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Last Updated: April 25, 2024

Details for Patent: 6,750,210


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Title: Formulation containing novel anti-inflammatory androstane derivative
Abstract:There is provided a pharmaceutical aerosol formulation comprising (i) a compound of formula (I) ##STR1## or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant; and characterized in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.
Inventor(s): Biggadike; Keith (Stevanage, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Filing Date:Feb 04, 2002
Application Number:10/066,964
Claims:1. A pharmaceutical aerosol formulation comprising (i) a compound of formula (I) ##STR9##

or a solvate thereof as medicament, (ii) a liquefied hydrofluoroalkane (HFA) gas as propellant; and characterised in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.

2. A formulation according to claim 1 which contains a hydroxy containing co-solvent liquid as solubilising agent.

3. A formulation according to claim 2 wherein the solubilsing agent is ethanol.

4. A formulation according to claim 1 further comprising a low volatility component.

5. A formulation according to claim 4 wherein the low volatility component is glycerol.

6. A formulation according to claim 1 wherein the propellant gas is 1,1,1,2-tetrafluoroethane.

7. A pharmaceutical aerosol formulation according to claim 1 comprising (i) a compound of formula (I) ##STR10##

or a solvate thereof as medicament, (ii) 1,1,1,2-tetrafluoroethane as propellant, (iii) a solubilising agent to assist the solubilisation of the medicament in the propellant and (iv) optionally a low volatility component; characterised in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.

8. A formulation according to claim 7 which contains ethanol as solubilising agent and glycerol as low volatility component.

9. A formulation according to claim 1 wherein the solubilising agent is an oligolactic acid or derivative thereof.

10. A formulation according to claim 9 wherein the solubilising agent is a compound of formula (IIA)

or a derivative thereof, wherein n is an integer from 3 to 15.

11. A canister comprising a container containing a formulation according to claim 1 and fitted with a metering valve.

12. A canister comprising a container containing a formulation according to claim 7 and fitted with a metering valve.

13. A canister comprising a container containing a formulation according to claim 9 and fitted with a metering valve.

14. A metered dose inhaler comprising a canister according to claim 11 fitted with an actuator adapted for topical administration of the formulation to the lung.

15. A metered dose inhaler comprising a canister according to claim 11 fitted with an actuator adapted for topical administration of the formulation to the nose.

16. A metered dose inhaler comprising a canister according to claim 12 fitted with an actuator adapted for topical administration of the formulation to the lung.

17. A metered dose inhaler comprising a canister according to claim 12 fitted with an actuator adapted for topical administration of the formulation to the nose.

18. A metered dose inhaler comprising a canister according to claim 13 fitted with an actuator adapted for topical administration of the formulation to the lung.

19. A metered dose inhaler comprising a canister according to claim 13 fitted with an actuator adapted for topical administration of the formulation to the nose.

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