Stable pharmaceutical budersonide preparation for producing propellant-free aerosols

Abstract

The invention relates to ethanol-containing pharmaceutical preparations for the production of propellant-free aerosols.

1 . A pharmaceutical preparation for use in producing propellant-free aerosols which comprises a pharmacologically active substance, and if necessary, pharmacologically-harmless adjuvants and/or flavourings, characterised in that the pharmaceutical preparation contains at least 70% (v/v) ethanol as a solvent.  
     
     
         2 . A pharmaceutical preparation according to  claim 1 , characterised in that it contains 96% (v/v) ethanol as a solvent.  
     
     
         3 . A pharmaceutical preparation according to  claim 1  or  2 , characterised in that the active substance is suitable for administration by inhalation and is selected from the group comprising betamimetics, anticholinergics, antiallergics and/or PAF-antagonists.  
     
     
         4 . A pharmaceutical preparation according to  claims 1  to  3 , characterised in that the proportion of dissolved pharmaceutical product in the pharmaceutical preparation is between 0.001 and 5.0 percent by volume.  
     
     
         5 . A pharmaceutical preparation for the production of propellant-free aerosols, comprising a steroid and, if necessary, pharmacologically-harmless adjuvants and/or flavourings, characterised in that the pharmaceutical preparation contains at least 85% (v/v) ethanol as a solvent, and if necessary, a complex forming agent.  
     
     
         6 . A pharmaceutical preparation according to  claim 5 , characterised in that the solvent is 96% (v/v) ethanol.  
     
     
         7 . A pharmaceutical preparation according to  claim 6 , characterised in that the complex forming agent is EDTA or a salt thereof.  
     
     
         8 . A pharmaceutical preparation according to  claim 5  or  claim 7 , characterised in that the quantity of complex forming agent is between 0.1 and 5 mg/100 ml of solution.  
     
     
         9 . A pharmaceutical preparation according to one of  claims 5  to  8 , characterised in that the pH value of the preparation is adjusted to a level between 3.2 and 4.5.  
     
     
         10 . A pharmaceutical preparation according to one of  claims 5  to  9 , characterised in that the active substance is Flunisolide or Budesonide.  
     
     
         11 . A pharmaceutical preparation according to one of  claims 1  to  6 , characterised in that the active substance is Tiotropium or an acid addition salt thereof.  
     
     
         12 . A pharmaceutical preparation according to one of  claims 1  to  6 , characterised in that the active substance is 3-[(hydroxydi-2-thienylacetyl)oxy]-8,8-dimethyl-8-azoniabicyclo[3,2,]oct-6-ene or an acid addition salt thereof.  
     
     
         13 . A pharmaceutical preparation for use in producing a propellant-free metering aerosol containing, per 100 ml of 96% (v/v) ethanol, 1.667 g of Flunisolide hemihydrate and 1 mg of disodium EDTA, the pH value of the pharmaceutical preparation being adjusted to 4.0.  
     
     
         14 . A pharmaceutical preparation for use in producing a propellant-free metering aerosol containing, per 100 ml of 90% (v/v) ethanol, 1.667 g of Flunisolide hemihydrate and 1 mg of disodium EDTA, the pH value of the pharmaceutical preparation being adjusted to 4.0.  
     
     
         15 . A pharmaceutical preparation for use in producing a propellant-free metering aerosol containing, per 100 ml of 96% (v/v) ethanol, 1.333 g of Budesonide and 1 mg of disodium EDTA, the pH value of the pharmaceutical preparation being adjusted to 4.0.  
     
     
         16 . A pharmaceutical preparation for use in producing a propellant-free metering aerosol containing, per 100 ml of 90% (v/v) ethanol, 1.333 g of Budesonide and 1 mg of disodium EDTA, the pH value of the pharmaceutical preparation being adjusted to 4.0.  
     
     
         17 . Use of a pharmaceutical preparation comprising a pharmacologically active substance in a solution containing at least 79% ethanol by volume in the preparation of a propellant-free composition for administration by inhalation.  
     
     
         18 . Use of a pharmaceutical preparation as defined in one of  claims 1  to  16  as a propellant-free composition for administration by inhalation.  
     
     
         19 . A process for preparing a pharmaceutical preparation as defined in  claim 1  which comprises dissolution of a pharmacologically active substance in at least 70% v/v.  
     
     
         20 . A delivery system for a pharmacologically active substance which comprises a preparation as defined in any one of  claims 1  to  16  in combination with a propellant-free nebuliser.