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

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	1317-1321
Number of pages	5
Journal	Journal of Pharmaceutical Sciences
Volume	106
Issue number	5
DOIs	https://doi.org/10.1016/j.xphs.2017.01.016
Publication status	Published - 1 May 2017

Keywords

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

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10.1016/j.xphs.2017.01.016

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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",

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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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DO - 10.1016/j.xphs.2017.01.016

M3 - Article

AN - SCOPUS:85012895637

SN - 0022-3549

VL - 106

SP - 1317

EP - 1321

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

IS - 5

ER -

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

Abstract

Keywords

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High Performance Computing Technology Platform

Physical Chemistry and characterization(PC2)

CCDC 1489557: Experimental Crystal Structure Determination

CCDC 1489558: Experimental Crystal Structure Determination

CCDC 1489556: Experimental Crystal Structure Determination

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

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Equipment

High Performance Computing Technology Platform

Physical Chemistry and characterization(PC2)

Datasets

CCDC 1489557: Experimental Crystal Structure Determination

CCDC 1489558: Experimental Crystal Structure Determination

CCDC 1489556: Experimental Crystal Structure Determination

Cite this