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PROCÉDÉ DE PRÉPARATION D'UNE FORMULATION DE POUDRE SÈCHE COMPRENANT UN ANTICHOLINERGIQUE, UN CORTICOSTÉROÏDE ET UN BÊTA-ADRÉNERGIQUE
专利权人:
CHIESI FARMACEUTICI S.P.A.
发明人:
CAVECCHI, Alessandro,MERUSI, Cristiana,PIVETTI, Fausto,SCHIARETTI, Francesca
申请号:
EPEP2018/061953
公开号:
WO2018/206618A1
申请日:
2018.05.09
申请国别(地区):
EP
年份:
2018
代理人:
摘要:
The invention relates to 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 micron; 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 (c) 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 glycopyrronium bromide, a long-acting O2 -agonist (LABA) and an inhaled corticosteroid (ICS), as active ingredients, said process comprising : (i) preparing by co-milling microparticles consisting of glycopyrronium bromide and a first part of an ICS in a ratio ranging from 80:20 to 70:30 by weight, wherein the volume diameter of said microparticles is not more than 15 micron; (ii) mixing the coarse particles of a physiologically acceptable excipient, the salt of a fatty acid, a first part of said micronized particles of a physiologically acceptable excipient, the micronized particles of said LABA, the co-milled microparticles obtained in step (i), and the remaining part of said ICS 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 (iii) adding the remaining part of the 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 a formulation.L'invention concerne un procédé de préparation d'une formulation de poudre à inhaler destinée à être utilisée dans un inhalateur de poudre sèche, ladite poudre comprenant : (A) un vecteur comprenant : (a) de 80 à 95 pour cen
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