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)
Disclosed are novel pharmaceutical compositions containing 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) (eltrombopag olamine) and processes for preparing the same.
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.