Claims for Patent: 6,946,120

Summary for Patent: 6,946,120

Title:	Pharmaceutical composition
Abstract:	A pharmaceutical composition for topical administration, including, as the pharmaceutically active component, at least 5% by weight, based on the total weight of the composition of a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; an acid in an amount to completely solubilise the piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; a solvent composition including at least two of water, a lower alcohol and a co-solvent selected from one or more of the group consisting of aromatic and polyhydric alcohols; wherein when the co-solvent includes propylene glycol, it is present in an amount of less than approximately 10% by weight.
Inventor(s):	Wai-Chiu So; Tony (Doncaster East, AU), Deo; Peter Paul (Oakleigh, AU), Tait; Russell John (Deepdene, AU)
Assignee:	Connetics Australia Pty. Ltd. (Victoria, AU)
Application Number:	10/124,197
Patent Claims:	1. A homogeneous aerosol formulation, said homogeneous aerosol formulation consisting essentially of: approximately 5% or greater by weight of minoxidil or a pharmaceutically acceptable salt thereof; an acid in an amount effective to solubilize the minoxidil or a pharmaceutically acceptable salt thereof, wherein the acid is a mineral acid selected from the group consisting of hydrochloric acid, sulphuric acid, nitric acid, and phosphoric acid, or an organic acid selected from the group consisting of citric acid, acetic acid, succinic acid, maleic acid, benzoic acid, lactic acid and mixtures thereof; a solvent of water and a lower alcohol wherein the ratio of water to alcohol is in a range of approximately 9:1 to 1:9 by volume; and a co-solvent of a polyhydric alcohol selected from 1,3-butylene glycol, polyethylene glycol, hexylene glycol, dipropylene glycol, glycerol or propylene glycol at less than approximately 10% by weight; wherein the final product of the homogeneous aerosol formulation is foam or a mousse. 2. A homogeneous aerosol formulation according to claim 1, wherein the acid is added in an amount sufficient to provide an apparent pH to the composition of approximately 7.0 or less. 3. A homogeneous aerosol formulation according to claim 1, wherein the minoxidil or pharmaceutically acceptable salt thereof is present in an amount of from approximately 5 to 25% by weight. 4. A homogeneous aerosol formulation according to claim 3, wherein the minoxidil or pharmaceutically acceptable salt thereof is present in an amount of approximately 7.5 to 12% by weight. 5. A homogeneous aerosol formulation according to claim 2, wherein the acid provides to the composition an apparent pH in the range of approximately 5.0 to 7.0. 6. A homogeneous aerosol formulation according to claim 5, wherein the acid is acetic acid or lactic acid. 7. A homogeneous aerosol formulation according to claim 1 wherein the lower alcohol is ethanol. 8. A homogeneous aerosol formulation according to claim 7, wherein the ratio of water to ethanol is in a range of approximately 1:1 to 1:3 by volume. 9. A homogeneous aerosol formulation according to claim 1 wherein the co-solvent is selected from glycerol, 1,3-butylene glycol or propylene glycol. 10. A homogeneous aerosol formulation according to claim 1, wherein the acid is present at a level that provides at least 0.01 Normal acid. 11. A homogeneous aerosol formulation according to claim 1, wherein the acid is present in an molar amount equal to or greater than the amount of the minoxidil or a pharmaceutically acceptable salt thereof in Normal amounts. 12. A homogeneous aerosol formulation according to claim 1, wherein the minoxidil or pharmaceutically acceptable salt thereof is minoxidil acetate or minoxidil lactate. 13. A homogeneous aerosol formulation according to claim 1, including approximately 5 to 12% by weight, based on the total weight of the composition, of minoxidil or pharmaceutically acceptable salt thereof; approximately 24 to 33% by weight water; approximately 43 to 60% by weight of ethanol; and less than 10% by weight, propylene glycol. 14. A homogeneous aerosol formulation, said homogeneous aerosol formulation consisting essentially of: approximately 5% by weight of minoxidil or a pharmaceutically acceptable salt thereof; an acid in an amount effective to solubilise the minoxidil or pharmaceutically acceptable salt thereof, wherein the acid is a mineral acid selected from the group consisting of hydrochloric acid, sulphuric acid, nitric acid, and phosphoric acid, or an organic acid selected from the group consisting of citric acid, acetic acid, succinic acid, maleic acid, benzoic acid, lactic acid and mixtures thereof; and water, ethanol, and less than approximately 10% by weight of propylene glycol; wherein the ratio of water to alcohol is in a range of approximately 9:1 to 1:9 by volume; wherein the final product of the homogeneous aerosol formulation is a foam or a mousse. 15. A homogeneous aerosol formulation according to claim 14, wherein the propylene glycol is approximately 5% or less by weight. 16. A homogeneous aerosol formulation according to claim 14, further comprising approximately 24 to 33% by weight water and approximately 43 to 60% by weight of ethanol. 17. A homogeneous aerosol formulation according to claim 14, wherein the acid is lactic acid. 18. A homogeneous aerosol formulation, said homogeneous aerosol formulation consisting essentially of: approximately 5% by weight of minoxidil or a pharmaceutically acceptable salt thereof; an acid in an amount effective to solubilise the minoxidil or pharmaceutically acceptable salt thereof, wherein the acid is a mineral acid selected from the group consisting of hydrochloric acid, sulphuric acid, nitric acid, and phosphoric acid, or an organic acid selected from the group consisting of citric acid, acetic acid, succinic acid, maleic acid, benzoic acid, lactic acid and mixtures thereof; water and ethanol, wherein the ratio of water to alcohol is in a range of approximately 9:1 to 1:9 by volume; cetyl alcohol, stearyl alcohol and polysorbate 60; and approximately 5% or less by weight of propylene glycol; wherein the final product of the homogeneous aerosol formulation is a foam or a mousse. 19. A method for the treatment of hair loss and related indications in humans comprising the step of applying topically to the human scalp a therapeutically or prophylactically effective amount of a homogeneous aerosol formulation wherein the final product is a foam or a mousse that breaks with shear according to any one of claims 1-4, 5, 6, 7, or 8-18. 20. A formulation comprising a homogeneous aerosol formulation according to any one of claims 1-4, 5, 6, 7, or 8-18 and a suitable propellant. 21. A homogeneous aerosol formulation, said aerosol formulation consisting essentially of: approximately 5% by weight of minoxidil or a pharmaceutically acceptable salt thereof; an acid in an amount effective to solubilise the minoxidil or pharmaceutically acceptable salt thereof, wherein the acid is a mineral acid selected from the group consisting of hydrochloric acid, sulphuric acid, nitric acid, and phosphoric acid, or an organic acid selected from the group consisting of citric acid, acetic acid, succinic acid, maleic acid, benzoic acid, lactic acid and mixtures thereof; water and ethanol, wherein the ratio of water to alcohol is in a range of approximately 9:1 to 1:9 by volume; cetyl alcohol, stearyl alcohol and polysorbate 60; approximately 5% or less by weight of propylene glycol; and an antioxidant, wherein the final product of the homogeneous aerosol formulation is a foam or a mousse.