3'-[(2z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4h-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid bis-(monoethanolamine)

Abstract

Disclosed are novel pharmaceutical compositions containing 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinol-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.

What is claimed is: 
     
         1 . The pharmaceutical tablet comprising:
 a) a drug, which is 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine);   wherein,   b) 90% of the drug particles have a particle size greater than 10 micron but less than 90 micron.   
     
     
         2 . A method of treating thrombocytopenia in a human in need thereof which comprises administering to such human a therapeutically effective amount of a pharmaceutical tablet according to  claim 1 . 
     
     
         3 . A process for preparing pharmaceutical tablets containing the compound of  claim 1 , which process comprises the steps of;
 a) admixing:
 the compound 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine), wherein 90% of the compound particles have a particle size of greater than 10 micron but less than 90 micron; and 
 one or more excipients; 
 to form a mixture; and 
   b) compressing the mixture into tablets.   
     
     
         4 . The pharmaceutical tablet comprising:
 a) a drug, which is 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine);   wherein,   b) 90% of the drug particles have a particle size greater than 20 micron but less than 50 micron.   
     
     
         5 . A method of treating thrombocytopenia in a human in need thereof which comprises administering to such human a therapeutically effective amount of a pharmaceutical tablet according to  claim 4 . 
     
     
         6 . A process for preparing pharmaceutical tablets containing the compound of  claim 4 , which process comprises the steps of;
 a) admixing:
 the compound 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine), wherein 90% of the drug particles have a particle size greater than 20 micron but less than 50 micron; and 
 one or more excipients; 
 to form a mixture; and 
   b) compressing the mixture into tablets.   
     
     
         7 . The pharmaceutical tablet comprising:
 a) a drug, which is 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine);   wherein,   b) 50% of the drug particles have a particle size greater than 5 micron but less than 50 micron.   
     
     
         8 . A method of treating thrombocytopenia in a human in need thereof which comprises administering to such human a therapeutically effective amount of a pharmaceutical tablet according to  claim 7 . 
     
     
         9 . A process for preparing pharmaceutical tablets containing the compound of  claim 7 , which process comprises the steps of;
 a) admixing:
 the compound 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine), wherein 50% of the drug particles have a particle size greater than 5 micron but less than 50 micron; and 
 one or more excipients; 
 to form a mixture; and 
   b) compressing the mixture into tablets.