Intranasal Opioid Compositions

• US 20120270895A1
• Filed: 06/12/2012
• Published: 10/25/2012
• Est. Priority Date: 05/10/2000
• Status: Abandoned Application

• Current Assignee: University Of Kentucky Research Foundation (University of Kentucky)
• Original Assignee: University Of Kentucky Research Foundation (University of Kentucky)
• Inventors: Wermeling, Daniel P.
• Application Number:
  US13/494,882
• Publication Number:
  US 20120270895A1
• Time in Patent Office: Days
• US Class Current: 514/282
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.

Claims

1. A pharmaceutical composition for intranasal administration to a mammal;

comprising;

an effective amount of an opioid;

a liquid nasal carrier for the opioid; and

one or more sweeteners, flavoring agents, or masking agents or combinations thereof.

2. A pharmaceutical composition according to claim 1, wherein the opioid is morphine, apomorphine, oxymorphone, dihydromorphine, levorphanol, levallorphan, levophenacylmorphan, norlevorphanol, nalorphine, nalbuphine, buprenorphine, butorphanol, naloxone, naltrexone, nalmexone, oxilorphan, cydorphan, ketobemidone, fentanyl, sufentanil, alfentanyl, or combinations thereof.

3. A pharmaceutical composition according to claim 2, wherein the opioid is naloxone or naltrexone.

4. A pharmaceutical composition according to claim 2, wherein the opioid is butorphanol.

5. A pharmaceutical composition according to claim 1, wherein the volume of the composition is about 0.1 ml.

6. A pharmaceutical composition according to claim 1, wherein the composition is preservative free.

7. A pharmaceutical composition according to claim 1, wherein the composition contains a buffer.

8. A pharmaceutical composition according to claim 1, wherein the composition is a sterile solution or suspension.

9. A pharmaceutical composition according to claim 1, wherein the one or more sweeteners, flavoring agents or masking agents is saccharin, sodium saccharin, xylitol, mannitol, sorbitol, sucrose, sucralose, maltodextrin, aspartame, acesulfame potassium, dextrose, glycosides, maltose, sweet orange oil, glycerin, wintergreen oil, peppermint oil, peppermint water, peppermint spirit, menthol, or combinations thereof.

10. A pharmaceutical composition according to claim 1, wherein the composition has a pH of about 3-6.

11. A pharmaceutical composition having improved bioavailability for intranasal administration to a mammal;

comprising;

an effective amount of butorphanol;

a preservative-free liquid nasal carrier.

12. A pharmaceutical composition according to claim 11, wherein the preservative-free liquid nasal carrier comprises anhydrous citric acid, purified water and has a pH of about 3-6, wherein the pharmaceutical composition is free from the preservative benzethonium.

13. A pharmaceutical composition according to claim 11, wherein the composition is a sterile solution or suspension.

14. A pharmaceutical composition according to claim 11, further comprising at least one sweetener, flavoring agent or masking agent.

15. A pharmaceutical composition according to claim 14, wherein the sweetener, flavoring agent or masking agent is saccharin, sodium saccharin, xylitol, mannitol, sorbitol, sucrose, sucralose, maltodextrin, aspartame, acesulfame potassium, dextrose, glycosides, maltose, sweet orange oil, glycerin, wintergreen oil, peppermint oil, peppermint water, peppermint spirit, menthol, or combinations thereof.

16. A pharmaceutical composition according to claim 11, wherein the composition has a pH of about 5.0.

22. A pharmaceutical composition according to claim 12, wherein the composition achieves a plasma butorphanol concentration of at least 4000 and 5000 pg/ml.

17-21. -21. (canceled)

23. (canceled)

24. A method of treating a mammal suffering from pain comprising intranasally administering to the mammal an effective amount of butorphanol or;

a preservative-free liquid nasal carrier comprising sodium chloride, citric acid, water and at least one sweetener, flavoring agent or masking agent.

25. A method according to claim 24, wherein the at least one sweetener, flavoring agent or masking agent is saccharin, sodium saccharin, xylitol, mannitol, sorbitol, sucrose, aspartame, acesulfame potassium, dextrose, glycosides, maltose, sweet orange oil, glycerin, wintergreen oil, peppermint oil, peppermint water, peppermint spirit, menthol, or combinations thereof.