Formulation of liquid propofol as a cocrystalline solid

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McKellar, Scott C. and Kennedy, Alan R. and McCloy, Neil C. and McBride, Eileen and Florence, Alastair J. (2014) Formulation of liquid propofol as a cocrystalline solid. Crystal Growth and Design, 14 (5). pp. 2422-2430. ISSN 1528-7483 (https://doi.org/10.1021/cg500155p)

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Abstract

This work details a crystal engineering strategy to obtain a novel solid form of the liquid drug molecule propofol using isonicotinamide as a cocrystal former. Knowledge of intermolecular hydrogen bonded supramolecular synthons has been exploited to select a potential cocrystal former based on the likely growth unit formed. The structure of the cocrystal, solved using single-crystal X-ray diffraction, is reported, confirming the molecular packing and key intermolecular interactions adopted in the novel solid form. The potential to enhance a drug’s properties is demonstrated by an increased melting point compared to the native drug form, such that the liquid drug becomes a stable solid at room temperature. Unusually, the propofol/isonicotinamide complex has three structurally similar, temperature-dependent polymorphs, and the crystal structure of each form is reported herein.

ORCID iDs

McKellar, Scott C., Kennedy, Alan R. ORCID logoORCID: https://orcid.org/0000-0003-3652-6015, McCloy, Neil C., McBride, Eileen and Florence, Alastair J. ORCID logoORCID: https://orcid.org/0000-0002-9706-8364;
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