Pharmaceutical granules

Abstract

A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients comprising at least 5% crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution; a substantially spherical granule for pharmaceutical use comprising famiciclovir and 5% or more crystalline cellulose, together with an optional coating; and a sachet containing a unit dose of famiciclovir in the form of such granules.

1 . A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients comprising at least 5% crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution.  
     
     
         2 . A method according to  claim 1 , wherein the medicament is caffeine which has an aqueous solubility 0.02 g/ml, pyridoxine hydrochloride which has an aqueous solubility of 0.22 g/ml or famciclovir and acyclovir which have an aqueous solubility of more than 0.25 g/ml.  
     
     
         3 . A method according to  claim 2  wherein the medicament is famciclovir.  
     
     
         4 . A method according to  claim 1 ,  2  or  3  wherein the proportion of medicament with respect to excipients in the composition of the granule is up to 25%.  
     
     
         5 . A method according to any one of  claims 2  to  4  wherein the mixture of medicament and excipients comprise at least 5% crystalline cellulose as the sole excipient.  
     
     
         6 . A method according to any one of  claims 1  to  5  where the amount of binder solution is regulated such that granules are suitable for administration by spoon and are generally more than 500 um in diameter.  
     
     
         7 . A method according to any one of  claims 1  to  5  wherein the granules are agitated in the granulator after spraying of the binder solution to improve the spherical shape and smooth the surface of the granules.  
     
     
         8 . A method according to  claim 1 , substantially as described herein with reference to any one of the Examples.  
     
     
         9 . A substantially spherical granule for pharmaceutical use comprising famciclovir and 5% or more crystalline cellulose, together with an optional coating.  
     
     
         10 . A granule according to  claim 9  comprising famciclovir and crystalline cellulose as the sole excipient.  
     
     
         11 . A granule according to  claim 10  containing approximately 25% famciclovir and approximately 75% cellulose.  
     
     
         12 . A granule according to  claim 9 , substantially as described herein with reference to any one of the Examples.  
     
     
         13 . A granule according to  claim 11  having a diameter of 500 to 1500 um.  
     
     
         14 . A sachet containing a unit dose of famciclovir in the form of granules as defined in any one of  claims 9  to  13 .