Physicochemical study of the solid forms of a new drug.
GV150526A is a new drug recently developed by GlaxoWellcome. It belongs to a novel group of 2-carboxyindole derivatives and is therapeutically effective in the treatment or prevention of CNS disorders resulting from neurotoxic damage. We present a physicochemical characterization of the three solid forms (hydrates) of GV150526A carried out mainly by thermal methods. It is shown that: (1) the different forms can be qualitatively and quantitatively distinguished by their thermal properties; (2) dehydration is followed or accompanied by a structural relaxation of the substrate that takes place at different rates and with different enthalpies in the three forms; (3) two of the solid forms can be converted into a phase that is thermodynamically stable at room temperature by partial dehydration/rehydration in a solid/vapor process.
Marini
A
A
C.S.G.I. e CSTE CNR - Dipartimento di Chimica Fisica, Università degli Studi di Pavia, Viale Taramelli 16, 27100 Pavia, Italy. marini@matsci.unipv.it
Berbenni
V
V
Bruni
G
G
Margheritis
C
C
Orlandi
A
A
D002152:Calorimetry, Differential Scanning; D003460:Crystallization; D003890:Desiccation; D004055:Differential Thermal Analysis; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry*; D006358:Hot Temperature; D007211:Indoles / Q000737:chemistry*; D008956:Models, Chemical; D017550:Spectroscopy, Fourier Transform Infrared; D013816:Thermodynamics; D013818:Thermogravimetry; D014961:X-Ray Diffraction
C105319:3-(2-((phenylamino)carbonyl)ethenyl)-4,6-dichloroindole-2-carboxylic acid; D018691:Excitatory Amino Acid Antagonists; D007211:Indoles