Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation

© 2018 The Royal Society of Chemistry. Fenofibrate (FEN) is a dyslipidemia treatment agent which is poorly soluble in water. FEN has tendency to form polymorphs and its crystallisation behaviour is difficult to predict. The nucleation process can be initiated by mechanical disruption such as ball mi...

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Main Authors: Pratchaya Tipduangta, Khaled Takieddin, László Fábián, Peter Belton, Sheng Qi
Format: Journal
Published: 2018
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http://cmuir.cmu.ac.th/jspui/handle/6653943832/58422
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Institution: Chiang Mai University
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spelling th-cmuir.6653943832-584222018-09-05T04:24:58Z Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation Pratchaya Tipduangta Khaled Takieddin László Fábián Peter Belton Sheng Qi Chemical Engineering Chemistry © 2018 The Royal Society of Chemistry. Fenofibrate (FEN) is a dyslipidemia treatment agent which is poorly soluble in water. FEN has tendency to form polymorphs and its crystallisation behaviour is difficult to predict. The nucleation process can be initiated by mechanical disruption such as ball milling or surface scratching which may result in different crystallisation behaviour to that observed in the unperturbed system. This study has obtained insights into the controllability of FEN crystallisation by means of regulating the exposed surface and growth temperatures during its crystallisation. The availability of an open top surface (OTS) during the crystallisation of the FEN melt resulted in a mixture containing FEN form I and IIa (I ≫ IIa) at room temperature, and in the range 40 to 70 °C. Covering the surface led to significant increases in the yield of form IIa at room temperature and at 40 and 50 °C. These temperatures also yielded the highest amount of form IIa in the OTS samples whilst crystallisation at 70 °C led to only FEN form I crystals regardless of the availability of the free surface. The metastable FEN form IIa transforms to the stable form I under the influence of a mechanical stress. Additionally, the introduction of OTS before the completion of crystallisation of form IIa led to a 'switch' of from IIa growth to form I. This study demonstrates that the polymorph selection of FEN can be obtained by the manipulation of the crystallisation conditions. 2018-09-05T04:23:53Z 2018-09-05T04:23:53Z 2018-01-01 Journal 20462069 2-s2.0-85045526216 10.1039/c8ra01182f https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85045526216&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/58422
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
topic Chemical Engineering
Chemistry
spellingShingle Chemical Engineering
Chemistry
Pratchaya Tipduangta
Khaled Takieddin
László Fábián
Peter Belton
Sheng Qi
Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation
description © 2018 The Royal Society of Chemistry. Fenofibrate (FEN) is a dyslipidemia treatment agent which is poorly soluble in water. FEN has tendency to form polymorphs and its crystallisation behaviour is difficult to predict. The nucleation process can be initiated by mechanical disruption such as ball milling or surface scratching which may result in different crystallisation behaviour to that observed in the unperturbed system. This study has obtained insights into the controllability of FEN crystallisation by means of regulating the exposed surface and growth temperatures during its crystallisation. The availability of an open top surface (OTS) during the crystallisation of the FEN melt resulted in a mixture containing FEN form I and IIa (I ≫ IIa) at room temperature, and in the range 40 to 70 °C. Covering the surface led to significant increases in the yield of form IIa at room temperature and at 40 and 50 °C. These temperatures also yielded the highest amount of form IIa in the OTS samples whilst crystallisation at 70 °C led to only FEN form I crystals regardless of the availability of the free surface. The metastable FEN form IIa transforms to the stable form I under the influence of a mechanical stress. Additionally, the introduction of OTS before the completion of crystallisation of form IIa led to a 'switch' of from IIa growth to form I. This study demonstrates that the polymorph selection of FEN can be obtained by the manipulation of the crystallisation conditions.
format Journal
author Pratchaya Tipduangta
Khaled Takieddin
László Fábián
Peter Belton
Sheng Qi
author_facet Pratchaya Tipduangta
Khaled Takieddin
László Fábián
Peter Belton
Sheng Qi
author_sort Pratchaya Tipduangta
title Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation
title_short Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation
title_full Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation
title_fullStr Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation
title_full_unstemmed Towards controlling the crystallisation behaviour of fenofibrate melt: Triggers of crystallisation and polymorphic transformation
title_sort towards controlling the crystallisation behaviour of fenofibrate melt: triggers of crystallisation and polymorphic transformation
publishDate 2018
url https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85045526216&origin=inward
http://cmuir.cmu.ac.th/jspui/handle/6653943832/58422
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