CRYSTALLINE OF CARBAPENEM DERIVATIVE OR ITS HYDRATE, PREPARATION METHODS AND USES THEREOF
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United States of America Patent
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Issued Date -
Mar 28, 2013
app pub date -
May 20, 2011
filing date -
May 21, 2010
priority date (Note) -
Abandoned
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Abstract
The present invention relates to a crystalline form of carbapenems derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid_as represented by formula (I) or hydrate thereof and the preparation methods thereof, wherein said method comprise: dissolving the compound as represented by formula (I) by an aqueous solution of N,N′-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), and then adding a poor solvent dropwise to this solution, filtering and drying to obtain a crystal. Another method comprises: formulating the compound as represented by formula (I) as an aqueous suspension; after adjusting pH until complete dissolution, adding a mixed solvent of organic solvent/water with a certain volume ratio; adjusting pH to 5.4-7.0, cooling to low temperature, filtering and drying to obtain a crystal. The invention also relates to the use of the crystalline form of compound A or hydrate thereof in the preparation of a medicament for treating and/or preventing infectious diseases. The invention further relates to a pharmaceutical composition comprising the crystalline form of compound A or hydrate thereof and one or more pharmaceutical carriers and/or diluents.
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