Pharmaceutical excipient having improved compressibility

Abstract

A method of preparing an excipient composition includes forming an aqueous slurry containing a mixture of microcrystalline cellulose in the form of a wet cake and a surfactant, said surfactant being present in an amount from about 0.1% to about 0.5% by weight of the wet-cake microcrystalline cellulose; and drying said slurry to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimiate association with said surfactant. The excipient may be mixed with a therapeutically active agent to form a dosage form. The surfactant provides a hydrophobic boundary at cellulose surfaces, and improves absorptivity of the therapeutically active agent.

1 . A method of preparing an excipient composition, comprising 
 forming an aqueous slurry containing a mixture of microcrystalline cellulose in the form of a wet cake and a surfactant, and    drying said slurry to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimate association with said surfactant, said surfactant being present in an amount sufficient to augment the compressibility of the microcrystalline cellulose, wherein said amount is from about 0.1% to about 0.5% by weight of the microcrystalline cellulose.    
     
     
         2 . The method of  claim 1 , wherein said surfactant is an ionic surfactant.  
     
     
         3 . The method of  claim 2 , wherein said ionic surfactant is an anionic surfactant.  
     
     
         4 . The method of  claim 3 , wherein said anionic surfactant is sodium lauryl sulfate.  
     
     
         5 . The method of  claim 3 , wherein said anionic surfactant is docusate sodium.  
     
     
         6 . The method of  claim 1 , wherein said surfactant is included in an amount of from about 0.15% to about 0.4%, based on the weight of said microcrystalline cellulose.  
     
     
         7 . The method of  claim 1 , wherein said surfactant is included in an amount of from about 0.2% to about 0.3%, based on the weight of said microcrystalline cellulose.  
     
     
         8 . The method of  claim 1 , wherein said excipient composition comprises particles having an average particle size of from about 10 μm to about 1,000 μm.  
     
     
         9 . The method of  claim 1 , wherein said excipient particles have an average particle size of from about 10 μm to about 500 μm.  
     
     
         10 . The method of  claim 1 , wherein said excipient particles have an average particle size of from about 30 μm to about 250 μm.  
     
     
         11 . The method of  claim 1 , wherein said excipient particles have an average particle size of from about 40 μm to about 200 μm.  
     
     
         12 . The method of  claim 1 , wherein said excipient composition has a moisture content from about 0.5% to about 15%.  
     
     
         13 . The method of  claim 1 , wherein said excipient composition further comprises from about 0.1 to about 20% by weight silicon dioxide, based on the weight of the microcrystalline cellulose.  
     
     
         14 . The method of  claim 1 , wherein said excipient composition further comprises from about 0.5 to about 10% by weight silicon dioxide, based on the weight of the microcrystalline cellulose.  
     
     
         15 . The method of  claim 1 , wherein said excipient composition further comprises from about 1.25 to about 5% by weight silicon dioxide, based on the weight of the microcrystalline cellulose.  
     
     
         16 . The method of  claim 14 , wherein said silicon dioxide is derived from colloidal silicon dioxide.  
     
     
         17 . The method of  claim 1 , wherein said excipient has a bulk density from about 0.2 g/ml to about 0.5 g/ml.  
     
     
         18 . The method of  claim 15 , wherein said excipient has a bulk density from about 0.22 g/ml to about 0.35 g/ml.  
     
     
         19 . The method of  claim 1 , wherein said excipient particles further comprise a member selected from the group consisting of non-silicon metal oxides, starches, starch derivatives, polyalkylene oxides, celluloses, cellulose ethers, cellulose esters and mixtures thereof.  
     
     
         20 - 34 . (canceled)