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AssigneeEisai Co., Ltd.
InventorsHiroyuki Chiba, Masahiko Tsujii, Astsushi Koiwa, Shin Sakurai, Akio Kayano, Hiroyuki Ishizuka, Hiroyuki Saito, Taiju Nakamura, Ikuo Kushida, Yasuyuki Suzuki, Takako Yoshiba, Kazuhide Ashizawa, Masahiro Sakurai, Eiichi Yamamoto
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The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 Å, a process for producing them, and a powdery charged preparation for injection containing them.
(+)-(1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(2S,4S)-2-[(3R)-pyrrolidine-3-yl-(R)-hydroxymethyl]pyrrolidine-4-yl]thio-1-carbapen-2-em-3-carboxylic acid monohydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 Å, represented by the following formula (1-1):
A process for producing (+)-(1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(2S,4S)-2-[(3R)-pyrrolidine-3-yl-(R)-hydroxymethyl]pyrrolidine-4-yl]thio-1-carbapen-2-em-3-carboxylic acid monohydrochloride trihydrate crystals, which comprises dissolving (+)-(1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(2S,4S)-2-[(3R)-pyrrolidine-3-yl-(R)-hydroxymethyl]pyrrolidine-4-yl]thio-1-carbapen-2-em-3-carboxylic acid or a salt thereof in a solvent system consisting of water and isopropanol;
A process for producing (+)-(1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(2S,4S)-2-[(3R)-pyrrolidine-3-yl-(R)-hydroxymethyl]pyrrolidine-4-yl]thio-1-carbapen-2-em-3-carboxylic acid monohydrochloride trihydrate crystals, which comprises dissolving (+)-(1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2′-[(2S,4S)-2-[(3R)-pyrrolidine-3-yl-(R)-hydroxymethyl]pyrrolidine-4-yl]thio-1-carbapen-2-em-3-carboxylic acid monohydrochloride monohydrate crystals in 50 to 90% (v/v) aqueous isopropanol solution;
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