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Novel crystalline forms of gatifloxacin

Inactive Publication Date: 2005-12-29
NIDDAM HILDESHEIM VALERIE +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0055] In a further aspect, the present invention relates to methods of making hydrated E1, which method includes the step of treating gatifloxacin form E1-ACN solvate with a moist gas, especially moist gas of about 55% to about 75%-relative humidity at a temperature from ambient temperature to about 60° C., especially about 20° to 30° C.; although treating at 50° C. can be advantageous.

Problems solved by technology

However, it is generally not possible to predict whether a particular organic compound will form different crystalline forms, let alone predict the structure and properties of the crystalline forms themselves.
Absorption of atmospheric moisture by compound in powder form can impede its ability to flow.
The hemihydrate reportedly has disadvantages for manufacturing of solid oral dosage forms, e.g., tablets.

Method used

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  • Novel crystalline forms of gatifloxacin
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  • Novel crystalline forms of gatifloxacin

Examples

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Effect test

example 1

Form A

[0233] 3 g of gatifloxacin were slurried in 20 mL of iso-propanol (IPA). The mixture was slurried at ambient temperature for a slurry time of 24 hours with a magnetic stirrer. The mixture was filtered under vacuum, rinsed with iso-propanol (IPA) (10 mL) and analyzed by XRD analysis and showed to be form A.

example 2

Form B

[0234] 3 g of gatifloxacin were slurried in 20 mL of 1-butanol. The mixture was stirred at ambient temperature for a slurry time of 24 hours with a magnetic stirrer. Then the mixture was filtered under vacuum, the isolated solid rinsed with 1-butanol (10 mL), and analyzed by XRD analysis.

[0235] A second portion of the solid obtained after filtration was dried under vacuum at 50° C. for 24 hours. This resulted in a partially amorphous form B.

example 3

Form B

[0236] 3 g of gatifloxacin were slurried in 20 mL of EtOH absolute. The mixture was stirred at ambient temperature for a slurry time of 24 hours with a magnetic stirrer. Then the mixture was filtered under vacuum, the isolated solid rinsed with absolute EtOH (10 mL), and analyzed by XRD. The product was partially amorphous form B.

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Abstract

Provided are novel crystalline forms of gatifloxacin denominated forms A, B, C, D, E1, F, G, H, I, and J, and methods for their preparation. Also provided are methods for making known crystalline forms of gatifloxacin, in particular forms omega and T2RP.

Description

RELATED APPLICATIONS [0001] The present application claims the benefit of the filing date of the following U.S. Provisional Patent Applications: 60 / 379,510; 60 / 389,093; 60 / 401,672; 60 / 402,749; 60 / 409,860, 60 / 423,338; 60 / 432,961; 60 / 444,812; and 60 / 448,062.FIELD OF THE INVENTION [0002] The present invent relates to novel polymorphs and and pseudopolymorphs of (±) 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, commonly known as gatifloxacin. BACKGROUND OF THE INVENTION [0003] Gatifloxacin, known as (±) 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, has the following structure: [0004] Gatifloxacin, an anti-bacterial agent, is marketed as Tequin® by Bristol-Myers Squibb. Tequin® is available in a dosage of 200 and 400 mg in the form of a vial or a tablet, which can be either injected or taken orally. [0005] Many pharmaceutically active organic compounds can crystallize ...

Claims

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Application Information

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IPC IPC(8): C07D215/56
CPCC07D215/56
Inventor NIDDAM-HILDESHEIM, VALERIEWIZEL, SHLOMITSTERIMBAUM, GRETAAMIR, EHUD
Owner NIDDAM HILDESHEIM VALERIE
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