Dissolution properties, solid-state transformation and polymorphic crystallization: progesterone case study

ARAJA-SIBAJA, A.M.; PAULINO A.S.; RAUBER G.S.; CAMPOS C.E.; CARDOSO S.G.; MONTI G.A.; HEREDIA V.; BIANCO I.D.; BELTRAMO D.M.; CUFFINI S.L.

TAYLOR & FRANCIS INC

Lugar: Londres; Año: 2014 vol. 19 p. 779 - 779

rogesterone is a natural steroid hormone and a poor soluble drug which presents two polymorphs (forms 1 and 2). Different methods to obtain form 2 were tested and a complete solid-state characterization of both polymorphs (forms 1 and 2) was conducted. X-ray powder diffraction, hot stage microscopy, Fourier transform infrared, dispersive Raman, 13C solid-state nuclear magnetic resonance spectroscopy, thermal analysis, scanning electron microscopy techniques and intrinsic dissolution rates (IDR) were applied to investigate physical?chemical and dissolution properties of these two polymorphs. Form 2 was obtained from diluted solutions and from melting after cooling at room temperature. Form 1 was obtained from concentrated solutions and, a mixture of both polymorphs was crystallized from intermediate solutions. The crystal habit was not a distinctive characteristic of each polymorph. The effect of mechanical stress was evaluated in the metastable polymorph (form 2). We observe