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Claims for Patent: 6,333,044

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Claims for Patent: 6,333,044

Title: Therapeutic compositions for intranasal administration which include KETOROLAC.RTM.
Abstract:An analgesic/anti-inflammatory pharmaceutical dosage form which comprises an effective amount of an active ingredient selected from the group consisting of racemic 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, optically active forms thereof and pharmaceutically acceptable salts thereof, in combination with a pharmaceutically acceptable excipient or diluent, said dosage form being an intranasally administrable dosage form.
Inventor(s): Santus; Giancarlo (Milan, IT), Bottoni; Giuseppe (Bergamo, IT), Bilato; Ettore (Padua, IT)
Assignee: Recordati, S.A. Chemical and Pharmaceutical Company (Chiasso, CH)
Application Number:08/383,707
Patent Claims: 1. An analgesic/anti-inflammatory pharmaceutical liquid dosage form which comprises a systemically effective amount of an active ingredient selected from the group consisting of racemic 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, of the formula ##STR2##

optically active forms thereof and pharmaceutically acceptable salts thereof, in combination with a pharmaceutically acceptable excipient or diluent, said dosage form being a non-thermosetting intranasally administrable transmucosally rapidly absorbable dosage form that achieves blood levels in a host effective for analgesic or anti-inflammatory use after intranasal administration.

2. The dosage form of claim 1 comprising 0.5-40 mg of said active ingredient.

3. The dosage form of claim 1 comprising 2-20 mg of said active ingredient.

4. The dosage form of claim 1 in a single-dose form.

5. The dosage form of claim 1 comprising 5-20% of said active ingredient (weight/volume).

6. The dosage form of claim 1 in the form of a solution or suspension.

7. The dosage form of claim 1 containing 15% of said active ingredient.

8. The dosage form of claim 1 wherein said excipient comprises a bioadhesive.

9. The dosage form of claim 1 further comprising as an excipient an intranasal absorption promoter.

10. The dosage form of claim 8 wherein said promoter is selected from the group consisting of POE (9) lauryl alcohol and sodium glycocholate and lysophosphatidyl choline.

11. A method for the treatment of inflammatory processes and pain of a traumatic or pathologic origin which comprises the administration by the intranasal route of a dosage form according to claim 1.

12. A method according to claim 11 wherein said mammal is a human and wherein said effective amount is sufficient to generate a plasma concentration of 5-benzdyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid within the range between 0.3 and 5 mg/liter of plasma.

13. The dosage form of claim 1 comprising a mucosal absorption promoter that is not a mucosal irritant.

14. A method for the treatment of inflammatory processes and pain of a traumatic or pathologic origin, which comprises the administration by the intranasal route of a dosage form comprising a systemically effective amount of the active ingredient 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, in a racemic or optically active form or in the form of a pharmaceutically acceptable salt, said dosage form being a non-thermosetting intranasally administrable transmucosally rapidly absorbable dosage form that achieves blood levels for said active ingredient effective for analgesic or anti-inflammatory use after intranasal administration.

15. A method according to claim 14 wherein said effective amount is within the range of 0.5-40 mg.

16. A method according to claim 14 wherein said effective amount is within the range of 5-30 mg.

17. A method according to claim 14 wherein said effective amount is within the range of 5-20% (weight/volume).

18. A method according to claim 14 wherein said effective amount is within the range of 15% (weight/volume).

19. A method according to claim 18 wherein said dosage form comprises said active ingredient is dissolved in an aqueous liquid carrier.

20. A method according to claim 18 wherein said dosage form also comprises a mucosal adsorption promoter that is not a mucosal irritant.

21. An analgesic/anti-inflammatory pharmaceutical liquid dosage form which comprises a systemically effective amount for a human of an active ingredient selected from the group consisting of racemic 5-benzoyl-2,3-dihyro-1H-pyrrolizine-1-carboxylic acid, of the formula ##STR3##

optically active forms thereof and pharmaceutically acceptable salts thereof, in combination with a pharmaceutically acceptable excipient or diluent, said dosage form being an intranasally administrable transmucosally rapidly absorbable dosage form that achieves blood levels in a host effective for analgesic or anti-inflammatory use after intranasal administration, wherein the dosage form is free of polymers providing a low viscosity composition at room temperature but an increased viscosity composition at body temperature.

