Pharmaceutical formulations for dry powder inhalers comprising an active ingredient in low dose concentration

摘要

A powder formulation for use in a dry powder inhaler, the powder comprises: i) from 0.5 to 5.0 percent by weight of microparticles consisting of an active ingredient that belongs to the long-acting beta2 agonist class of concentration of low dosage having a therapeutic therapeutic dose equal to or less than 4 μg (microg) on each actuation of the alpha-lactose monohydrate powder inhaler and microparticles in a ratio between 1: 5 and 1: 100 by weight, ii) from 99.5 to 95 percent by weight of a carrier comprising coarse particles of alpha-lactose monohydrate having a mass diameter of between 150 and 400 microns, a crack rate of not less than 1.5 and a roughness coefficient of at least minus 1.25 where both microparticles of i) have: - the average mass diameter (MMD) between 2 and 15 μm (microns); - d (0.1) greater than 0.5 μm; and - d (0.9) less than 60 μm .; and wherein said formulation has an apparent density before sedimentation of at least 0.5 g / ml.