Suspension aerosol formulations of pharmaceutical products

Abstract

Pharmaceutical preparations for producing powder aerosols using propellant gases which use TG 227, and possibly also TG 11, TG 12, TGH 114, propane, butane, pentane or DME.

1 . Propellent gases characterised in that they contain TG 227, optionally in admixture with one of more propellent gases from the group comprising TG 11, TG 12, TG 114, propane, butane, pentane and DME.  
     
     
         2 . Propellent gases according to  claim 1 , characterised in that they additionally contain at least one surface-active substance.  
     
     
         3 . Propellent gases according to  claim 2 , characterised in that the surface-active substance is a phospholipid, a sorbitan ester with a higher saturated or unsaturated fatty acid or a polyethoxysorbitan ester of a higher, preferably unsaturated fatty acid.  
     
     
         4 . Propellent gases according to  claim 2 , characterised in that the surface-active substance is a lecithin, a polyethoxyethylenesorbitan oleate or sorbitan trioleate.  
     
     
         5 . Pharmaceutical preparations for producing powder aerosols based on propellent gases according to  claim 1 ,  2 ,  3  or  4 , characterised in that they contain as active substance a betamimetic, an anticholinergic, a steroid, an antiallergic or a PAF-antagonist or a combination of such compounds.  
     
     
         6 . Pharmaceutical preparations according to  claim 5 , characterised in that the betamimetic used is: 
 Bambuterol    Bitolterol    Carbuterol    Clenbuterol    Fenoterol    Hexoprenalin    Ibuterol    Pirbuterol    Procaterol    Reproterol    Salbutamol    Salmeterol    Sulfonterol    Terbutalin    Tulobuterol    1-(2-fluoro-4-hydroxyphenyl)-2-[4-(1-benzimidazolyl)-2-methyl-2-butylamino]ethanol    erythro-5′-hydroxy-8′-(1-hydroxy-2-isopropylaminobutyl)-2H-1,4-benzoxazin-3-(4H)-one    1-(4-amino-3-chloro-5-trifluoromethylphenyl)-2-tert.-butylamino)ethanol    1-(4-ethoxycarbonylamino-3-cyano-5-fluorophenyl)-2-(tert.-butylamino)ethanol    the anticholinergic used is:    Ipratropium bromide    Oxitropium bromide    Trospium chloride    Benzilic acid-N-β-fluoroethylnortropine ester methobromide    the steroid used is:    Budesonide    Beclomethasone (or the 17, 21-dipropionate thereof)    Dexamethason-21-isonicotinate    Flunisolide    The antiallergic agent is:    Disodium cromoglycate    Nedocromil    The PAF-antagonist is:    WEB 2086    WEB 2170    WEB 2347.    
     
     
         7 . Pharmaceutical preparations according to  claim 5 , characterised in that the combination of the active substances comprises one of the betamimetics specified in  claim 6  and one of the anticholinergics specified in  claim 6 .  
     
     
         8 . Pharmaceutical preparation according to  claim 5 , characterised in that the combination of the active substances comprises one of the betamimetics specified in  claim 6  and disodium chromoglycate.  
     
     
         9 . Pharmaceutical preparation according to  claim 5 , characterised in that the combination of the active substances contains one of the betamimetics specified in  claim 6  and one of the PAF-antagonists specified in  claim 6 .  
     
     
         10 . Pharmaceutical preparation according to  claim 5 , characterised in that the combination of the active substances comprises disodium chromoglycate and one of the PAF-antagonists specified in  claim 6 .  
     
     
         11 . Process for preparing pharmaceutical preparations according to  claims 5  to  10 , characterised in that pharmaceutically active substances micronised by conventional methods are suspended in a liquefied propellent gas mixture according to  claim 1 ,  2 ,  3  or  4 , optionally with the addition of surface-active substances.