Propofol hydrofluorocarbon propellant formulations

• US 5,496,537 A
• Filed: 03/23/1995
• Issued: 03/05/1996
• Est. Priority Date: 03/23/1995
• Status: Expired due to Term

• Current Assignee: Lynchris Pharmaceuticals, Ltd.
• Original Assignee: Richard A. Henry
• Inventors: Henry, Richard A.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Bawa, Raj
• Application Number:
  US08/408,866
• Time in Patent Office: 348 Days
• Field of Search: 424/45, 424/47, 424/46, 514/818, 514/974
• US Class Current: 424/45
• CPC Class Codes: A61K 31/05 Phenols cannabinoids A61K31/658
• 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 23/00 Anaesthetics

Abstract

Non-volatile general anesthetics are advantageously provided to patients in aerosolized form using a metered dose inhaler. The anesthetics are highly lipophilic in character and are rapidly absorbed through the nasal, oral, and lung mucosa. Experiments have shown that propofol is readily soluble in hydrofluorocarbon propellants without the use of surfactants and co-solvents. The solubility allows for the controlled delivery of concentrated pure anesthetic agents like propofol to the airway mucosa of human and animal patients to cause rapid onset of sedation or anesthesia without the requirement of prior intravenous access.

Claims

1. An aerosol formulation for oral or nasal delivery to a patient, consisting essentially of:

1-40% w/w propofol; and

60-99% w/w hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane and combinations thereof.

2. The aerosol formulation of claim 1 wherein said propofol is present in its base form.

5. An aerosol formulation as recited in claim 1 further comprising 0.1-10% by weight of a taste enhancer.

3. An aerosol formulation for oral or nasal delivery to a patient, comprising:

1-40% w/w propofol;

60-98% w/w hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane; and

1-10% w/w of a medicament selected from the group consisting of beta-2 agonists, synthetic noncatecholamines, local anesthetic other than propofol, salicylates, para-aminophenols, propionic acids, and sympathomimetrics.

4. A method of solubilizing medicaments in hydrofluorocarbon propellants, comprising the step of using propofol at 1-40% w/w to dissolve or disperse 1-10% w/w of a medicament in 60-98% w/w of said hydrofluorocarbon propellant which is selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane.