US 9,808,422 B2
Dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic for administration by inhalation
Irene Pasquali, Parma (IT); Rossella Musa, Parma (IT); Francesca Schiaretti, Parma (IT); and Azita Askey-Sarvar, Parma (IT)
Assigned to Chiesi Farmaceutici S.p.A., Parma (IT)
Filed by CHIESI FARMACEUTICI S.p.A., Parma (IT)
Filed on May 20, 2016, as Appl. No. 15/160,593.
Application 15/160,593 is a continuation of application No. 14/327,920, filed on Jul. 10, 2014, granted, now 9,402,825.
Claims priority of application No. 13176114 (EP), filed on Jul. 11, 2013; and application No. 13194763 (EP), filed on Nov. 28, 2013.
Prior Publication US 2016/0263027 A1, Sep. 15, 2016
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/14 (2006.01); A61K 9/00 (2006.01); A61K 31/167 (2006.01); A61K 31/573 (2006.01); A61K 31/40 (2006.01); A61K 45/06 (2006.01); A61J 3/02 (2006.01); A61M 15/00 (2006.01)
CPC A61K 9/0075 (2013.01) [A61J 3/02 (2013.01); A61K 9/145 (2013.01); A61K 31/167 (2013.01); A61K 31/40 (2013.01); A61K 31/573 (2013.01); A61K 45/06 (2013.01); A61M 15/00 (2013.01); Y10S 514/958 (2013.01)] 15 Claims
 
1. 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.