Compositions for oral adminstration of active principles requiring masking of taste

Abstract

Composition intended for the oral administration of active principles with unacceptable taste, which comprises from about 15% to about 30% of organoleptically unpleasant active ingredient (principle) that is mixed with from about 60% to about 80% of an ester of glycerol or of a fatty acid, to which a wax is optionally added and to which a surfactant is added, and in that it is prepared by a spray-cooling process which can produce a particle size of less than 350 μm.

1 . A composition intended for the oral administration of active ingredients with unacceptable taste, which comprises from about 15 to about 30% of an active ingredient mixed with from about 60% to about 80% of an ester of glycerol or of a fatty acid, to which a wax is optionally added, and to which a surfactant is added, and wherein the composition is prepared by a spray-cooling process which can produce a particle size of less than about 350 μm. 
   
   
       2 . The composition as set forth in  claim 1 , wherein the ester of glycerol is chosen from glyceryl stearate or glyceryl palmitostearate. 
   
   
       3 . The composition as set forth in  claim 1 , wherein the ester of glycerol is present between of the total mixture of the composition. 
   
   
       4 . The composition as set forth in  claim 1 , wherein the ester of glycerol is present between about 60% and about 80% by weight of the total mixture of the composition. 
   
   
       5 . The composition as set forth in  claim 2 , wherein the ester of glycerol is present between about 60% and about 80% by weight of the total mixture of the composition. 
   
   
       6 . The composition as set forth in  claim 3 , wherein the ester of glycerol is present between about 60% and about 80% by weight of the total mixture of the composition. 
   
   
       7 . The composition as set forth in  claim 1 , wherein the ester of glycerol is present between about 70% and about 80% by weight of the total mixture of the composition. 
   
   
       8 . The composition as set forth in  claim 2 , wherein the ester of glycerol is present between about 70% and about 80% by weight of the total mixture of the composition. 
   
   
       9 . The composition as set forth in  claim 3 , wherein the ester of glycerol is present between about 70% and about 80% by weight of the total mixture of the composition. 
   
   
       10 . The composition as set forth in  claim 4 , wherein the ester of glycerol is present between about 70% and about 80% by weight of the total mixture of the composition. 
   
   
       11 . The composition as set forth in  claim 1 , wherein the active ingredient is a pharmaceutically active ingredient. 
   
   
       12 . The composition as set forth in  claim 2 , wherein the active ingredient is a pharmaceutically active ingredient. 
   
   
       13 . The composition as set forth in  claim 12 , wherein the pharmaceutically active ingredient is selected from the group consisting of anti-bacterial agents, antifungal agents, metronidazole, anti-parasitic agents, nivaquine, antiviral agents, anti-cancer agents, analgesics, non-steroidal anti-inflammatories, (NSAIDS), anti-tussives, psychotropic agents, steroids, anti-histamines, anti-allergics, anti-asthmatics, anti-spasmodics, cardiovascular agents, roxitromycin, anti-ulcer agents for the gastrointestinal agents and mixtures thereof. 
   
   
       14 . The composition as set forth in  claim 13 , wherein the active ingredient is an antibiotic. 
   
   
       15 . The composition as set forth in  claim 14 , wherein the antibiotic is selected from the group consisting of pristinamycine, spiramycin, ketolides, telithromycin, quinolones, streptogramins, pristamycins, pyostacin and mixtures thereof. 
   
   
       16 . A process for the preparation of a composition intended for the oral administration of active ingredients with unacceptable taste, comprising:
 mixing one or more active ingredients in a molten ester of glycerol;   optionally adding to the above molten mixture one or more excipients; and   spray-cooling the resulting molten mixture by spraying using a device equipped with a two-fluid nozzle at the top of a tower into which a cold gaseous counter-current is optionally introduced.   
   
   
       17 . The process as recited in  claim 16 , wherein the device is further equipped with a fluidized bed. 
   
   
       18 . The process as recited in  claim 16 , wherein the ester of glycerol is chosen from glyceryl stearate or glyceryl palmitostearate. 
   
   
       19 . The process as set forth in  claim 18 , wherein the ester of glycerol is present between about 50% and about 85% by weight of the total mixture of the composition. 
   
   
       20 . The process as set forth in  claim 19 , wherein the active ingredient is a pharmaceutically active ingredient selected from the group consisting of anti-bacterial agents, antifungal agents, metronidazole, anti-parasitic agents, nivaquine, antiviral agents, anti-cancer agents, analgesics, non-steroidal anti-inflammatories, (NSAIDS), anti-tussives, psychotropic agents, steroids, anti-histamines, anti-allergics, anti-asthmatics, anti-spasmodics, cardiovascular agents, roxitromycin, anti-ulcer agents for the gastrointestinal agents and mixtures thereof. 
   
   
       21 . The process as recited in  claim 20  wherein the active ingredient is an antibiotic. 
   
   
       22 . The process as recited in  claim 21  wherein the antibiotic is selected from the group consisting of pristinamycine, spiramycin, ketolides, telithromycin, quinolones, streptogramins, pristamycins, pyostacin and mixtures thereof.