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.

Physico-chemical study of the solid forms of a new drug

MARINI, AMEDEO;BERBENNI, VITTORIO;BRUNI, GIOVANNA;MARGHERITIS, CHIARA;
2001-01-01

Abstract

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.
2001
The Physical Chemistry/Chemical Physics category includes resources on photochemistry, solid state chemistry, kinetics, catalysis, quantum chemistry, surface chemistry, electro-chemistry, chemical thermodynamics, thermo-physics, colloids, fullerenes and zeolites. Resources dealing with (liquid) crystals and crystallography are also included in this category. This category also includes resources on atomic, molecular and chemical physics, which concerns the structure of atoms and molecules, atomic and molecular interactions with radiation, magnetic resonance and relaxation, Mossbauer effect, and atomic and molecular collision processes and interactions.
Sì, ma tipo non specificato
Inglese
Internazionale
STAMPA
90
12
2131
2140
THERMODINAMICS; Polimorphisms; hydrates; dehydration; Thermal methods
5
info:eu-repo/semantics/article
262
Marini, Amedeo; Berbenni, Vittorio; Bruni, Giovanna; Margheritis, Chiara; Orlandi, Alessandra
1 Contributo su Rivista::1.1 Articolo in rivista
none
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11571/133243
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