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Claims for Patent: 8,247,402

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Claims for Patent: 8,247,402

Title:Crystal form of pyrrolidylthiocarbapenem derivative
Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfa- moylaminomethyl)p yrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2.theta.) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) and a crystal of said compound having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2.theta.) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.
Inventor(s): Saitoh; Izumi (Hyogo, JP), Takahira; Masayuki (Hyogo, JP), Kawakita; Toshio (Hyogo, JP), Yoshioka; Yasuyuki (Hyogo, JP)
Assignee: Shiongi & Co., Ltd. (Osaka, JP)
Application Number:12/012,932
Patent Claims: 1. A crystal of a monohydrate of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfa- moylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carb- oxylic acid, said crystal having a powder X-ray diffraction pattern comprising peaks at diffraction angles (2.theta.) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees), wherein the powder X-ray diffraction pattern is obtainable using Cu K.alpha. ray, 1.34 Angstroms (monochromator), tube voltage 40 kV, and tube current 40 mA.

2. A medicament comprising a crystal of a monohydrate of (+)-(4R,5S,6S)-6-[1R)-1-hydroxyethyl]-4-methyl-7-oxo-3 [[(3S,5S)-5-(sulfamoylaminomethyl) pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid in a solid form, said crystal having a powder X-ray diffraction pattern comprising peaks at diffraction angles (2.theta.) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees), wherein the powder X-ray diffraction pattern is obtainable using Cu K.alpha. ray, 1.34 Angstroms (monochromator), tube voltage 40 kV, and tube current 40 mA; and one or more pharmaceutically acceptable ingredients.

3. A medicament according to claim 2, wherein the medicament is a powder filling preparation.

4. A method for producing a crystal according to claim 1, comprising the steps of: (A) dissolving (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3 [[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1azabicyclo[3.2.0- ]hept-2-ene-2-carboxylic acid or a hydrate thereof in water; (B) depositing crystals from the aqueous solution obtained in step (A); (C) determining the powder X-ray diffraction pattern of the crystals; (D) selecting a crystal having a powder X-ray diffraction pattern comprising peaks at diffraction angles (2.theta.) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees), wherein the powder X-ray diffraction pattern is obtainable using Cu K.alpha. ray, 1.34 Angstroms (monochromator), tube voltage 40 kV, and tube current 40 mA; and (E) drying the crystal obtained in step (D).

5. A method for preparing an injectable solution comprising the step of dissolving the crystal according to claim 1, or a medicament according to claim 2, in a physiologically acceptable agent.
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