Pharmaceutical excipient having improved compressibility

Abstract

A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

1 - 64 . (Cancelled)  
     
     
         65 . A solid dosage form comprising: 
 a compressed mixture of from about 1% to about 99% of an excipient comprising a particulate agglomerate of coprocessed microcrystalline cellulose and from about 0.1% to about 20% by weight silicon dioxide, the microcrystalline cellulose and silicon dioxide being in intimate association with each other, said silicon dioxide portion of said agglomerate being derived from a silicon dioxide having an average primary particle size from about 1 nm to about 100 μm and from about 99% to about 1% of an active agent; and    a coating over said compressed mixture.    
     
     
         66 . The solid dosage form of  claim 65 , wherein the coating is a sustained release coating.  
     
     
         67 . The solid dosage form of  claim 66 , wherein the sustained release coating provides a sustained-release of the active agent over a period of at least 12 hours.  
     
     
         68 . The solid dosage form of  claim 65 , wherein the active agent is a systemically active therapeutic agent.  
     
     
         69 . The solid dosage form of  claim 65 , wherein the active agent is a locally active therapeutic agent.  
     
     
         70 . The solid dosage form of  claim 65 , wherein said coating comprises a hydrophobic polymer.  
     
     
         71 . The solid dosage form of  claim 65 , wherein said coating is an enteric coating  
     
     
         72 . The solid dosage form of  claim 65 , wherein said coating comprises a hydrophilic material.  
     
     
         73 . The solid dosage form of  claim 65 , wherein said coating is a support platform.  
     
     
         74 . The solid dosage form of  claim 73 , wherein said support platform partially coats the compressed mixture.  
     
     
         75 . The solid dosage form of  claim 65 , wherein a portion of the active agent is in the coating.  
     
     
         76 . A tablet comprising: 
 an excipient including microcrystalline cellulose in intimate association with 0.1% to 20% weight by weight SiO 2 ;    an active agent; and    a coating.    
     
     
         77 . The tablet of  claim 76 , wherein said coating comprises a hydrophobic polymer.  
     
     
         78 . The tablet of  claim 76 , wherein said coating is an enteric coating.  
     
     
         79 . The tablet of  claim 76 , wherein said coating comprises a hydrophilic material.  
     
     
         80 . The tablet of  claim 76 , wherein said coating is a support platform.  
     
     
         81 . The tablet of  claim 80 , wherein said support platform partially coats the tablet.  
     
     
         82 . The tablet of  claim 76 , wherein a portion of the active agent is in the coating.