A kind of crystal form of carbapenem antibacterial drug and preparation method thereof

Abstract

The invention provides a novel crystal form of a carbapenem antimicrobial medicament, namely, (+)-(4R,5S,6S)-3-[[(3S,5S)-5-(aminosulfonyl)aminomethyl]-3-pyrrolidine]sulfur]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclic[3,2,0]heptyl-2-ene-2-carboxylic acid-hydrate (doripenem). The X-ray powder diffraction pattern of the crystal powder shows main peaks when 2theta is equal to 15.20 degrees, 16.06 degrees, 16.83 degrees, 19.40 degrees, 21.29 degrees, 23.68 degrees, 24.08 degrees, 24.70 degrees, 26.28 degrees, 28.43 degrees, 29.17 degrees and 34.35 degrees. The novel crystal form has the advantages of easiness in preparation and industrial production, low cost, high solubility and high stability.

Description

technical field

[0001] The invention relates to a new crystal form of a drug, in particular to a carbapenem antibacterial drug (+)-(4R,5S,6S)-3-[[(3S,5S)-5-[[(aminosulfonyl)amino ]methyl]-3-pyrrolidine]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3,2,0]heptyl- New crystalline form of 2-ene-2-carboxylic acid monohydrate (doripenem) and process for its preparation. Background technique

[0002] Doripenem (S-4661) is a broad-spectrum carbapenem antibiotic developed by Shionogi Company in Japan. -1 stability and other advantages. Its chemical name is (+)-(4R,5S,6S)-3-[[(3S,5S)-5-[[(aminosulfonyl)amino]methyl]-3-pyrrolidine]sulfur]-6 -[(1R)-1-Hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylic acid monohydrate, the structural formula is as follows Formula (I) shown.

[0003]

[0004] Chinese patents CN200510021270.1 and CN92111069.3 describe the preparation of its amorphous powder. Due to the relatively poor stability of the amorphous pow...

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