Crystalline Forms of D-Glucitol, 1-Deoxy-1-(Methylamino)-, 1-(6-Amino-3,5-Difluoropyridine-2-Yl)-8-Chloro-6-Fluoro-1,4-Dihydro-7-(3-Hydroxyazetidin-1-Yl)-4-Oxo-3-Quinolinecarboxylate

摘要

The present disclosure relates generally to crystalline forms of anhydrous D-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1- yl)-4-oxo-3-quinolinecarboyxlate, compositions comprising the same, and methods of making the same. Delafloxacin is an fluoroquinolone antibiotic with the chemical structure and the chemical name 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboyxlate. Studies have indicated the existence of three anhydrous polymorphs of delafloxacin, as well as a trihydrate and methanol and ethanol solvates.

主权项

1. A process for the preparation of a crystalline anhydrous Form 1A of D-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboyxlate, which comprises the steps of:
(a) drying delafloxacin meglumine trihydrate; and (b) exposing the dried delafloxacin meglumine to heat and humidity.