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Generated: June 22, 2017

DrugPatentWatch Database Preview

Claims for Patent: 4,414,209

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Claims for Patent: 4,414,209

Title: Micronized aerosol steroids
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.
Inventor(s): Cook; Peter B. (Standon, GB2), Hunt; John H. (Theydon Bois, GB2)
Assignee: Allen & Hanburys Limited (London, GB2)
Application Number:05/805,910
Patent Claims: 1. An antiinflammatory 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 is beclomethasone dipropionate, betamethasone-21-acetate-17-isobutyrate or 21-chloro-21-desoxybetamethasone-17-propionate, said steroid being stabilized with respect to further crystal growth in a chloro or chlorofluoro hydrocarbon solvent having 1 or 2 carbon atoms and the particle size of substantially all of the steroid material being such as to permit inhalation into the human bronchial system.

2. A steroid material as claimed in claim 1 in which the particle size is not greater than 20 microns.

3. A steroid material as claimed in claim 1 in which the particle size is from 2 to 5 microns.

4. A steroid material as claimed in claim 1 in which the steroid is beclomethasone dipropionate.

5. A steroid material as claimed in claim 4 in which the halogenated hydrocarbon is trichloromonofluoromethane.

6. A steroid material as claimed in claim 5 in which the halogenated hydrocarbon is difluorodichloromethane.

7. A steroid material as claimed in claim 32 in which the steroid is betamethasone 21-acetate-17-isobutyrate or 21-chloro-21-desoxy-betamethasone-17-propionate.

8. A steroid material as claimed in claim 4 in the form of a solvate with trichloromonofluoromethane having the I.R. spectrum as shown in FIG. 1 of the accompanying drawings.

9. A steroid material as claimed in claim 7 in the form of a solvate of betamethasone 21-acetate-17-isobutyrate with trichloromonofluoromethane having the I.R. spectrum as shown in FIG. 2 of the accompanying drawings.

10. A steroid material as claimed in claim 7 in the form of a solvate of 21-chloro-21-desoxy-betamethasone-17-propionate with chloroform having the I.R. spectrum as shown in FIG. 4 of the accompanying drawings.
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Serving 500+ biopharmaceutical companies globally:

Novartis
Harvard Business School
Merck
Johnson and Johnson
AstraZeneca
US Department of Justice
Queensland Health
QuintilesIMS
Farmers Insurance
Daiichi Sankyo

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