Intranasal Pharmaceutical Dosage Forms Comprising Naloxone

• US 20150018379A1
• Filed: 05/11/2012
• Published: 01/15/2015
• Est. Priority Date: 05/13/2011
• Status: Abandoned Application

• Current Assignee: Euroceltique SA
• Original Assignee: Euroceltique SA
• Inventors: Oksche, Alexander, Smith, Kevin, Strang, John, Harris, Stephen, Mottier, Lucie Helene Jeanne
• Application Number:
  US14/084,551
• Publication Number:
  US 20150018379A1
• 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 47/02 Inorganic compounds
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/36 Opioid-abuse
• CPC Class Codes: A61P 39/02 Antidotes
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention relates to an intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof in an amount of equivalent to ≧0.5 mg naloxone HCl dissolved in an application fluid of a volume of ≦250 μl. Furthermore, the present invention relates to such an intranasal pharmaceutical dosage form for use in the treatment of opioid overdosing and/or at least one symptom thereof.

Claims

1-21. -21. (canceled)

22. An intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof dissolved in an application fluid of a volume of ≦

about 250 μ

l or ≦

about 200 μ

l, wherein the dosage from includes naloxone in an amount equivalent to from about 0.65 mg naloxone HCl to about 0.8 mg naloxone HCl or an amount equivalent to from about 1.3 mg naloxone HCl to about 1.6 mg naloxone HCl.

23. The dosage form according to claim 22, wherein said dosing unit comprises naloxone or a pharmaceutically acceptable salt thereof in an amount equivalent to from about 0.65 mg naloxone HCl to about 0.8 mg naloxone HCl.

24. The dosage form according to claim 22, wherein said dosing unit comprises naloxone or a pharmaceutically acceptable salt thereof in an amount equivalent to from about 1.3 mg naloxone HCl to about 1.6 mg naloxone HCl.

25. The dosage form according to claim 22, wherein the volume of the application fluid is from about 200 μ

l to about 35 μ

l, from about 200 μ

l to about 50 μ

l, or from about 200 μ

l to about 100 μ

l.

26. The dosage form according to claim 22, wherein the application fluid is water or an aqueous saline solution.

27. The dosage form according to claim 22, wherein the dosage form is a nasal spray, a nasal mucoadhesive dosage form, or a mucosal atomizer device.

28. A method of treating opioid overdosing or at least one symptom thereof, the method comprising administering to a patient in need there of an effective amount of an intranasal pharmaceutical dosage form, the dosage form comprising naloxone or a pharmaceutically acceptable salt thereof dissolved in an application fluid, wherein an amount equivalent to from about 1.3 mg naloxone HCl to about 1.6 mg naloxone HCl is administered intranasally, wherein said amount is provided by administration to one nostril or wherein said amount is provided by administration to two nostrils, and wherein the volume of the application fluid per nostril is ≦

about 250 μ

l or ≦

about 200 μ

l.

29. The method of claim 28, wherein the amount of naloxone or the pharmaceutically acceptable salt thereof administered intranasally is equivalent to about 1.3 mg naloxone HCl, about 1.4 mg naloxone HCl, about 1.5 mg naloxone HCl, or about 1.6 mg naloxone HCl.

30. The method of claim 28, wherein the volume of the application fluid is from about 200 μ

l to about 35 μ

l per nostril, from about 200 μ

l to about 50 μ

l per nostril, or from about 200 μ

l to about 100 μ

l per nostril.

31. The method of claim 28, wherein the volume of the application fluid is from about 150 μ

l to about 100 μ

l per nostril.

32. The method of claim 28, wherein said amount is provided by administration to one nostril.

33. The method of claim 28, wherein the application fluid is water or an aqueous saline solution.

34. The method of claim 28, wherein the dosage form comprises said amount or half of said amount dissolved in an application fluid in a dosing unit, the amount being dependent on whether said amount is provided by administration to one nostril or by administration to two nostrils.

35. The method of claim 28, wherein the dosage form comprises a single dosing unit or two dosing units, dependent on whether said amount is provided by administration to one nostril or by administration to two nostrils.

36. The method of claim 28, wherein the dosage form comprises at least two dosing units and is for multiple uses.

37. The method of claim 28, wherein the dosage form is a nasal spray, a nasal mucoadhesive dosage form, or a mucosal atomizer device.

38. The method of claim 28, wherein the dosage form comprises naloxone as the only pharmaceutically active compound.

39. The method of claim 28, wherein said amount is re-administered during an initial titration period in order to provide for an effective amount of naloxone.

40. The method of claim 28, wherein the dosage form is co-administered with an intramuscular and/or intravenous dosage form comprising naloxone or a pharmaceutically acceptable salt thereof.