Method of intrapulmonary administration of a narcotic drug

• US 5,910,301 A
• Filed: 03/07/1997
• Issued: 06/08/1999
• Est. Priority Date: 05/13/1994
• Status: Expired due to Fees

• Current Assignee: Aradigm Corporation
• Original Assignee: Aradigm Corporation
• Inventors: Rubsamen, Reid, Farr, Stephan J., Rowe, Antony M.
• Primary Examiner(s): Bawa, Raj
• Application Number:
  US08/813,094
• Time in Patent Office: 823 Days
• Field of Search: 424/45, 424/46
• US Class Current: 424/45
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 31/4535 containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

An aerosol formulation of an aerosol propellant and a base form of a narcotic drug selected from the group consisting of fentanyl, sufentanil and remfentanyl is provided. Such a formulation allows for the drug to be dissolved within the propellant and used within a device which does not require the use of a lubricant. Formulations are also disclosed which include lubricants, wherein the lubricant and propellant are both either polar or both non-polar. Thus, the lubricant component does not act as a solvent or cosolvent, but rather acts as a lubricant for the valve used for dispersing the formulation to a patient. Typical non-polar propellants include chlorofluorocarbons, which are typically used in connection with non-polar lubricants such as saturated vegetable oils, e.g. fractionated coconut oils. Typical polar propellants include hydrofluoroalkanes, which are typically used in connection with polar lubricants such as polyethylene glycols.

Claims

1. A method of intrapulmonary administration of a narcotic drug, comprising:

determining a patient'"'"'s inspiratory flow rate and inspiratory volume;

calculating a point in the patient'"'"'s inspiratory cycle for release of an aerosol of narcotic drug wherein the point in that most likely to result in reproducible delivery;

releasing, at the calculated point, a metered dose of aerosolized formulation from a pressurized canister wherein the formulation consists essentially of a free base form of a narcotic drug, a low boiling point propellant liquified under pressure and gaseous under atmospheric pressure, wherein the free base form of the drug is completely dissolved in the propellant; and

inhaling the metered dose of aerosolized formulation into the lungs of the patient thereby obtaining a blood plasma level of narcotic of above 1.5 ng/ml within 30 seconds or less from the inhaling.

2. The method of claim 1, wherein the narcotic drug is a free base form of fentanyl.

3. The method of claim 1, wherein the narcotic drug is a free base form of sufentanyl.

4. The method of claim 1, wherein the narcotic drug is a free base form of remifentanyl.

5. The method of claim 1, wherein the narcotic is present in an amount in the range of from about 0.01% to about 1% by weight based on the total volume of the formulation.