A Study of Fasoracetam's Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical

Bram Harmsen; Koen Robeyns; Johan Wouters; Tom Leyssens

doi:10.1016/j.xphs.2017.01.016

A Study of Fasoracetam's Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical

Bram Harmsen, Koen Robeyns, Johan Wouters, Tom Leyssens

Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

Résumé

Different solid state forms of the research chemical fasoracetam, which counters the effects of Alzheimer's disease, have been subjected to a thermal and structural analysis. Single crystals were obtained from solution evaporation and from the melt. Single-crystal X-ray analyses of the crystals show the existence of 2 hydrated and 1 non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57C. This low melting point, combined with possible water losses could cause problems when formulating the hydrated form and impact the storage conditions of the compound.

langue originale	Anglais
Pages (de - à)	1317-1321
Nombre de pages	5
journal	Journal of Pharmaceutical Sciences
Volume	106
Numéro de publication	5
Les DOIs	https://doi.org/10.1016/j.xphs.2017.01.016
Etat de la publication	Publié - 1 mai 2017

Accès au document

10.1016/j.xphs.2017.01.016

Autres fichiers et liens

Link to publication in Scopus

Physico-chimie et caractérisation (PC2)
Wouters, J. (!!Manager), Aprile, C. (!!Manager) & Fusaro, L. (!!Manager)
Plateforme technologique Caracterisation physico-chimiques
Equipement/installations: Plateforme technolgique
Plateforme Technologique Calcul Intensif
Champagne, B. (!!Manager)
Plateforme technologique Calcul intensif
Equipement/installations: Plateforme technolgique

CCDC 1489557: Experimental Crystal Structure Determination
Harmsen, B. (Contributeur), Leyssens, T. (Contributeur), Robeyns, K. (Contributeur) & Wouters, J. (Contributeur), Cambridge Crystallographic Data Centre, 1 janv. 2017
DOI: 10.5517/ccdc.csd.cc1m007w, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccdc.csd.cc1m007w&sid=DataCite
Ensemble de données
CCDC 1489556: Experimental Crystal Structure Determination
Harmsen, B. (Contributeur), Leyssens, T. (Contributeur), Robeyns, K. (Contributeur) & Wouters, J. (Contributeur), Cambridge Crystallographic Data Centre, 1 janv. 2017
DOI: 10.5517/ccdc.csd.cc1m006v, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccdc.csd.cc1m006v&sid=DataCite
Ensemble de données
CCDC 1489558: Experimental Crystal Structure Determination
Harmsen, B. (Contributeur), Leyssens, T. (Contributeur), Robeyns, K. (Contributeur) & Wouters, J. (Contributeur), Cambridge Crystallographic Data Centre, 1 janv. 2017
DOI: 10.5517/ccdc.csd.cc1m008x, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccdc.csd.cc1m008x&sid=DataCite
Ensemble de données

Contient cette citation

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title = "A Study of Fasoracetam's Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical",

abstract = "Different solid state forms of the research chemical fasoracetam, which counters the effects of Alzheimer's disease, have been subjected to a thermal and structural analysis. Single crystals were obtained from solution evaporation and from the melt. Single-crystal X-ray analyses of the crystals show the existence of 2 hydrated and 1 non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57C. This low melting point, combined with possible water losses could cause problems when formulating the hydrated form and impact the storage conditions of the compound.",

keywords = "Alzheimer's disease, calorimetry (DSC), crystal structure, hydrate, polymorphism, solvent evaporation, thermogravimetric analysis",

author = "Bram Harmsen and Koen Robeyns and Johan Wouters and Tom Leyssens",

year = "2017",

month = may,

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doi = "10.1016/j.xphs.2017.01.016",

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T1 - A Study of Fasoracetam's Solid State Forms

T2 - A Potential Anti-Alzheimer Pharmaceutical

AU - Harmsen, Bram

AU - Robeyns, Koen

AU - Wouters, Johan

AU - Leyssens, Tom

PY - 2017/5/1

Y1 - 2017/5/1

N2 - Different solid state forms of the research chemical fasoracetam, which counters the effects of Alzheimer's disease, have been subjected to a thermal and structural analysis. Single crystals were obtained from solution evaporation and from the melt. Single-crystal X-ray analyses of the crystals show the existence of 2 hydrated and 1 non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57C. This low melting point, combined with possible water losses could cause problems when formulating the hydrated form and impact the storage conditions of the compound.

AB - Different solid state forms of the research chemical fasoracetam, which counters the effects of Alzheimer's disease, have been subjected to a thermal and structural analysis. Single crystals were obtained from solution evaporation and from the melt. Single-crystal X-ray analyses of the crystals show the existence of 2 hydrated and 1 non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57C. This low melting point, combined with possible water losses could cause problems when formulating the hydrated form and impact the storage conditions of the compound.

KW - Alzheimer's disease

KW - calorimetry (DSC)

KW - crystal structure

KW - hydrate

KW - polymorphism

KW - solvent evaporation

KW - thermogravimetric analysis

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U2 - 10.1016/j.xphs.2017.01.016

DO - 10.1016/j.xphs.2017.01.016

M3 - Article

AN - SCOPUS:85012895637

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VL - 106

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JO - Journal of Pharmaceutical Sciences

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ER -

A Study of Fasoracetam's Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical

Résumé

Accès au document

Autres fichiers et liens

Empreinte digitale

Équipement

Physico-chimie et caractérisation (PC2)

Plateforme Technologique Calcul Intensif

Ensembles de données

CCDC 1489557: Experimental Crystal Structure Determination

CCDC 1489556: Experimental Crystal Structure Determination

CCDC 1489558: Experimental Crystal Structure Determination

Contient cette citation