Micronized aerosol steroids

• US 4,414,209 A
• Filed: 06/13/1977
• Issued: 11/08/1983
• Est. Priority Date: 04/20/1972
• Status: Expired due to Term

• Current Assignee: Allen & Hanburys Limited (GlaxoSmithKline PLC)
• Original Assignee: Allen & Hanburys Limited (GlaxoSmithKline PLC)
• Inventors: Hunt, John H., Cook, Peter B.
• Primary Examiner(s): Jiles, Henry R.
• Assistant Examiner(s): Whittenbaugh, Robert C.
• Application Number:
  US05/805,910
• Time in Patent Office: 2,339 Days
• Field of Search: 260/397.45, 424/243
• US Class Current: 514/180
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]

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.

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.

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.

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.

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.