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      Utilization of oriented crystal growth for screening of aromatic carboxylic acids cocrystallization with urea

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      Journal of Crystal Growth
      Elsevier BV

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          Summary

          The possibility of molecular complex formation in the solid state of urea with benzoic acid analogues was measured directly on the crystallite films deposited on the glass surface using powder X-ray diffractometry (PXRD). Obtained solid mixtures were also analyzed using Fourier transform infrared spectroscopy (FTIR). The simple droplet evaporation method was found to be efficient, robust, fast and cost-preserving approach for first stage cocrystal screening. Additionally, the application of orientation effect to cocrystal screening simplifies the analysis due to damping of majority of diffraction signals coming from coformers. During validation phase the proposed approach successfully reproduced both positive cases of cocrystallization (urea:salicylic acid and urea:4-hydroxy benzoic acid) as well as pairs of co-formers immiscible in the solid state (urea:benzoic acid and urea:acetylsalicylic acids). Based on validated approach new cocrystals of urea were identified in complexes with 3-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, 2,5-dihydroxybenzoic acid, 2,6-dihydroxybenzoic acid and 3,5-dihydroxybenzoic acid. In all cases formation of multicomponent crystal phase was confirmed by the appearance of new reflexes on the diffraction patterns and FTIR absorption band shifts of O–H and N–H groups.

           

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          https://www.infona.pl/resource/bwmeta1.element.elsevier-5c3813ca-d6e6-3963-bfa6-1da763947953

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          The role of solvent in mechanochemical and sonochemical cocrystal formation: a solubility-based approach for predicting cocrystallisation outcome

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            Pharmaceutical cocrystals and poorly soluble drugs.

            In recent years cocrystal formation has emerged as a viable strategy towards improving the solubility and bioavailability of poorly soluble drugs. In this review the success of numerous pharmaceutical cocrystals for the improvement of the solubility and dissolution rates of poorly soluble drugs is demonstrated using various examples taken from the literature. The role of crystal engineering principles in the selection of appropriate coformers and the nature of the supramolecular synthons present within the crystals are described. Evidence for improved animal pharmacokinetic data is given for several systems. A summary is provided of our current understanding of the relationship between cocrystal structure and solution phase interactions on solubility as well as those factors that influence overall cocrystal thermodynamic stability.
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              Pharmaceutical cocrystals: an overview.

              Pharmaceutical cocrystals are emerging as a new class of solid drugs with improved physicochemical properties, which has attracted increased interests from both industrial and academic researchers. In this paper a brief and systematic overview of pharmaceutical cocrystals is provided, with particular focus on cocrystal design strategies, formation methods, physicochemical property studies, characterisation techniques, and recent theoretical developments in cocrystal screening and mechanisms of cocrystal formations. Examples of pharmaceutical cocrystals are also summarised in this paper. Copyright © 2011 Elsevier B.V. All rights reserved.
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                Author and article information

                Journal
                Journal of Crystal Growth
                Journal of Crystal Growth
                Elsevier BV
                00220248
                January 2016
                January 2016
                : 433
                :
                : 128-138
                Article
                10.1016/j.jcrysgro.2015.10.015
                5d8162a2-f6b7-4994-9c20-5c63fd3276cb
                © 2016
                History

                Organic & Biomolecular chemistry,Chemistry,Pharmaceutical chemistry,Physical chemistry,Analytical chemistry
                urea,cocrystal screening,crystallites,carboxylic acids,surfaces

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