Steroidal aerosol compositions and process for the preparation thereof
AssigneeAllen & Hanburys Limited
InventorsPeter Barry Cook, John Harold Hunt
Life of this patent
Estimating the term…
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 micronized 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.
Claims16
A method of converting an anti-inflammatory steroid selected from the group consisting of pregn-4-en-3,20-diones having at the 17.alpha.-position a hydroxy or acyloxy group, provided that when the 17.alpha.-position is substituted by a hydroxy group, the 21-position is substituted by an acyloxy group, or having a 16,17-ketonide group;
- having an axo group or a .beta.-chlorine or .beta. -hydroxy group at the 11-position;
- and having a single or double bond in the 1,2-position, the 21-position being unsubstituted or substituted by a hydroxy or acyloxy group or a halogen atom, said steroid having a hydrogen, fluorine or chlorine atom or a methyl group in the 6.alpha.-position;
- a hydrogen or chlorine atom in the 9.alpha.-position when there is a .beta.-chlorine atom in the 11-position;
- a fluorine, chlorine or hydrogen atom in the 9.alpha.-position when there is an oxygen function at the 11-position;
- and a hydrogen atom or a methyl or methylene group at the 16-position;
- said steroid exhibiting crystal growth in aerosol propellants into a form which does not exhibit such growth whereby the said steroid is contacted with a halogenated hydrocarbon to form a crystalline solvate therewith, the crystalline material so formed being, if desired after removal of some or all of the halogenated hydrocarbon therefrom, reduced to a particle size permitting inhalation into the human bronchial system when dispersed as an aerosol.
Dependencies are inferred from the claim text.