22. The dosage form of claim 21 in the form of a solution.

23. The dosage form of claim 21 in combination with a container suitable for delivering a spray of the liquid dosage form.

24. The dosage form of claim 21 comprising about 5-20% of said active ingredient (weight/volume).

25. The dosage form of claim 24 containing about 15% of said active ingredient (weight/volume).

26. The liquid dosage form of claim 21, wherein the active ingredient is a pharmaceutically acceptable salt.

27. The liquid dosage form of claim 26, wherein the active ingredient is ketorolac tromethamine and the diluent is water.

28. The dosage form of claim 27 in the form of a solution.

29. The dosage form of claim 28 comprising about 5-20% of ketorolac tromethamine (weight/volume).

30. The dosage form of claim 29 containing about 15% of ketorolac tromethamine (weight/volume).

31. The dosage form of claim 27 consisting essentially of an aqueous solution of ketorolac tromethamine optionally containing at least one additive chosen from a humectant, isotoning agent, antioxidant, buffer, preservative, and chelating agent.

32. The dosage form of claim 31 consisting essentially of an aqueous solution of ketorolac tromethamine that optionally contains a chelating agent and optionally a preservative.

33. The dosage form of claim 27, wherein said amount of ketorolac tromethamine is sufficient to generate, upon administration of said dosage from to a human subject, a plasma concentration of 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid within said subject between about 0.3 and 5 mg/liter of plasma.

34. The dosage form of claim 27 that includes an atomizer that administers the liquid nasally in the form of a spray.

35. The liquid dosage form of claim 21, wherein the active ingredient is the optically active form.

36. A method for the treatment of inflammatory processes and pain of a traumatic or pathologic origin in human, which method comprises the administration by the intranasal route of a dosage form comprising a systemically effective amount of an active ingredient selected from the group consisting of racemic 5-benzoyl-2,3-dihyro-1H-pyrrolizine-1-carboxylic acid, of the formula ##STR4##

optically active forms thereof and pharmaceutically acceptable salts thereof, said dosage form being an intranasally-administrable dosage form that achieves blood levels in a host effective for analgesic or anti-inflammatory use after intranasal administration, wherein the dosage form is free of polymers providing a low viscosity at room temperature but an increased viscosity composition at body temperature.

37. The method of claim 36, wherein the dosage form is a solution.

38. The method of claim 36, wherein the dosage form is administered in the form of a spray.

39. The method of claim 36, wherein said effective amount is within the range of about 5-20% (weight/volume).

40. The method of claim 39, wherein said effective amount is about 15% (weight/volume).

41. The method of claim 36, wherein the active ingredient is a pharmaceutically acceptable salt.

42. The method of claim 41, wherein the active ingredient is ketorolac tromethamine and the diluent is water.

43. The method of claim 42, wherein the dosage form is a solution.

44. The method of claim 43, wherein said effective amount is within the range of about 5-20% (weight/volume).

45. The method of claim 44, wherein said effective amount is about 15% (weight/volume).

46. The method of claim 42, wherein the dosage form consists essentially of an aqueous solution of ketorolac tromethamine optionally containing at least one additive chosen from a humectant, isotoning agent, antioxidant, buffer, preservative, and chelating agent.

47. The method of claim 46, wherein the dosage form consists essentially of an aqueous solution of ketorolac tromethamine that optionally comprises a chelating agent and optionally a preservative.

48. The method of claim 42, wherein the active ingredient is ketorolac tromethamine and the effective amount is sufficient to generate aplasma concentration of 5-benzoyl-2,3-dehydro-1H-pyrolizine-1-carboxylic acid between about 0.3 and 5 mg/liter of plasma.

49. The method of claim 42, wherein the liquid is administered nasally in the form of a spray.

50. The method of claim 36, wherein the active ingredient is the optically-active form.

51. An analgesic/anti-inflammatory aqueous solution as an intranasally administrable pharmaceutical dosage form in a bottle suitable for delivering a spray of the solution, which dosage form comprises about 5% to about 20% (weight/volume) ketorolac tromethamine, optionally less than about 0.1% (weight/volume) sodium ethylenediaminetetretraacetic acid, and optionally a preservative, wherein the dosage form is free of any polymer providing a low viscosity composition at room temperature but an increased viscosity composition at body temperature.
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