Crystal of pyrrolidylthiocarbapenem derivative, lyophilized...

C - Chemistry – Metallurgy – 07 – D

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C07D 477/20 (2006.01) A61K 9/19 (2006.01) A61K 31/407 (2006.01)

Patent

CA 2188529

The present invention provides a crystal of (1R,5S,6S)-6-[(1R)-1-hydroxyethyl]-2-[(3S,5S)-5- sulfamoylaminomethyl-1-pyrrolidin-3-yl]thio-1-methyl-1- carba-2-penem-3-carboxylic acid represented by the following formula, a lyophilized preparation comprising the crystal, and a process for producing the same. The production process comprises the steps of freezing an aqueous solution containing the above-mentioned compound by cooling to -20°C or lower; warming the frozen solution to 0 to -10°C; and cooling and warming the frozen solu- tion at least twice in a temperature range of 0 to -10°C. Image

Cristal d'acide (1R, 5S, 6S)-6-[(1R)-1-hydroxyéthyl]-2-[(3S, 5S)-5-sulfamoylaminométhyl-1-pyrrolidin-3-yl]thio-1-méthyl-1-carba-2-penem-3-carboxylique représenté par la formule (I). Le procédé de production d'une préparation lyophilisée contenant les cristaux comprend l'étape de congélation d'une solution aqueuse du composé précité par refroidissement à -20 DEG C ou moins, l'étape de réchauffement de la solution congelée entre 0 et -10 DEG C, et l'étape de refroidissement et de réchauffement de la solution au moins deux fois dans la plage de températures comprise entre 0 et -10 DEG C.

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