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Solid state characterization of mometasone furoate anhydrous and monohydrate forms

✍ Scribed by Xiaoming (Sean) Chen; Matthew Carillo; R. Curtis Haltiwanger; Prudence Bradley

Publisher
John Wiley and Sons
Year
2005
Tongue
English
Weight
335 KB
Volume
94
Category
Article
ISSN
0022-3549

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✦ Synopsis

Mometasone furoate is a potent glucocorticoid anti-inflammatory agent. Its anhydrous Form 1 and monohydrate form were characterized by X-ray crystallography, X-ray powder diffraction at ambient and elevated temperature, thermal analysis, FT-IR, and dynamic moisture adsorption. In Form 1, mometasone furoate molecules pack tightly with molecules interlocked in a space group of P2 1 2 1 2 1 . The monohydrate form crystallizes in space group P1. The unit cell of the monohydrate contains one water molecule and one mometasone furoate molecule. The water molecules form channels along the a axis and mometasone furoate molecules pack in layers in the same direction. Dehydration was observed between 60 and 1008C by thermogravimetric analysis with a heating rate of 108C/min. It corresponds to a broad endotherm over the same temperature range in the differential scanning calorimetry with the same heating rate. Variable temperature X-ray powder diffraction reveals that a new anhydrous form (Form 2) was fully produced above 908C. This crystalline form was converted to Form 1 after being heated above 1508C; and was totally converted to the monohydrate after 1 day at 238C, 45% RH.

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