EP1527772A1 — An aerosol pharmaceutical solution formulation suitable for oral or nasal inhalation containing glucocorticoids stable to the storage; method for stabilizing formulations and use of a stabilizer

USPTO Abstract

Aerosol pharmaceutical solution formulations containing glucocorticosteroids stabilized by adding water or a mixture of water and citric acid, avoiding corrosion of the elements of container under standard storage conditions are described. The formulations comprise:between 0.05 and 1.0 % by weight of a glucocorticoid having a C-20 ketone and OH group in carbons 17 and/or 21 as active substance;between 0.10 and 3 % by weight of a selected stabilizer selected between water, or a mixture of water and organic acid selected between citric acid and tartaric acid;a cosolvent in amount sufficient to solubilize the active substance;optionally a surfactant; andpropellant in sufficient amount to achieve100% by weight of the finished solution.Glucocorticosteroids having a C-20 ketone and an OH group at the C-17 and/or 21 position with varying substituents, have many well-known therapeutic uses, especially based upon their anti-inflammatory activity. This types of steroids, glucocorticosteroids, and their pharmaceutical formulations are useful in the treatment of several diseases including bronchial disorders and inflammatory conditions. Preferably, the glucocorticoid is selected between Triamcinolone Acetonide, budesonide, Dexamethasone and betamethasone 17-valerate.A method for stabilizing aerosol pharmaceutical solution formulations containing glucocorticoids susceptible to oxidative degradation and use of a stabilizer selected between water and a mixture of water and organic acid selected between citric acid and tartaric acid are also described