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New cocrystals of bexarotene with pyridinecarboxamide isomers sustained by the acid∙∙∙aromatic nitrogen supramolecular heterosynthon

  • Pharmaceutical cocrystals are homogenous crystalline structures made up of two or more components in a definite stoichiometric ratio, where at least one of the components in the crystal lattice is an active pharmaceutical ingredient (API).1 Pharmaceutical cocrystals have opened the opportunity for engineering solid-state forms designed to have tailored properties to enhance drug product bioavailability and stability, as well a enhance processability of the solid material inputs in drug product manufacture. In this work the cocrystallization of bexarotene, an approved API by the U.S. Food and Drug Administration that belongs to Biopharmaceutics Classification System Class II (low solubility–high permeability), with pyridine carboxamide isomers (picolinamide, nicotinamide and isonicotinamide) was successfully undertaken. The synthesis was achieved by liquid assisted grinding (LAG) and the solids obtained were characterized by differential scanning calorimetry (DSC), infrared spectroscopyPharmaceutical cocrystals are homogenous crystalline structures made up of two or more components in a definite stoichiometric ratio, where at least one of the components in the crystal lattice is an active pharmaceutical ingredient (API).1 Pharmaceutical cocrystals have opened the opportunity for engineering solid-state forms designed to have tailored properties to enhance drug product bioavailability and stability, as well a enhance processability of the solid material inputs in drug product manufacture. In this work the cocrystallization of bexarotene, an approved API by the U.S. Food and Drug Administration that belongs to Biopharmaceutics Classification System Class II (low solubility–high permeability), with pyridine carboxamide isomers (picolinamide, nicotinamide and isonicotinamide) was successfully undertaken. The synthesis was achieved by liquid assisted grinding (LAG) and the solids obtained were characterized by differential scanning calorimetry (DSC), infrared spectroscopy (FTIR-ATR), powder X-ray diffraction (XRPD), single crystal X-ray diffraction (SXD), and polarized light thermomicroscopy (PLTM). For bexarotene: picolinamide and bexarotene:isonicotinamide, 1:1 cocrystals were obtained directly from milling. SXD data of bexarotene:isonicotinamide cocrystal reveal acid∙∙∙aromatic nitrogen supramolecular heterosynthon and that the homosynthon amide∙∙∙amide in isonicotinamide is preserved. The bexarotene:nicotinamide mixtures prepared by ball milling give rise to simple binary solid–liquid phase diagram with an eutectic point, well described by the Schröder-van Laar equation. Melt crystallization of the 1:1 mixture gives rise to a cocrystal for which a complex phase behaviour is observed.zeige mehrzeige weniger

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Metadaten
Autor*innen:R. A. E. Castro
Koautor*innen:A. M. Cortesao, T. M. R. Maria, M. R. Silva, Franziska Emmerling, J. Canotilho, M. E. S. Eusebio
Dokumenttyp:Posterpräsentation
Veröffentlichungsform:Präsentation
Sprache:Englisch
Jahr der Erstveröffentlichung:2017
DDC-Klassifikation:Technik, Medizin, angewandte Wissenschaften / Ingenieurwissenschaften / Ingenieurwissenschaften und zugeordnete Tätigkeiten
Freie Schlagwörter:Bexarotene; Crystalline structure; Infrared spectroscopy; Powder X-ray diffraction; Single crystal X-ray diffraction
Veranstaltung:6th Meeting IAPC
Veranstaltungsort:Zagreb, Croatia
Beginndatum der Veranstaltung:04.09.2017
Enddatum der Veranstaltung:06.09.2017
Verfügbarkeit des Dokuments:Datei im Netzwerk der BAM verfügbar ("Closed Access")
Datum der Freischaltung:31.08.2017
Referierte Publikation:Nein
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