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US 2020/0368252 A1Published application
Process for preparing a dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic
AssigneeChiesi Farmmaceutici S.P.A.
InventorsClaudio CAFIERO, Leonardo ORTENZI, Francesca SCHIARETTI
Life of this patent
Estimating the term…
Abstract
Dry powder formulations for inhalation containing a combination of an anti-cholinergic, a long-acting beta2-adrenoceptor agonist, and a corticosteroid are useful for the prevention and/or treatment of an inflammatory and/or obstructive airways disease.
Claims20
A process for preparing a powder formulation for inhalation for use in a dry powder inhaler, said powder comprising:
- (A) a carrier, comprising:
- (a) 80 to 95 percent by weight, based on the total weight of said carrier, of coarse particles of a physiologically acceptable excipient having a mean particle size of at least 175 m;
- and
- (b) 19.6 to 4.9 percent by weight, based on the total weight of said carrier, of micronized particles of a physiologically acceptable excipient, and 0.1 to 0.4 percent by weight, based on the total weight of said carrier, of a salt of a fatty acid;
- and
- (B) micronized particles of an anti-muscarinic drug, a long-acting β2-agonist, and optionally, an inhaled corticosteroid, as active ingredients,
- said process comprising:
- (i) mixing all of said coarse particles of a physiologically acceptable excipient;
- all of said salt of a fatty acid;
- a first portion of said micronized particles of a physiologically acceptable excipient;
- and all of said micronized particles of said long-acting β2-agonist, said anti-muscarinic drug, and, optionally, said inhaled corticosteroid in a vessel of a shaker mixer at a speed of rotation not lower than 16 r.p.m. for a time of not less than 60 minutes, to obtain a first mixture;
- and
- (ii) adding the remaining part of said micronized particles of a physiologically acceptable excipient to said first mixture, to obtain a second mixture, and mixing said second mixture at a speed of rotation not lower than 16 rpm for a time of at least 120 minutes, to obtain said formulation.
10 more elements
A powder formulation for inhalation for use in a dry powder inhaler, said powder comprising:
- (A) a carrier, comprising:
- (a) 80 to 95 percent by weight, based on the total weight of said carrier, of coarse particles of a physiologically acceptable excipient having a mean particle size of at least 175 μm;
- and
- (b) 19.6 to 4.9 percent by weight, based on the total weight of said carrier, of micronized particles of a physiologically acceptable excipient, and 0 to 0.4 percent by weight, based on the total weight of said cattier, of magnesium stearate;
- and
- (B) micronized particles of glycopyrronium bromide, beclometasone dipropionate, and formoterol fumarate dihydrate, as active ingredients,
- wherein said formulation is obtainable by a process comprising:
- (i) mixing all of said coarse particles of a physiologically acceptable excipient;
- all of said magnesium stearate;
- a first portion of said micronized particles of a physiologically acceptable excipient;
- and all of said micronized particles of glycopyrronium bromide, beclometasone dipropionate, and formoterol fumarate dihydrate in a vessel of a shaker mixer at a speed of rotation not lower than 16 rpm for a time of not less than 60 minutes, to obtain a first mixture;
- and
- (ii) adding the remaining part of said micronized particles of a physiologically acceptable excipient to said first mixture, to obtain a second mixture, and mixing said second mixture at a speed of rotation not lower than 16 for a time of at least 120 minute, to obtain said formulation,
- whereby the extrafine particle fraction of each active ingredient is from 20 to 35%.
11 more elements
Dependencies are inferred from the claim text.