Compositions of glycopyrronium salt for inhalation

Abstract

A process for preparing dry powder formulations of a glycopyrronium salt for inhalation that have good stability. The process involves (a) micronising a glycopyrronium salt together with an anti-adherent agent, and (b) admixing carrier particles to form the dry powder formulation.

1 . A process for preparing a dry powder formulation of a glycopyrronium salt for inhalation that comprises the steps of (a) mixing a glycopyrronium salt and an anti-adherent agent to give a homogeneous blend; (b) micronising the blend; and (c) admixing carrier particles to form a dry powder formulation, wherein the carrier particles are mixed with the blend of micronized glycopyrronium salt and anti-adherent agent in a ratio of 2000:1 to 5:1 by mass. 
     
     
         2 . (canceled) 
     
     
         3 . A process according to  claim 1  wherein the anti-adherent agent is a metal stearate, a crystalline sugar or a mixture thereof. 
     
     
         4 . A process according to  claim 3  wherein the anti-adherent agent is a metal stearate. 
     
     
         5 . A process according to  claim 4  wherein the metal stearate is magnesium stearate or calcium stearate. 
     
     
         6 . A process according to  claim 4  wherein the glycopyrronium salt is micronised with from 1 to 20% by mass of the metal stearate. 
     
     
         7 . A process according to  claim 6  wherein the glycopyrronium salt is micronised with from 2 to 10% by mass of the metal stearate. 
     
     
         8 . (canceled) 
     
     
         9 . A process according to  claim 1  wherein the carrier particles are mixed with the blend of micronised glycopyrronium salt and anti-adherent agent in a ratio of from 200:1 to 20:1 by mass. 
     
     
         10 . A process according to  claim 1  wherein the carrier particles are crystalline sugars. 
     
     
         11 . A process according to  claim 1  wherein the glycopyrronium salt is glycopyrronium bromide, glycopyrronium chloride or glycopyrronium iodide. 
     
     
         12 . A process according to  claim 11  wherein the glycopyrronium salt is glycopyrronium bromide. 
     
     
         13 . A process according to  claim 1  in which the blend of glycopyrronium salt and the anti-adherent agent are micronised together with one, two, three or more additional active ingredients. 
     
     
         14 . (canceled) 
     
     
         15 . A process according to  claim 13  in which the one, two, three or more additional active ingredients is selected from the group consisting of anti-inflammatory, bronchodilatory, antihistamine, decongestant and anti-tussive drug substances. 
     
     
         16 . A process according to  claim 15  in which the one, two, three, or more additional active ingredients is selected from the group consisting of beta-2 adrenoceptor agonists, antimuscarinic agents, steroids, PDE4 inhibitors and calcium channel blockers. 
     
     
         17 . A process according to  claim 16  in which the one, two, three, or more additional active ingredients is selected from the group consisting of salmeterol, indacaterol and mometasone. 
     
     
         18 . A process according to  claim 1  wherein the anti-adherent agent is an amino acid, a phospholipid or a fatty acid derivative. 
     
     
         19 . A process according to  claim 18  wherein the anti-adherent agent a phospholipid. 
     
     
         20 . A process according to  claim 19  wherein the anti-adherent agent is a lecithin.