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    Co-crystal screening of poorly water-soluble active pharmaceutical ingredients. Application of hot stage microscopy on curcumin-nicotinamide system and construction of ternary phase diagram of fenbufen-nicotinamide-water co-crystal system.

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    Thesis (2.197Mb)
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    Publication date
    2010-03-10T16:44:43Z
    Author
    Chan, Hin Chung Stephen
    Supervisor
    Wright, Colin W.
    Keyword
    Curcumin
    Co-crystal
    Nicotinamide
    Fenbufen
    X-ray powder diffractometry
    Kofler hot stage microscopy
    Ternary phase diagram
    Differential scanning calorimetry
    Thermal gravimetric analysis
    Rights
    Creative Commons License
    The University of Bradford theses are licenced under a Creative Commons Licence.
    Institution
    University of Bradford
    Department
    The Institute of Pharmaceutical Innovation
    Awarded
    2009
    
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    Abstract
    Curcumin is the major phenolic diarylheptane derivative in Curcuma longa and has been reported to possess pharmacological activities. Unfortunately this compound suffers from poor bioavailability and rapid neutral-alkaline degradation. Co-crystal of curcumin is one option under exploration, motivated by the fact that a number of active pharmaceutical ingredient (API) co-crystals with improved dissolution have recently been synthesized. Hence, co-crystallization technique highlights an alternative means to improve the performance of curcumin. Within our work evidences for a co-crystal was ascertained from DSC, Kofler hot stage screening and PXRD, and all confirmed a new crystal phase could have been formed between curcumin and a co-crystallizing agent, nicotinamide. We report that re-crystallization step essentially aids the purification of commercial curcumin, a herbal based actives. Otherwise the prevalence of a new crystal phase in solvent-mediated co-crystallization will be significantly reduced. Besides, phase diagram is an effective tool for the study of solubility behaviours in co-crystal system. In order to acquire related techniques, fenbufen, a poorly water soluble drug, was selected. The result showed the huge difference in solubility between fenbufen and nicotinamide lead to difficulty in the construction of phase diagram.
    URI
    http://hdl.handle.net/10454/4253
    Type
    Thesis
    Qualification name
    MPhil
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