Therapeutic compositions for intranasal administration which include ketorolac

• US 20020077346A1
• Filed: 07/13/2001
• Published: 06/20/2002
• Est. Priority Date: 07/22/1991
• Status: Active Grant

• Current Assignee: Egalet US Incorporated (Assertio Holdings, Inc.)
• Original Assignee: Recordati S.A. Chemical and Pharmaceutical Company
• Inventors: Santus, Giancarlo, Bilato, Ettore, Bottoni, Giuseppe
• Granted Patent: US 7,267,827 B2
• Time in Patent Office: Days
• US Class Current: 514/412
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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.

Claims

1. 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, of the formula

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

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

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

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

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 wherein said excipient comprises a polymer that dissolves vehicle viscosity based on temperature change, to increase said viscosity at body temperature.

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

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

13. A method according to claim 8 wherein said effective amount is within the range of 0.5-40 mg.

14. A method according to claim 8 wherein said effective amount is within the range of 5-30 mg.

15. A method according to claim 8 wherein said effective amount is within the range of 5-20% (weight/volume).

16. A method according to claim 8 wherein said effective amount is within the range of 15% (weight/volume).

17. 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.

18. A method according to claim 17 wherein said mammal is a human and wherein said effective amount is sufficient to generate a plasma concentration of 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid within the range between 0.3 and 5 mg/liter of plasma.

12. 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 an 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.