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 dry powder formulations of a glycopyrronium salt for inhalation that comprises the steps of (a) micronising a glycopyrronium salt together with an anti-adherent agent, and (b) admixing carrier particles to form the dry powder formulation. 
   
   
       2 . A process according to  claim 1  wherein the glycopyrronium salt and the anti-adherent agent are mixed prior to being micronised together. 
   
   
       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 . A process according to  claim 1  wherein the carrier particles are mixed with the micronised glycopyrronium salt and anti-adherent agent in a ratio of 2000:1 to 5:1 by mass. 
   
   
       9 . A process according to  claim 8  wherein the carrier particles are mixed with the 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 glycopyrronium salt and the anti-adherent agent are micronised together with one, two, three or more additional active ingredients. 
   
   
       14 . A process according to  claim 13  in which the resulting product is mixed with one or more additional active ingredients that have already been micronised. 
   
   
       15 . A process according to  claim 14  in which the or each additional active ingredient 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 or each additional active ingredient is selected from the group consisting of beta-2 adrenoceptor agonists, antimuscarinic agents, steroids, PDE4 inhibitors or calcium channel blockers. 
   
   
       17 . A process according to  claim 16  in which the or each additional active ingredient 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 fafty 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.