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US4364923A Expired / Lapsed US ⏱️ 0.0 years remaining

Chemical compounds

Assignee: Allen and Hanburys Ltd
•
Filing: 1981-04-30
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Granted: 1982-12-21
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Expires: 2001-04-30
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Abstract

Abstract An antiinflammatory steroid exhibiting a tendency to crystal growth in suspension in aerosol propellants is contacted with a halogenated hydrocarbon to form a crystalline solvate, which, after removal of some or all of the propellant from the crystals, is reduced to a particle size permitting inhalation into the human bronchial system when dispersed as an aerosol, the micronised crystalline solvate not thereafter exhibiting crystal growth in the aerosol propellant. The solvate is a new composition of matter which has been characterized by I.R. spectra and the aerosol formulation prepared therefrom has valuable therapeutic properties, particularly in the treatment of asthma.

Inventors

  • 👤 Peter B. Cook
  • 👤 John H. Hunt

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-31 19:35
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/007; A61K9/0073; A61K9/008

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 95 words
An aerosol formulation comprising an aerosol propellant containing suspended therein an anti-inflammatory steroid in the form of a crystalline solvate with a halogenated hydrocarbon or said crystalline solvate from which part or all of the halogenated hydrocarbon has been removed, wherein said halogenated hydrocarbon is a chloro or chlorofluoro hydrocarbon having 1 or 2 carbon atoms; said steroid being stabilized with respect to further growth in said aerosol propellant and the particle size of substantially all of said steroid material being such as to permit inhalation into the bronchial system when dispersed as an aerosol.
Claim 2
Dependent Claim 95 words
An aerosol formulation comprising an aerosol propellant containing suspended therein an anti-inflammatory steroid in the form of a crystalline solvate with a halogenated hydrocarbon or said crystalline solvate from which part or all of the halogenated hydrocarbon has been removed, wherein said halogenated hydrocarbon is a chloro or chlorofluoro hydrocarbon having 1 or 2 carbon atoms; said steroid being stabilized with respect to further growth in said aerosol propellant and the particle size of substantially all of said steroid material being such as to permit inhalation into the bronchial system when dispersed as an aerosol.
Claim 3
Dependent Claim 17 words
An aerosol formulation as claimed in claim 1 in which the anti-inflammatory steroid is beclomethasone 17, 21-dipropionate.
Claim 4
Dependent Claim 19 words
An aerosol formulation as claimed in claim 1 in which the anti-inflammatory steroid is betamethasone 21-acetate-17-isobutyrate or 21-chloro-21-desoxy betamethasone-17-propionate.
Claim 5
Dependent Claim 15 words
An aerosol formulation as claimed in claim 1 in which the halogenated hydrocarbon is trichloromonofluoromethane.
Claim 6
Dependent Claim 17 words
An aerosol formulation as claimed in claim 1 in which the halogenated hydrocarbon is dichlorodifluoromethane or trichlorotrifluoroethane.
Claim 7
Dependent Claim 24 words
An aerosol formulation as claimed in claim 1 in which the particle size of the solvate crystals is reduced to less than 20 microns.
Claim 8
Dependent Claim 21 words
An aerosol formulation as claimed in claim 5 in which the particle size is reduced to from 2 to 5 microns.
Claim 9
Dependent Claim 22 words
An aerosol formulation as claimed in claim 1 in which the steroid is beclomethasone 17, 21-dipropionate and the halogenated hydrocarbon is trichloromonofluoromethane.
Claim 10
Dependent Claim 37 words
An aerosol formulation as claimed in claim 1 contained in an aerosol container equipped with a metering valve to enable a metered dose to be dispensed, the metered dose containing from 10 to 1000 μg of steroid.
Claim 11
Dependent Claim 32 words
An aerosol formulation as claimed in claim 9 where the steroid is beclomethasone 17, 21-dipropionate the halogenated hydrocarbon is trichloromonofluoromethane and the metered dose contains from 30 to 80 μg of steroid.
Claim 12
Dependent Claim 58 words
An aerosol formulation comprising an aerosol propellant containing suspended therein beclomethasone dipropionate in the form of a crystalline solvate which is stabilized with respect to further crystal growth in said aerosol propellant and the particle size of substantially all of said beclomethasone dipropionate being such as to permit inhalation into the bronchial system when dispersed as an aerosol.
Claim 13
Dependent Claim 58 words
An aerosol formulation comprising an aerosol propellant containing suspended therein beclomethasone dipropionate in the form of a crystalline solvate which is stabilized with respect to further crystal growth in said aerosol propellant and the particle size of substantially all of said beclomethasone dipropionate being such as to permit inhalation into the bronchial system when dispersed as an aerosol.
Claim 14
Dependent Claim 16 words
An aerosol formulation as claimed in claim 11, wherein the aerosol propellant is a halogenated hydrocarbon.

References Cited (Backward Citations)

US3312590A Cited
US3721687A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-12-20 1986-06-21 1986-12-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-12-20 1990-06-21 1990-12-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-12-20 1994-06-21 1994-12-21 $7700.00 Window Closed / Lapsed

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