Ionic co-crystals of racetams: Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg2+ and Ca2+ chlorides

Fabrizia Grepioni; Johan Wouters; Dario Braga; Saverio Nanna; Baptiste Fours; Gérard Coquerel; Geraldine Longfils; Sandrine Rome; Luc Aerts; Luc Quéré

doi:10.1039/c4ce00409d

Ionic co-crystals of racetams: Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg²⁺ and Ca²⁺ chlorides

Fabrizia Grepioni, Johan Wouters, Dario Braga, Saverio Nanna, Baptiste Fours, Gérard Coquerel, Geraldine Longfils, Sandrine Rome, Luc Aerts, Luc Quéré

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

Abstract

Mechanochemical and solution based reactions of solid brivaracetam (BRV) and seletracetam (SEL), antiepileptic drugs from UCB's pipeline, with the inorganic salts MgCl₂ and CaCl₂, yield ionic co-crystals with changed or improved physico-chemical properties with respect to pure drugs (melting point, hygroscopicity, crystal morphology). All co-crystals are characterized via a combination of solid-state techniques, i.e. single crystal and powder X-ray diffraction, variable temperature X-ray diffraction, DSC, TGA and hot-stage microscopy (HSM).

Original language	English
Pages (from-to)	5887-5896
Number of pages	10
Journal	CrystEngComm
Volume	16
Issue number	26
DOIs	https://doi.org/10.1039/c4ce00409d
Publication status	Published - 14 Jul 2014
Externally published	Yes

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10.1039/c4ce00409d

Cite this

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title = "Ionic co-crystals of racetams: Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg2+ and Ca2+ chlorides",

abstract = "Mechanochemical and solution based reactions of solid brivaracetam (BRV) and seletracetam (SEL), antiepileptic drugs from UCB's pipeline, with the inorganic salts MgCl2 and CaCl2, yield ionic co-crystals with changed or improved physico-chemical properties with respect to pure drugs (melting point, hygroscopicity, crystal morphology). All co-crystals are characterized via a combination of solid-state techniques, i.e. single crystal and powder X-ray diffraction, variable temperature X-ray diffraction, DSC, TGA and hot-stage microscopy (HSM).",

author = "Fabrizia Grepioni and Johan Wouters and Dario Braga and Saverio Nanna and Baptiste Fours and G{\'e}rard Coquerel and Geraldine Longfils and Sandrine Rome and Luc Aerts and Luc Qu{\'e}r{\'e}",

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doi = "10.1039/c4ce00409d",

language = "English",

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T2 - Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg2+ and Ca2+ chlorides

AU - Grepioni, Fabrizia

AU - Wouters, Johan

AU - Braga, Dario

AU - Nanna, Saverio

AU - Fours, Baptiste

AU - Coquerel, Gérard

AU - Longfils, Geraldine

AU - Rome, Sandrine

AU - Aerts, Luc

AU - Quéré, Luc

PY - 2014/7/14

Y1 - 2014/7/14

N2 - Mechanochemical and solution based reactions of solid brivaracetam (BRV) and seletracetam (SEL), antiepileptic drugs from UCB's pipeline, with the inorganic salts MgCl2 and CaCl2, yield ionic co-crystals with changed or improved physico-chemical properties with respect to pure drugs (melting point, hygroscopicity, crystal morphology). All co-crystals are characterized via a combination of solid-state techniques, i.e. single crystal and powder X-ray diffraction, variable temperature X-ray diffraction, DSC, TGA and hot-stage microscopy (HSM).

AB - Mechanochemical and solution based reactions of solid brivaracetam (BRV) and seletracetam (SEL), antiepileptic drugs from UCB's pipeline, with the inorganic salts MgCl2 and CaCl2, yield ionic co-crystals with changed or improved physico-chemical properties with respect to pure drugs (melting point, hygroscopicity, crystal morphology). All co-crystals are characterized via a combination of solid-state techniques, i.e. single crystal and powder X-ray diffraction, variable temperature X-ray diffraction, DSC, TGA and hot-stage microscopy (HSM).

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Ionic co-crystals of racetams: Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg²⁺ and Ca²⁺ chlorides

Abstract

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Physical Chemistry and characterization(PC2)

CCDC 988340: Experimental Crystal Structure Determination

CCDC 988342: Experimental Crystal Structure Determination

CCDC 988343: Experimental Crystal Structure Determination

Cite this

Ionic co-crystals of racetams: Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg2+ and Ca2+ chlorides

Abstract

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Other files and links

Fingerprint

Equipment

Physical Chemistry and characterization(PC2)

Datasets

CCDC 988340: Experimental Crystal Structure Determination

CCDC 988342: Experimental Crystal Structure Determination

CCDC 988343: Experimental Crystal Structure Determination

Cite this

Ionic co-crystals of racetams: Solid-state properties enhancement of neutral active pharmaceutical ingredients via addition of Mg²⁺ and Ca²⁺ chlorides