Dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic for administration by inhalation
AssigneeChiesi Farmaceutici S.p.A.
InventorsIrene Pasquali, Rossella Musa, Francesca Schiaretti, Azita Askey-Sarvar
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Abstract
Dry powder formulations for inhalation comprising a combination of an anticholinergic, a long-acting beta2-adrenoceptor agonist, and a corticosteroid are useful for the prevention and/or treatment of inflammatory and/or obstructive airways diseases.
Claims15
A dry powder formulation for use in a dry powder inhaler (DPI) to deliver by inhalation a combination of micronized particles of glycopyrronium bromide, beclometasone dipropionate, and formoterol fumarate dihydrate as active ingredients in a combined therapeutically effective dose of 100 to 500 μg, comprising:
- (a) a fraction of fine particles, consisting of a mixture of 90 to 99.5 percent by weight micronized particles of alpha-lactose monohydrate and 0.5 to 10 percent by weight of magnesium stearate, wherein at least 90% of all said particles have a volume diameter lower than 12 microns and the volume median diameter of said particles is from 4 to 6 microns;
- (b) a fraction of coarse particles consisting of alpha-lactose monohydrate having a mass median diameter of 200 to 400 microns, wherein the ratio between said fine particles (a) and said coarse particles is from 5:95 to 15:85 percent by weight;
- and
- (c) micronized particles of glycopyrronium bromide, beclomatasone dipropionate, and formoterol fumarate dihydrate as active ingredients,
- wherein at least 90% of all said micronized particles of said active ingredients have a volume diameter lower than 6.0 microns, and the volume median diameter of said particles is from 1.2 to 2.5 microns, and
- wherein the width of the particle distribution of all of the above active ingredients, expressed as a span, is comprised between 1.2 and 3.0.
A dry powder formulation for use in a dry powder inhaler (DPI) to deliver by inhalation a combination of micronized particles of glycopyrronium bromide, beclometasone dipropionate, and formoterol fumarate dihydrate as active ingredients in a combined therapeutically effective dose of 100 to 500 μg, comprising:
- (a) a fraction of fine particles, consisting of a mixture of 90 to 99.5 percent by weight micronized particles of alpha-lactose monohydrate and 0.5 to 10 percent by weight of magnesium stearate, wherein at least 90% of all said particles have a volume diameter lower than 15 microns and the volume median diameter of said particles is from 3 to 7 microns, and no more than 10% of said particles have a volume diameter lower than 1.8 microns;
- (b) a fraction of coarse particles consisting of alpha-lactose monohydrate having a mass median diameter of 200 to 400 microns, wherein the ratio between said fine particles (a) and said coarse particles is from 5:95 to 15:85 percent by weight;
- and
- (c) micronized particles of glycopyrronium bromide, beclomatasone dipropionate, and formoterol fumarate dihydrate as active ingredients,
- wherein at least 90% of all said micronized particles of said active ingredients have a volume diameter lower than 6.0 microns, and the volume median diameter of said particles is from 1.2 to 2.5 microns, and
- wherein the width of the particle distribution of all of the above active ingredients, expressed as a span, is comprised between 1.2 and 3.0.
Dependencies are inferred from the claim text.