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1. WO2007146126 - INSULIN COMPOSITION

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[ EN ]

We claim:

Claim 1. An insulin composition in a form suitable for nasal delivery to a patient, comprising: a therapeutically effective amount of insulin, a permeation enhancer, a liquid carrier, and an acid present in said composition in an amount sufficient to provide an acidic pH, but not greater than a pH of 4.5, said acid being selected from the group consisting of: monovalent inorganic acid(s), sulfuric acid, and acetic acid.

Claim 2. The composition of claim 1, wherein said acid is a monovalent inorganic acid.

Claim 3. The composition of claim 2, wherein said composition is essentially-free of citrate(s).

Claim 4. The composition of claim 2, wherein said composition is essentially-free of phosphate(s).

Claim 5. The composition of claim 2, wherein said composition is essentially-free of citrate(s), and wherein said composition is essentially-free of phosphate(s).

Claim 6. The composition of claim 1, wherein said acidic pH is from about 2 to about 4.

Claim 7. The composition of claim 1, wherein said acidic pH is about 3.5.

Claim 8. The composition of claim 1, further comprising a crystallization inhibitor.

Claim 9. The composition of claim 1, wherein said composition is in the form of an emulsion.

Claim 10. The composition of claim 1, wherein said composition is in the form of a spray emulsion.

Claim 1 1. The composition of claim 1, wherein said permeation enhancer is a macrocyclic permeation enhancer.

Claim 12. -The composition of claim 1 1, wherein said macrocyclic permeation enhancer is selected from the group consisting of macrocyclic ketones and macrocyclic esters.

Claim 13. The composition of claim 12, wherein said macrocyclic ketone is selected from the group consisting of 3 methylcyclopentadecanone (muscone), 9-cycloheptadecen-l-one (civetone), cyclohexadecanone, and cyclopentadecanone (normuscone).

Claim 14. The composition of claim 12, wherein said macrocyclic ester is a pentadecalactone.

Claim 15. The composition of claim 14, wherein said pentadecalactone is oxacyclohexadecan-2-one (cyclopentadecanolide, ω-pentadecalactone).

Claim 16. A product including the pharmaceutical composition of claim 1, wherein said pharmaceutical composition is contained in, and deliverable from, an applicator selected from the group consisting of: nasal spray applicators, intra-nasal spray-dosing devices, and atomizers.

Claim 17. The composition of claim 1, wherein said permeation enhancer is emulsified by a surfactant(s).

Claim 18. The composition of claim 17, wherein said surfactant(s) is / are selected from the group consisting of: non-ionic surfactants and combinations thereof.

Claim 19. The composition of claim 18, wherein said combination of non-ionic surfactants comprises: (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol.

Claim 20. The composition of claim 19, wherein said combination of non-ionic surfactants, comprising (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol, has a combined hydrophilic-Iipophilic balance (HLB) of from about 7 to about 14.

Claim 21. The composition of claim 1, wherein the osmolality of the composition is < 200 mOsmol/Kg H2O.

Claim 22. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 1.

Claim 23. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 2.

Claim 24. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 3.

Claim 25. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 4.

Claim 26. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 5.

Claim 27. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 6.

Claim 28. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 7.

Claim 29. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 8.

Claim 30. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 9.

Claim 31. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 10.

Claim 32. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 1 1.

Claim 33. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 12.

Claim 34. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 13.

Claim 35. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 14.

Claim 36. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 15.

Claim 37. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 16.

Claim 38. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 17.

Claim 39. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 18.

Claim 40. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 19.

Claim 41. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 20.

Claim 42. A method for treating a patient in need of insulin comprising treating said patient by nasally administering to said patient the composition of claim 21.

Claim 43. A pharmaceutical composition for nasal administration to humans, or to warmblooded animals, comprising: (A) a therapeutically effective amount of insulin, (B) a permeation enhancer, (C) a liquid carrier, and (D) a combination of non-ionic surfactants; wherein the combination of non-ionic surfactants comprises: (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol; and said composition is other than a composition of Example 1.

Claim 44. The pharmaceutical composition of Claim 43, wherein said combination of non-ionic surfactants, comprising (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol, has a combined hydrophilic-lipophilic balance (HLB) of from about 7 to about 14.

