Granulate for the formulation of orodispersible tablets

Abstract

This invention relates to a granulate comprising mannitol and sorbitol in a weight ratio of between 70:30 and 97:3. This invention also relates to the use of the said granulate in the preparation of orodispersible tablets, to the orodispersible tablets obtained with the said granulate and to a process of production for obtaining the said granulate.

1 . A granulate comprising a mixture of mannitol and sorbitol in a ratio by weight of between approximately 70:30 and approximately 97:3. 
     
     
         2 . The granulate according to  claim 1 , comprising a mixture of mannitol and sorbitol in a ratio by weight of between approximately 80:20 and approximately 95:5. 
     
     
         3 . The granulate according to  claim 2 , comprising a mixture of mannitol and sorbitol in a ratio by weight of approximately 90:10. 
     
     
         4 . The granulate according to any one of  claims 1  to  3 , in which the said mixture is formed of granules having an average size of between 50 μm and 500 μm. 
     
     
         5 . The granulate according to  claims 4 , in which the said mixture is formed of granules having an average size of between 150 μm and 350 μm. 
     
     
         6 . The granulate according to any one of  claims 1  to  5 , characterised in that it has a residual moisture content of less than 0.20% by weight relative to the weight of the same granulate. 
     
     
         7 . The granulate according to  claim 6 , characterised by a residual moisture content equal to or lower than 0.10% by weight. 
     
     
         8 . The granulate according to any one of  claims 1  to  7 , characterised by a compressibility index of more than 4.5. 
     
     
         9 . An orodispersible tablet comprising at least one active ingredient dispersed in a granulate comprising a mixture of mannitol and sorbitol in a ratio by weight of between approximately 70:30 and approximately 97:3. 
     
     
         10 . The tablet according to  claim 9 , in which the quantity of the said granulate is equal to or greater than 50% by weight relative to the weight of the said tablet. 
     
     
         11 . The tablet according to either of  claim 9  or  10 , in which the said active ingredient is selected from the group comprising non-steroidal anti-inflammatory drugs (NSAIDs), anxiolytics, antiemetics, antihistaminics and proton pump inhibitors. 
     
     
         12 . The tablet according to any one of  claims 9  to  11 , comprising a further excipient selected from the group consisting of diluents, sweeteners and flavourings. 
     
     
         13 . A process for the production of a granulate comprising mannitol and sorbitol, the said process comprising the following steps:
 (i) providing mannitol and sorbitol in the form of powder,   (ii) providing a mixture of the said mannitol and the said sorbitol in a ratio by weight of between approximately 70:30 and approximately 97:3,   (iii) introducing the said mixture into a fluidised bed granulator,   (iv) granulating the said mixture under the following conditions:
 (a) spraying a quantity of water of between 5% and 35% by weight with respect to the weight of the said mixture, and 
 (b) introducing air at a temperature below 80° C. with a moisture content of less than 5000 ppm. 
   
     
     
         14 . The process according to  claim 13 , in which the said mannitol has an average particle size of less than 100 μm and the said sorbitol has an average particle size of between 200 μm and 250 μm. 
     
     
         15 . The process according to  claim 13  or  14 , in which the said mixture has an average particle size of less than 200 μm, preferably between 100 μm and 150 μm. 
     
     
         16 . The process according to any one of  claims 13  to  15 , in which the said mixture has a ratio by weight between the said mannitol and the said sorbitol between approximately 80:20 and approximately 95:5. 
     
     
         17 . The process according to any one of  claims 13  to  16 , in which the quantity of water is between 15% and 25% by weight with respect to the weight of the mixture. 
     
     
         18 . The process according to any one of  claims 13  to  17 , in which the said air has a temperature between 65° C. and 75° C. 
     
     
         19 . The process according to any one of  claims 13  to  18 , in which the said air has a moisture content equal to or lower than 1000 ppm.