising a lubricating agent.

45. The kit of claim 44, wherein said eye disease is dry eye syndrome.

46. The kit of claim 39, wherein said container is a dropper.

47. The kit of claim 39, wherein said container is a tube for dispensing ointment or gel.

51. The kit of claim 39, wherein said container further comprises a preservative.

52. The method of claim 51, wherein said preservative is benzalkonium chloride.

53. The kit of claim 44, wherein said lubricating agent comprises carboxymethylcellulose.