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Polymorphic Crystallization and Structural Aspects of Agomelatine Metastable Form X Prepared by Combined Antisolvent/Cooling Process

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F16%3A43901963" target="_blank" >RIV/60461373:22340/16:43901963 - isvavai.cz</a>

  • Alternative codes found

    RIV/60461373:22310/16:43901963

  • Result on the web

    <a href="http://pubs.acs.org/doi/abs/10.1021/acs.oprd.5b00241" target="_blank" >http://pubs.acs.org/doi/abs/10.1021/acs.oprd.5b00241</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1021/acs.oprd.5b00241" target="_blank" >10.1021/acs.oprd.5b00241</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Polymorphic Crystallization and Structural Aspects of Agomelatine Metastable Form X Prepared by Combined Antisolvent/Cooling Process

  • Original language description

    Polymorphism is of great interest to the pharmaceutical industry because polymorphs have different physicochemical properties such as dissolution rate. In the present work, the influence of process conditions on the polymorphic antisolvent crystallization and transformations during cooling crystallization of agomelatine metastable form X from water/methanol solution has been investigated with a view of designing a robust process that includes not only crystallization but also filtration, filter cake washing, and drying. The competitive stability method was used in order to identify regions of the parametric space (water/methanol ratio, process temperature, and initial concentration) in which the crystallization of form X can be feasible. The formation of agomelatine form X was confirmed by subsequent kinetic experiments. The influence of process parameters such as the intensity of agitation, the antisolvent addition rate, and the precipitation temperature on the yield and particle size of the crystalline product was also investigated. The batch antisolvent crystallization of the metastable form X was monitored using in-line Raman spectroscopy and FBRM probe, and the type of the resulting polymorph has been confirmed by X-ray powder diffraction (XRPD). Finally, the effect of the obtained crystals of metastable form X on downstream operations-namely, filtration and drying-has been studied.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    CI - Industrial chemistry and chemical engineering

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/GA15-05534S" target="_blank" >GA15-05534S: Structure-property relationships and breakage dynamics of complex granular material</a><br>

  • Continuities

    S - Specificky vyzkum na vysokych skolach

Others

  • Publication year

    2016

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Organic Process Research &amp; Development

  • ISSN

    1083-6160

  • e-ISSN

  • Volume of the periodical

    20

  • Issue of the periodical within the volume

    1

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    11

  • Pages from-to

    33-43

  • UT code for WoS article

    000369880400004

  • EID of the result in the Scopus database