Stabilisation of metastable polymorphs: the case of paracetamol form III

Richard Telford; Colin C. Seaton; Alexander Clout; Asma Buanz; Simon Gaisford; Gareth R. Williams; Timothy J. Prior; Chidera H. Okoye; Tasnim Munshi; Ian J. Scowen

doi:10.1039/C6CC05006A

Stabilisation of metastable polymorphs: the case of paracetamol form III†

Richard Telford,^a Colin C. Seaton,^a Alexander Clout,^b Asma Buanz,^b Simon Gaisford,^b Gareth R. Williams,

^b Timothy J. Prior,^c Chidera H. Okoye,^d Tasnim Munshi^d and Ian J. Scowen*^d

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* Corresponding authors

^a School of Chemistry and Forensic Sciences, University of Bradford, Richmond Road, Bradford, UK

^b UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK

^c Department of Chemistry, University of Hull, Cottingham Road, Hull, UK

^d School of Chemistry, University of Lincoln, Lincoln LN6 7DL, UK
E-mail: iscowen@lincoln.ac.uk

Abstract

The design of a melt synthesis of the first air-stable formulation of the metastable form III of paracetamol is derived from thermo-spectroscopic and thermo-diffraction experiments. Melt crystallisation in the presence of β-1,4-saccharides produces form III selectively and the excipients appear to act as stabilising ‘active’ templates of the metastable polymorph.

This article is part of the themed collection: Pharmaceutical Solids

Chemical Communications

Stabilisation of metastable polymorphs: the case of paracetamol form III†

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Stabilisation of metastable polymorphs: the case of paracetamol form III

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