Glyburide composition

Abstract

The present invention relates to a physical form of the known drug substance glyburide, also known as glibenclamide, and chemically defined as 5-chloro-N-[2-[4-[[[(cyclohexylamino)-carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxybenzamide (Merck Index, Tenth Edition, p. 642), as well as to dosage forms, e.g., tablets and capsules, incorporating said physical form of glyburide.

What is claimed is:  
     
         1 . The substance 5-chloro-N-[2-[4-[[[(cyclohexylamino)-carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxybenzamide having the following particle size distribution characteristics: 
 25% undersize value between 3 and 11 μm,    50% undersize value between 6 and 23 μm, and    75% undersize value between 15 and 46 μm.    
     
     
         2 . The substance of    claim 1    wherein the particle size distribution is 
 25% undersize value between 4 and 7 μm,  
 50% undersize value between 7 and 13 μm, and 75% undersize value between 17 and 23 μm.  
 
     
     
         3 . The use of the substance of    claim 1    in a tablet or capsule.  
     
     
         4 . A tablet or capsule comprising the substance of    claim 1    and a second drug, the second drug being a drug that is useful for the treatment of type II diabetes.  
     
     
         5 . The tablet or capsule of    claim 4    wherein the second drug is selected from the group consisting of glycosidase inhibitors, thiazolidonediones, biguanides and aglinides.  
     
     
         6 . The tablet or capsule of    claim 5    wherein the second drug is selected from the group consisting of acarbose, rosiglitazone, pioglitazone, metformin fumarate and repaglinide.  
     
     
         7 . A tablet or capsule comprising the substance of    claim 1    and at least one highly water soluble excipient.  
     
     
         8 . The tablet or capsule of    claim 7    wherein the at least one highly water soluble excipient comprises 45 to 90% by weight of the total formulation.  
     
     
         9 . A method of treating type II diabetes which comprises administering to a patient in need of such treatment a therapeutically effective amount of the substance of    claim 1   .  
     
     
         10 . The substance 5-chloro-N-[2-[4-[[[(cyclohexylamino)-carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxybenzamide having the following particle size distribution characteristics: 
 25% undersize value not more than 6 microns,    50% undersize value not more than 7 to 10 microns, and    75% undersize value not more than 21 microns.