UNIT DOSAGE FORM IN THE FORM OF A DRY POWDER COMPOSITION, USE OF THE UNIT DOSAGE FORM, AND DRY POWDER INHALER FILLED WITH THE UNIT DOSAGE FORM

摘要

Provided is a unit dosage form in the form of a dry powder composition for the prevention and/or treatment of an inflammatory or obstructive disease of upper airways suitable for administering by means of a dry powder inhaler, the unit dosage comprising: a) a fraction of fine alpha lactose monohydrate particles having a mass median diameter less than 20 μm; b) a fraction of coarse alpha lactose monohydrate particles having a mass median diameter of 175 μm or more, where the ratio of fine and coarse particles is 1:99 to 30:70 wt.%; c1) micronized formoterol fumarate dihydrate for delivery in a therapeutic dose of 6 or 12 μg per inhaler actuation, wherein (1) not more than 10% of said particles have a volumetric diameter less than 0.8 μm, (2) not more than 50% of the particles have a volumetric diameter less than 1.7 μm, and (3) at least 90% of the particles have a volumetric diameter less than 5.0 μm, and wherein the particles are characterized by a specific surface area of 5 to 7.5 m²/g; c2) micronized beclomethazone dipropionate (BDP) for delivery in a therapeutic dose of 100 or 200 μg per inhaler actuation, wherein (1) not more than 10% of BDP particles have a volumetric diameter less than 0.6 μm, (2) not more than 50% of the particles have a volumetric diameter of 1.5 to 2.0 μm; and (3) at least 90% of the particles have a volumetric diameter less than 4.7 μm, and wherein the particles are characterized by a specific surface area of 5.5 to 7.0 m²/g; by means of which said composition, as the inhaler is actuated, allows generation of a fraction of particles having a diameter of 1.1 μm or less and accounting for more than 25% of both active ingredients, and is therapeutically equivalent to the respective composition for a pressurized metered dose inhaler (pMDI) including said active ingredients dissolved in mixture of ethanol and propellant HFA134a. Also provided are the use of said unit dosage form and a dry powder inhaler.