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Conformational polymorphic changes in the crystal structure of the chiral antiparasitic drug praziquantel and interactions with calcium carbonate.
Borrego-Sánchez, Ana; Carazo, Esperanza; Albertini, Beatrice; Passerini, Nadia; Perissutti, Beatrice; Cerezo, Pilar; Viseras, César; Hernández-Laguna, A; Aguzzi, Carola; Sainz-Díaz, C Ignacio.
Afiliación
  • Borrego-Sánchez A; Instituto Andaluz de Ciencias de la Tierra (CSIC-University of Granada), Av. de las Palmeras 4, 18100 Armilla, Granada, Spain; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
  • Carazo E; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
  • Albertini B; Department of Pharmacy and BioTechnology, University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy.
  • Passerini N; Department of Pharmacy and BioTechnology, University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy.
  • Perissutti B; Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy.
  • Cerezo P; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
  • Viseras C; Instituto Andaluz de Ciencias de la Tierra (CSIC-University of Granada), Av. de las Palmeras 4, 18100 Armilla, Granada, Spain; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
  • Hernández-Laguna A; Instituto Andaluz de Ciencias de la Tierra (CSIC-University of Granada), Av. de las Palmeras 4, 18100 Armilla, Granada, Spain.
  • Aguzzi C; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain. Electronic address: carola@ugr.es.
  • Sainz-Díaz CI; Instituto Andaluz de Ciencias de la Tierra (CSIC-University of Granada), Av. de las Palmeras 4, 18100 Armilla, Granada, Spain.
Eur J Pharm Biopharm ; 132: 180-191, 2018 Nov.
Article en En | MEDLINE | ID: mdl-30267834
Praziquantel is an antiparasitic drug used for decades. Currently, the praziquantel commercial preparation is a racemic mixture, in which only the levo-enantiomer possesses anthelmintic activity. The knowledge of its properties in the solid state and other chemical-physical properties is necessary for improving its efficacy and applications. Drug solid dispersions were prepared with calcium carbonate at 1:5 drug to excipient weight ratio by solvent evaporation method. Then, the modification of the crystal structure of the racemic polymorph of praziquantel in presence of calcium carbonate has been studied by means of several analytical techniques (DSC, TGA, XRD, SEM, FTIR, Raman spectroscopy and chiral liquid chromatography). This study has been completed with atomistic calculations based on empirical interatomic force fields and quantum mechanics methods applied to the crystal structure of praziquantel and of intermolecular interactions. The results evidenced that calcium carbonate provoked a conformational change in the praziquantel molecule yielding the formation of different polymorphs of praziquantel crystal. These alterations were not observed replacing calcium carbonate with colloidal silica as excipient in the solid dispersion.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Praziquantel / Carbonato de Calcio / Excipientes / Antihelmínticos Idioma: En Revista: Eur J Pharm Biopharm Asunto de la revista: FARMACIA / FARMACOLOGIA Año: 2018 Tipo del documento: Article País de afiliación: España Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Praziquantel / Carbonato de Calcio / Excipientes / Antihelmínticos Idioma: En Revista: Eur J Pharm Biopharm Asunto de la revista: FARMACIA / FARMACOLOGIA Año: 2018 Tipo del documento: Article País de afiliación: España Pais de publicación: Países Bajos