Physically stable solid form of a fluoroquinolone

Details Physically stable solid form of a fluoroquinolone Physically stable solid form of a fluoroquinolone

1996-05-01

1999-11-16

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546156, A61K 3147, C07D21556

Patent

active

059858931

ABSTRACT:
Novel crystal forms of the fluoroquinolone, [S-(R*,S*)]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-[1-(methylam ino)ethyl]-1-pyrrolidinyl]-4-oxo-3-quinolinecarboxylic acid are disclosed. The forms are characterized by one methanol solvate form, and three anhydrous polymorphic forms, of which, Form III exhibits greatest stability and decreased hygroscopicity.

REFERENCES:
patent: 4521431 (1985-06-01), Crooks
patent: 5563155 (1996-10-01), Domagala
B. Sustar, N. Bukovec, and P. Bukovec, J. Therm. Anal. 40, 475-481 (1993).
Katdare, A.V.; J.A. Ryan; J. F. Bavitz, et al. Mikrochim Acta, (1986) vol. 3(1-2), pp. 1-12.
J. M. Domagala et al., Journal of medicinal chemistry, 36, 7, pp. 871-882 (1993).
Domagala JM, Hagen SE, Joannides T, Kiely JS, Laborde E, Schroeder MC, Sesnie JA, Shapiro MA, Suto MJ, Vanderroest S. (1993) J. Med. Chem. 36, 871-882.

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