Taurine compositions suitable for inhalation

Abstract

The invention discloses spray-dried compositions for inhalation and methods for preparing such powder compositions. The compositions of the invention are produced by spray-drying taurine under conditions that (i) retain the physical and chemical stability of the composition during spray drying and upon storage, (ii) protect the powder composition from aggregation and (iii) provide particles suitable for aerosolisation.

1 . A method for preparing conditioned taurine, the method comprising
 a conditioning step, wherein the conditioning step is   a spray drying step, to produce taurine that:   (a) demonstrates no significant net change in the D 90  (±20%) after 7 days of ambient storage and   (b) have a particle size D 90  of <20 μm, but more preferably <10 μm after 7 days of ambient storage;   
     
     
         2 . Conditioned taurine obtained by the method of  claim 1 . 
     
     
         3 . The conditioned taurine according to  claim 2 , which is suitable for inhalation. 
     
     
         4 . The conditioned taurine according to  claim 2 , which is at least 95% crystalline. 
     
     
         5 . A composition comprising conditioned taurine, in a dry powder form suitable for inhalation, wherein the dry powder form is prepared by spray drying. 
     
     
         6 . A composition according to  claim 5 , further comprising an amino acid. 
     
     
         7 . A composition according to  claim 5  or  6 , wherein the amino acid is selected from the group consisting of alanine, leucine, isoleucine, lysine, valine, methionine or phenylalanine. 
     
     
         8 . A composition according to  claim 5  or  6 , wherein the amino acid is leucine. 
     
     
         9 . A composition according to  claim 8 , wherein the leucine is present in an amount less than 10% by weight based on the dry weight of the composition. 
     
     
         10 . A composition according to  claim 5 , further comprising a medicament. 
     
     
         11 . A composition according to  claim 10  in which the medicament is selected from budesonide, formoterol fumarate dihydrate, tiotropium, fluticasone propionate, salmeterol xinafoate, vilanterol trifenatate, umeclidinium bromide, glycopyrronium bromide or indacaterol maleate. 
     
     
         12 . A composition according to  claim 5 , further comprising combinations of medicaments. 
     
     
         13 . A composition according to  claim 12  in which the combination of medicaments is selected from budesonide and formoterol fumarate dehydrate; fluticasone propionate and salmeterol xinafoate; fluticasone propionate and vilanterol trifenatate; and umeclidinium bromide and vilanterol trifenatate. 
     
     
         14 . (canceled) 
     
     
         15 . A method for preparing conditioned taurine, the method comprising
 drying solubilised taurine, by spray drying with one or more of the following parameters:   (a) the pH of the feedstock to be spray dried is acidic e.g. less than pH 5, preferably equal to or less then pH 4, such as about pH 4;   (b) wherein the feedstock concentration is between 0.1% and 10%, more preferably between 1% and 5%;   (c) the feedstock temperature is between 0.1° C. and 100° C., more preferably between 20° C. and 70° C.;   (d) the outlet temperature is between 50° C. and 120° C., more preferably between 60° C. and 100° C.;   (e) the T (solid:gas)  ratio is between 2.00×10 −6  and 2.75×10 −3 .   
     
     
         16 . A method for preparing conditioned taurine, the method comprising
 drying solubilised taurine, by spray drying with one or more of the following parameters:   (a) the pH of the feedstock to be spray dried is less then pH 4;   (b) wherein the feedstock concentration is between 1% and 5%;   (c) the feedstock temperature is between 20° C. and 70° C.;   (d) the outlet temperature is between 60° C. and 100° C.;   (e) the T (solid:gas)  ratio is between 2.00×10 −6  and 2.75×10 −3 .   
     
     
         17 . A kit comprising a container which holds one selected from the group consisting of:
 (a) conditioned taurine; and   (b) a composition comprising conditioned taurine   which is prepared by spray drying.   
     
     
         18 . A container according to  claim 17  selected from the group consisting of the reservoir for a dry powder inhaler, a blister and a capsule. 
     
     
         19 . A method for preparing conditioned taurine, the method comprising a one-step spray drying process.