Agglomerates by crystallisation

Abstract

The present invention describes novel agglomerates in crystalline form of β-lactum compounds, Furthermore, a process for the preparation of said agglomerates, wherein a solution or suspension of at least one β-lactum compound in a solvent is mixed with one or more anti-solvents has been described.

1 . An agglomerate of potassium clavulanate crystals, wherein said agglomerate has a loose bulk density between about 0.20 and 0.60 g/mL, a tapped bulk density between about 0.50 and 0.90 g/mL, and a compressibility between about 10 and 40%, wherein said compressibility is calculated as 100 times the ratio of the difference between tapped bulk density and loose bulk density to the tapped bulk density, and said agglomerate has a weight percentage of between 0% and 10% potassium clavulanate crystals in the needle form, with the proviso that the rosette-like crystalline form of potassium clavulanate is excluded.  
     
     
         2 . The agglomerate of  claim 1 , wherein said agglomerate contains no potassium clavaulate crystals in the needle form.  
     
     
         3 . The agglomerate of  claim 1 , further comprising amoxicillin.  
     
     
         4 . The agglomerate of  claim 1 , further comprising one or more excipients.  
     
     
         5 . The agglomerate of  claim 4 , wherein said one or more excipients is selected from the group consisting of microcrystalline cellulose and silica.  
     
     
         6 . The agglomerate of  claim 1 , wherein said agglomerate has an average particle size between about 1 μm and 1500 μm.  
     
     
         7 . The agglomerate of  claim 6 , wherein said agglomerate has an average particle size of about 100 μm.  
     
     
         8 . The agglomerate of  claim 6 , wherein said agglomerate has an average particle size of about 1000 μm.  
     
     
         9 . A pharmaceutical formulation comprising the agglomerate of  claim 1  and one or more pharmaceutically acceptable excipients.  
     
     
         10 . The pharmaceutical formulation of  claim 9 , further comprising amoxicillin.  
     
     
         11 . The pharmaceutical formulation of  claim 9 , wherein said one or more pharmaceutically acceptable inert excipients is selected from the group consisting of microcrystalline cellulose and silica.  
     
     
         12 . A pharmaceutical dosage form comprising a pharmaceutical formulation of  claim 9.