Suspension aerosol formulations

• US 6,743,413 B1
• Filed: 05/31/1995
• Issued: 06/01/2004
• Est. Priority Date: 12/18/1991
• Status: Expired due to Term

• Current Assignee: 3M Company
• Original Assignee: 3M Company
• Inventors: Schultz, Robert K., Schultz, David W., Moris, Robert A., Jinks, Philip A., Oliver, Martin J.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Sheikh, Humera N.
• Application Number:
  US08/455,280
• Time in Patent Office: 3,289 Days
• Field of Search: 424/43-45
• US Class Current: 424/45
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• 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: A61K 9/124 characterised by the propellant
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system

Abstract

Pharmaceutical suspension aerosol formulations containing a therapeutically effective amount of a drug and HFC 134a, HFC 227, or a mixture thereof.

Claims

1. A pharmaceutical suspension formulation suitable for aerosol administration consisting essentially of:

(i) particulate drug; and

(ii) 1,1,1,2-tetrafluoroethane as propellant,

wherein the formulation is further characterized in that it contains no surfactant.

2. The pharmaceutical suspension aerosol formulation of claim 1, wherein the particulate drug is micronized.

3. An aerosol canister equipped with a metering valve, containing a formulation according to claim 1 in an amount sufficient to provide a plurality of therapeutically effective doses of the drug.

4. A pharmaceutical formulation consisting essentially of (i) one or more particulate drugs, and (ii) 1,1,1,2-tetrafluoroethane as propellant, which formulation is free of surfactant, the particulate drug or drugs being present in a therapeutically effective amount less than 1.6% w/w relative to the total weight of the formulation and wherein 90% or more of the particles have a diameter of less than 10 microns.

5. A metered dose inhaler containing a pharmaceutical suspension formulation suitable for aerosol administration, wherein the formulation consists essentially of:

(i) particulate drug; and

(ii) 1,1,1,2-tetrafluoroethane as propellant,

wherein the formulation is substantially free of surfactant.

6. A pharmaceutical suspension formulation suitable for aerosol administration, consisting essentially of:

a therapeutically effective amount of particulate drug; and

propellant HFC 134a,

wherein the formulation is substantially and readily redispersible, and upon redispersion does not flocculate so quickly as to prevent reproducible dosing of the drug and wherein the formulation is free of a surfactant.

7. The formulation of claim 6, wherein the formulation exhibits substantially no growth in particle size or change in crystal morphology of the drug over a prolonged period.

8. The formulation according to claim 6, wherein the drug concentration is less than about 0.1 percent.

9. The formulation according to claim 6, wherein the drug concentration is greater than about 0.1 percent and less than about 0.5 percent.

10. The formulation according to claim 6, wherein the drug concentration is greater than about 0.5 percent.

11. The formulation according to claim 6, wherein the drug has a potency such that a concentration of less than about 0.1 percent is therapeutically effective.

12. An aerosol canister containing a formulation suitable for aerosol administration, consisting essentially of:

particulate drug in an amount sufficient to provide a plurality of therapeutically effective doses of drug; and

propellant HFC 134a,

wherein the formulation is substantially and readily redispersible, and upon redispersion does not flocculate so quickly as to prevent reproducible dosing of the drug and wherein the formulation is substantially free of surfactant.

13. A metered dose aerosol canister containing a formulation suitable for aerosol administration, consisting essentially of:

a therapeutically effective amount of particulate drug in an amount sufficient to provide a plurality of therapeutically effective doses of drug; and

propellant HFC 134a,

wherein the formulation is substantially and readily redispersible, and upon redispersion does not flocculate so quickly as to prevent reproducible dosing of the drug and wherein the formulation is substantially free of surfactant.

14. A method of treating a mammal having a condition capable of treatment by inhalation, comprising the step of:

administering by inhalation a formulation suitable for aerosol administration, wherein the formulation consists essentially of;

(i) particulate drug; and

(ii) 1,1,1,2-tetrafluoroethane as propellant,

wherein the formulation is substantially free of surfactant.

15. A method according to claim 14, wherein the condition capable of treatment by inhalation is asthma.

16. A method according to claim 14, wherein the condition capable of treatment by inhalation is chronic obstructive pulmonary disease.

17. A method of treating a mammal having a condition capable of treatment by inhalation, comprising the step of:

administering by inhalation a formulation suitable for aerosol administration, consisting essentially of;

a therapeutically effective amount of particulate drug; and

propellant HFC 134a,

wherein the formulation is substantially and readily redispersible, and upon redispersion does not flocculate so quickly as to prevent reproducible dosing of the drug to the mammal and wherein the formulation contains no surfactant or less than a stabilizing amount of a surfactant.

18. A method according to claim 17, wherein the condition capable of treatment by inhalation is asthma.

19. A method according to claim 17, wherein the condition capable of treatment by inhalation is chronic obstructive pulmonary disease.

20. An aerosol canister containing a formulation suitable for aerosol administration, wherein said formulation consists essentially of:

particulate drug in an amount sufficient to provide a plurality of therapeutically effective doses of drug; and

propellant HFC 134a,

wherein the formulation is free of surfactant or contains less than a stabilizing amount of surfactant.

21. A metered dose aerosol canister containing a formulation suitable for aerosol administration, wherein said formulation consists essentially of:

particulate drug in an amount sufficient to provide a plurality of therapeutically effective doses of drug; and

propellant HFC 134a,

wherein the formulation is free of surfactant or contains less than a stabilizing amount of surfactant.

22. A method of treating a mammal having a condition capable of treatment by inhalation, comprising:

administering by inhalation a formulation consisting essentially of particulate drug in an amount sufficient to provide a plurality of therapeutically effective doses of drug; and

propellant HFC 134a,

wherein the formulation is free of surfactant or contains less than a stabilizing amount of surfactant.

23. A method according to claim 22, wherein the condition capable of treatment by inhalation is asthma.

24. A method according to claim 22, wherein the condition capable of treatment by inhalation is chronic obstructive pulmonary disease.