Claim 45. A pharmaceutical composition for nasal administration to humans, or to warmblooded animals, comprising: (A) a therapeutically effective amount of insulin, (B) a permeation enhancer, (C) a liquid carrier, and (D) a combination of non-ionic surfactants; wherein the combination of non-ionic surfactants comprises: (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol; and wherein the composition is at an acidic pH, but no greater than a pH of 4.5; and said composition is other than a composition of Example 1.

Claim 46. The pharmaceutical composition of Claim 45, wherein said combination of non-ionic surfactants, comprising (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol, has a combined hydrophilic-Hpophilic balance (HLB) of from about 7 to about 14.

Claim 47. A pharmaceutical composition for nasal administration to humans, or to warmblooded animals, comprising: (A) a therapeutically effective amount of insulin, (B) a permeation enhancer, and (C) a liquid carrier; wherein the osmolality of the composition is < 200 mOsmol/Kg H2O; and said composition is other than a composition of Example 1.

Claim 48. The pharmaceutical composition of Claim 47, wherein the osmolality of the composition is < 150 mOsmol/Kg H2O.

Claim 49. The pharmaceutical composition of Claim 47, wherein the osmolality of the composition is < 30 mOsmol/Kg H2O.

Claim 50. A pharmaceutical composition for nasal administration to humans, or to warmblooded animals, comprising: (A) a therapeutically effective amount of insulin, (B) a permeation enhancer, and (C) a liquid carrier; wherein the osmolality of the composition is < 200 mOsmol/Kg H2O; and wherein the composition is at an acidic pH, but no greater than a pH of 4.5; and said composition is other than a composition of Example 1.

Claim 51. The pharmaceutical composition of Claim 50, wherein the osmolality of the composition is < 150 mOsmol/Kg H2O.

Claim 52. The pharmaceutical composition of Claim 50, wherein the osmolality of the composition is < 30 mOsmol/Kg H2O.

Claim 53. A pharmaceutical composition for nasal administration to humans, or to warmblooded animals, comprising: (A) a therapeutically effective amount of insulin, (B) a permeation enhancer, (C) a liquid carrier, and (D) a combination of non-ionic surfactants; wherein the combination of non-ionic surfactants comprises: (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol; and wherein the osmolality of the composition is < 200 mOsmol/TCg H2O; and said composition is other than a composition of Example 1.

Claim 54. The pharmaceutical composition of Claim 53, wherein said combination of non-ionic surfactants, comprising (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol, has a combined hydrophilic-lipophilic balance (HLB) of from about 7 to about 14.

Claim 55. The pharmaceutical composition of Claim 53, wherein the osmolality of the composition is < 150 mOsmol/Kg H2O.

Claim 56. The pharmaceutical composition of Claim 53, wherein the osmolality of the composition is < 30 mOsmol/Kg H2O.

Claim 57. A pharmaceutical composition for nasal administration to humans, or to warmblooded animals, comprising: (A) a therapeutically effective amount of insulin, (B) a permeation enhancer, (C) a liquid carrier, and (D) a combination of non-ionic surfactants; wherein the combination of non-ionic surfactants comprises: (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol; wherein the osmolality of the composition is < 200 mOsmol/Kg H2O; and wherein the composition is at an acidic pH, but no greater than a pH of 4.5; and said composition is other than a composition of Example 1.

Claim 58. The pharmaceutical composition of Claim 57, wherein said combination of non-ionic surfactants, comprising (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol, has a combined hydrophilic-lipophilic balance (HLB) of from about 7 to about 14.

Claim 59. The pharmaceutical composition of Claim 57, wherein the osmolality of the composition is < 150 mOsmol/Kg H2O.

Claim 60. The pharmaceutical composition of Claim 57, wherein the osmolality of the composition is < 30 mOsmol/Kg H2O.

Claim 61. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 43.

Claim 62. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 44.

Claim 63. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 45.

Claim 64. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 46.

Claim 65. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 47.

Claim 66. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 48.

Claim 67. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 49.

Claim 68. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 50.

Claim 69. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 51.

Claim 70. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 52.

Claim 71. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 53.

Claim 72. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 54.

Claim 73. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 55.

Claim 74. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 56.

Claim 75. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 57.

Claim 76. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 58.

Claim 77. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 59.

Claim 78. A method for treating a patient with insulin comprising nasally administering to a patient in need of insulin treatment the composition of claim 60.