Method for producing a crystalline tableting additive, additive thus obtained and use thereof

Abstract

A method for producing a tableting additive, which method comprises providing a spray dried tableting additive in particulate form which particles at least partially consist of amorphous additive material and at least partially of crystalline additive material; and crystallising the amorphous additive material by subjecting the particles for a short time and under agitation to a temperature between 30 and 100° C. at a relative humidity between 60 and 25%. More in particular, the relationship between relative humidity and temperature is defined by the formula: % relative humidity =218−47*Ln(T(° C.)), wherein T(° C.) is the temperature to which the particles are subjected.

1 . Method for producing a tableting additive, which method comprises: 
 a) providing a spray dried tableting additive in particulate form which particles at least partially consist of amorphous additive material and at least partially of crystalline additive material; and    b) crystallising the amorphous additive material by subjecting the particles for a short time and under agitation to a temperature between 30 and 100° C. at a relative humidity between 60 and 25%.    
     
     
         2 . Method as claimed in  claim 1 , wherein the relative humidity is as defined by the formula: 
       % relative humidity=218−47*Ln( T (° C.)) 
       wherein T(° C.) is the temperature to which the particles are subjected.  
     
     
         3 . Method as claimed in  claim 1  or  2 , wherein the temperature is 36° C. and the relative humidity is more than 50%.  
     
     
         4 . Method as claimed in  claim 1  or  2 , wherein the temperature is 40° C. and the relative humidity lies between 50% and 65%.  
     
     
         5 . Method as claimed in  claim 1  or  2 , wherein the temperature is 47° C. and the relative humidity is about 48%.  
     
     
         6 . Method as claimed in  claim 1  or  2 , wherein the temperature is 53° C. and the relative humidity lies between 50% and 65%.  
     
     
         7 . Method as claimed in  claim 1  or  2 , wherein the temperature is 60° C. and the relative humidity lies 31 and 44%.  
     
     
         8 . Method as claimed in  claim 1  or  2 , wherein the temperature is 75° C. and the relative humidity is 25%.  
     
     
         9 . Method as claimed in claims  1 - 8 , wherein the short time is less than 10 minutes.  
     
     
         10 . Method as claimed in  claim 9 , wherein the short time is less than 5 min.  
     
     
         11 . Method as claimed in  claim 10 , wherein the short time is about 2 min.  
     
     
         12 . Method as claimed in claims  1 - 11 , wherein the agitation is provided by a fluid bed device.  
     
     
         13 . Method as claimed in claims  1 - 11 , wherein the agitation is a mechanical form of agitation.  
     
     
         14 . Method as claimed in claims  1 - 13 , wherein the additive material is lactose.  
     
     
         15 . Tableting additive being in particulate form, wherein the particles comprise substantially no or no additive material in amorphous form.  
     
     
         16 . Tableting additive as claimed in  claim 15 , obtainable by the method of claims  1 - 14 .  
     
     
         17 . Tableting additive as claimed in  claim 15  or  16 , wherein the additive is lactose.  
     
     
         18 . Tableting additive as claimed in  claim 17 , wherein the additive comprises 5-20% β-lactose based on the total lactose content, the remainder being lactose monohydrate particles and a maximum of 5% water.  
     
     
         19 . Tableting additive as claimed in  claim 18 , wherein the β-lactose is substantially in the form of α/β mix crystal.  
     
     
         20 . Use of the tableting additive as claimed in claims  15 - 19  for the preparation of tablets.