Prediction of polymorphic transformations of paracetamol in solid dispersions

Maniruzzaman, Mohammed and Islam, Muhammad T. and Moradiya, Hiren G. and Halsey, Sheelagh A. and Slipper, Ian J. and Chowdhry, Babur Z. and Snowden, Martin J. and Douroumis, Dennis (2014) Prediction of polymorphic transformations of paracetamol in solid dispersions. Journal of Pharmaceutical Sciences, 103 (6). pp. 1819-1828. ISSN 1520-6017

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Abstract

A novel approach employing variable-temperature X-ray powder diffraction (VTXRPD) was used to exploit its suitability as an off-line predictive tool to study the polymorphic transformations of paracetamol (PMOL) in melt-extruded hydrophilic polymer matrices. Physical mixtures (PMs) and extruded formulations of PMOL with either polyvinyl caprolactam graft copolymer (Soluplus®) or vinylpyrrolidone–vinyl acetate copolymer (Kollidon®) in the solid state were characterized by using differential scanning calorimetry, hot-stage microscopy, and scanning electron microscopy. The experimental findings from VTXRPD showed that the stable Form I (monoclinic) of PMOL transformed to the metastable polymorph Form II (orthorhombic) at temperatures varying from 112°C to 120°C, in both the PMs and extrudates suggesting an effect of both temperature and identity of the polymers. The findings obtained from VTXRD analysis for both the PMs and the extruded formulations were confirmed by in-line near-infrared (NIR) monitoring during the extrusion processing. In the NIR study, PMOL underwent the same pattern of polymorphic transformations as those detected using VTXPRD. The results of this study suggest that VTXRPD can be used to predict the polymorphic transformation of drugs in polymer matrices during extrusion processing and provides a better understanding of extrusion processing parameters.

ORCID iDs

Maniruzzaman, Mohammed, Islam, Muhammad T. ORCID logoORCID: https://orcid.org/0000-0002-3530-0519, Moradiya, Hiren G., Halsey, Sheelagh A., Slipper, Ian J., Chowdhry, Babur Z., Snowden, Martin J. and Douroumis, Dennis;
  • Item type:Article
    ID code:53178
    Dates:
    Date
    Event
    1 June 2014
    Published
    30 April 2014
    Published Online
    Keywords:polymorphs, crystals, drug delivery, polynorphism, near-infrared spectroscopy, extrudates, caprolactam, variable-temperature XRPD, transformation, Pharmacy and materia medica, Pharmacology, Toxicology and Pharmaceutics(all)
    Subjects:Medicine > Pharmacy and materia medica
    Department:Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
    Depositing user: Pure Administrator
    Date deposited:02 Jun 2015 09:45
    Last modified:20 Jan 2021 22:09
    URI:https://strathprints.strath.ac.uk/id/eprint/53178
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