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Summary for Patent: 5,849,752
|Title:||Crystal modification of CDCH a process for its preparation and pharmaceutical formulations comprising this modification|
|Abstract:||The invention relates to the new monohydrate of 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo-[4.3.0]non-8-yl)6-fluoro-1,4-dihyd ro-8-methoxy-4-oxo-3-quinolinecarboxylic acid hydrochloride (CDCH), a process for its preparation and pharmaceutical formulations which comprise this monohydrate as the active compound.|
|Inventor(s):||Grunenberg; Alfons (Dormagen, DE), Bosche; Patrick (Odenthal, DE)|
|Assignee:||Bayer Aktiengesellschaft (Leverkusen, DE)|
1. Monohydrate of CDCH, of the formula ##STR2## which has a characteristic peak at 168.1 ppm in the .sup.13 C-NMR spectrum and a band at 2.THETA.=26.7 in the X-ray diffractogram.
2. Compound according to claim 1 in the prismatic crystal form.
3. Process for the preparation of the CDCH monohydrate according to claim 1, characterized in that anhydrous CDCH is treated with an amount of water which is at least sufficient for thorough mixing and hydration until the stoichiometric content of water of crystallization has been absorbed and conversion of the crystals is complete, the crystals of the monohydrate thus obtained are separated off and the adsorbed water present is removed.
4. Process according to claim 3, characterized in that a suspension of the anhydrous CDCH in aqueous media is stirred until hydration and conversion of the crystals is complete.
5. Process according to claim 3, characterized in that, to prepare the monohydrate in the form of prisms, anhydrous CDCH or CDCH monohydrate in the form of needles is dissolved in media having a water content which is stoichiometrically sufficient but limited to 10%, and the solvent is then removed.
6. Process according to claim 3, characterized in that anhydrous CDCH is exposed to humidity until the crystals have been converted quantitatively.
7. An antibacterial composition comprising an antibacterially effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
8. An antibacterial composition comprising an antibacterially effective amount of a compound according to claim 2 and a pharmaceutically acceptable carrier.
9. A method of combating bacteria in a patient comprising administering to said patient an antibacterially effective amount of a compound according to claim 1.
10. A method of combating bacteria in a patient comprising administering to said patient an antibacterially effective amount of a compound according to claim 2.
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