Method for administering acylated insulin

{
  "publication_number": "US6335316B1",
  "country": "US",
  "kind": "B1",
  "title": "Method for administering acylated insulin",
  "abstract": "The invention relates to a method of administering a fatty acid-acylated insulin or insulin analog by inhalation, a method for treating diabetes by administering a fatty acid-acylated insulin or insulin analog by inhalation, and a method for treating hyperglycemia by administering a fatty acid-acylated insulin or insulin analog by inhalation.",
  "claims": [
    "1. A pharmaceutical formulation comprising a fatty acid-acylated human insulin or a fatty acid-acylated human insulin analog and a liquid carrier, for administration by inhalation to a patient in need thereof.",
    "2. The formulation according to claim 1, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is acylated with a fatty acid having ten to sixteen carbon atoms.",
    "3. The formulation according to claim 2, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is selected from the group consisting of B29-Nε-myristoyl-human insulin, B29-Nε-palmitoyl-human insulin, B28-Nε-myristoyl-LysB28,ProB29-human insulin analog, and B29-Nε-myristoyl-des(ThrB30)-human insulin analog.",
    "4. The formulation according to claim 3, wherein the fatty acid-acylated human insulin analog is B29-Nε-myristoyl-des(ThrB30)-human insulin.",
    "5. The formulation according to claim 1, further comprising a non-acylated insulin or insulin analog.",
    "6. The formulation according to claim 5, wherein the non-acylated insulin is human insulin.",
    "7. The formulation according to claim 5, wherein the non-acylated insulin analog is LysB28,ProB29-human insulin.",
    "8. The formulation according to claim 5, wherein the non-acylated insulin analog is AspB28-human insulin.",
    "9. The formulation according to claim 1, wherein the formulation is an aqueous solution or an aqueous suspension of the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog.",
    "10. The formulation according claim 1, further comprising zinc ions.",
    "11. A method of delivering a fatty acid-acylated human insulin or fatty acid-acylated human insulin analog, comprising the step of using an inhalation device to deposit in the lungs of a patient in need thereof an effective amount of a pharmaceutical formulation comprising a fatty acid-acylated human insulin or a fatty acid-acylated human insulin analog and a liquid carrier.",
    "12. The method according to claim 11, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is acylated with a fatty acid having ten to sixteen carbon atoms.",
    "13. The method according to claim 12, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is selected from the group consisting of B29-Nε-myristoyl-human insulin, B29-Nε-palmitoyl-human insulin, B28-Nε-myristoyl-LysB28,ProB29-human insulin analog, and B29-Nε-myristoyl-des(ThrB30)-human insulin analog.",
    "14. The method according to claim 13, wherein the fatty acid-acylated human insulin analog is B29-Nε-myristoyl-des(ThrB30)-human insulin.",
    "15. The method according to claim 11, wherein the formulation further comprises a non-acylated insulin or insulin analog.",
    "16. The method according to claim 15, wherein the non-acylated insulin is human insulin.",
    "17. The method according to claim 15, wherein the non-acylated insulin analog is LysB28,ProB29-human insulin.",
    "18. The method according to claim 15, wherein said non-acylated insulin analog is AspB28-human insulin.",
    "19. The method according to claim 11, wherein the formulation is an aqueous solution or an aqueous suspension of the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog.",
    "20. The method according to claim 11, wherein the formulation further comprises zinc ions.",
    "21. The method according to claim 11, wherein the inhalation device is a nebulizer or a sprayer.",
    "22. A pharmaceutical formulation comprising a fatty acid-acylated human insulin or a fatty acid-acylated human insulin analog in dry powder form, for administration by inhalation to a patient in need thereof.",
    "23. The formulation according to claim 22, wherein the dry powder comprises particles of the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog having an MMEAD of less than 10 μm.",
    "24. The formulation according to claim 23, wherein the MMEAD is in the range of about 1 μm to about 5 μm.",
    "25. The formulation according to claim 24, wherein the MMEAD is in the range of about 1 μm to about 3 μm.",
    "26. The formulation according to claim 25, wherein the MMEAD is in the range of about 2 μm to about 3 μm.",
    "27. The formulation according to claim 22, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is acylated with a fatty acid having ten to sixteen carbon atoms.",
    "28. The formulation according tc claim 27, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is selected from the group consisting of B29-Nε-myristoyl-human insulin, B29-Nε-palmitoyl-human insulin, B28-Nε-myristoyl-LysB28,ProB29-human insulin analog, and B29-Nε-myristoyl-des(ThrB30)-human insulin analog.",
    "29. The formulation according to claim 28, wherein the fatty acid-acylated human insulin analog is B29-Nε-myristoyl-des(ThrB30)-human insulin.",
    "30. The formulation according to claim 22, further comprising a non-acylated insulin or insulin analog.",
    "31. The formulation according to claim 30, wherein the non-acylated insulin is human insulin.",
    "32. The formulation according to claim 30, wherein the non-acylated insulin analog is LysB28,ProB29-human insulin.",
    "33. The formulation according to claim 30, wherein the non-acylated insulin analog is AspB28-human insulin.",
    "34. The formulation according to claim 22, wherein the formulation further comprises zinc ions.",
    "35. A method of delivering a fatty acid-acylated human insulin or fatty acid-acylated human insulin analog, comprising the step of using an inhalation device to deposit in the lungs of a patient in need thereof an effective amount of a pharmaceutical formulation comprising a fatty acid-acylated human insulin or a fatty acid-acylated human insulin analog in dry powder form.",
    "36. The method according to claim 35, wherein the dry powder comprises particles of the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog having an MMEAD of less than 10 μm.",
    "37. The method according to claim 36, wherein the MMEAD is in the range of about 1 μm to about 5 μm.",
    "38. The method according to claim 37, wherein the MMEAD is in the range of about 1 μm to about 3 μm.",
    "39. The method according to claim 38, wherein the MMEAD is in the range of about 2 μm to about 3 μm.",
    "40. The method according to claim 35, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is acylated with a fatty acid having ten to sixteen carbon atoms.",
    "41. The method according to claim 40, wherein the fatty acid-acylated human insulin or fatty acid-acylated human insulin analog is selected from the group consisting of B29-Nε-myristoyl-human insulin, B29-Nε-palmitoyl-human insulin, B28-Nε-myristoyl-LysB28,ProB29-human insulin analog, and B29-Nε-myristoyl-des(ThrB30)-human insulin analog.",
    "42. The method according to claim 41, wherein the fatty acid-acylated human insulin analog is B29-Nε-myristoyl-des(ThrB30)-human insulin.",
    "43. The method according to claim 35, wherein the formulation further comprises a non-acylated insulin or insulin analog.",
    "44. The method according to claim 43, wherein the non-acylated insulin is human insulin.",
    "45. The method according to claim 43, wherein the non-acylated insulin analog is LysB28,ProB29-human insulin.",
    "46. The method according to claim 43, wherein the non-acylated insulin analog is AspB28-human insulin.",
    "47. The method according to claim 35, wherein the formulation further comprises zinc ions."
  ],
  "cpc": [
    "A61K 38/28",
    "A61K 9/0073",
    "A61M 15/02",
    "A61P 3/10"
  ],
  "assignees": [
    "LILLY CO ELI"
  ],
  "filing_date": "2000-03-10",
  "publication_date": "2002-01-01",
  "grant_date": "2002-01-01",
  "priority_date": "1997-10-31",
  "application_number": "US-52309000-A",
  "family_id": "22055992",
  "citations": [
    "US6051551A"
  ]
}