Pharmaceutical formulation comprising ciclesonide

Abstract

The disclosure relates to the field of medicine, in particular to the field of veterinary medicine. The disclosure relates to a pharmaceutical (medicament) formulation of glucocorticoids, especially ciclesonide or a pharmaceutically acceptable derivative thereof.

1 . A method of preparing a pharmaceutical formulation, comprising the following steps:
 dissolving ciclesonide in a solvent comprising ethanol and water to form a solution;   and adding a fixed amount of a pharmaceutically acceptable acid at 0.1 or 1.0 molar to reach a value of —log 10 [H+] in the range of 4.0 to 4.6 for the solution.   
     
     
         2 . The method of  claim 1 , wherein a proportion of ethanol in the solvent is in a range of 85-100% V/V. 
     
     
         3 . The method of  claim 1 , wherein a proportion of ethanol in the solvent is in a range of 90-95% V/V. 
     
     
         4 . The method of  claim 1 , wherein a proportion of ethanol in the solvent is 90% V/V ethanol. 
     
     
         5 . The method of  claim 1 , wherein ciclesonide is first dissolved in ethanol and an amount of water needed to reach a target solvent composition for the solution is then added. 
     
     
         6 . The method of  claim 1 , further comprising:
 mixing until a homogeneous solution is formed.   
     
     
         7 . The method of  claim 1 , further comprising:
 filtering the solution through one or more filters with a pore size of maximum 1.0 for at least one of the filters.   
     
     
         8 . The method of  claim 7 , wherein said pore size maximum for at least one of the filters is 0.2 
     
     
         9 . The method of  claim 1 , further comprising:
 filling the solution into containers appropriate for long term storage and for use with an inhaler.   
     
     
         10 . The method of  claim 1 , wherein the acid comprises hydrochloric acid (HCl). 
     
     
         11 . The method of  claim 1 , wherein ciclesonide is dissolved in the solvent in a sufficient amount such that the formulation includes ciclesonide at a concentration of 0.7 g/100 mL to 5 g/100 mL. 
     
     
         12 . The method of  claim 1 , wherein ciclesonide is dissolved in the solvent in a sufficient amount such that the formulation includes ciclesonide at a concentration of 0.7 g/100 mL to 3.1 g/100 mL. 
     
     
         13 . The method of  claim 1 , wherein ciclesonide is dissolved in the solvent in a sufficient amount such that the formulation includes ciclesonide at a concentration of 3 g/100 mL. 
     
     
         14 . A pharmaceutical formulation comprising ciclesonide as active substance and obtained by the method of  claim 1 .