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Preparation, characterization and dissolution studies of pharmaceutical co-crystals containing indomethacin

By A. Dalpiaz, V. Bertolasi and V. Ferretti


Purpose: To change the dissolution properties of indomethacin, a non-steroidal anti-inflammatory drug characterized by weak solubility and bioavailability, we propose the preparation of co-crystals where the active pharmaceutical ingredient is indomethacin and the partners are aromatic nitrogen bases (+ 2-hydroxy-4-methyl-pyridine or 2-methoxy-5-nitro-anyline) or saccharine. In co-crystals different molecules are linked in the same crystalline lattice by intermolecular interactions, so can be defined supramolecular complexes.\ud Methods: The packing of structures have been determined with the employment of a X-ray Nonius Kappa CCD diffractometer and have been analyzed from the point of view of intermolecular interactions. The dissolution studies have been performed by incubation of free or co-crystalized indomethacin in phosphate buffer whose concentrations have been analyzed by HPLC during time.\ud Results: The carboxylic group usually forms COOH...HOOC homosyntons to give dimers, using other functional groups to interact via H bond with the partners. In all co-crystals indomethacin has showed significantly different solubility and dissolution rates with respect to those of the free drug. The simple mix of indomethacin and partners without co-crystallization processes showed for indomethacin the same solubility and dissolution rate of the pure drug. \ud Conclusions: The co-crystallization with appropriate partners can induce important changes in solubility and dissolution rates of indomethacin allowing to hypothesize interesting influences in the bioavailability or local delivery of the drug

Topics: Cocrytals, solulity, DISSOLUTION RATE, Indomethacin
Publisher: Associazione Docenti e Ricercatori Italiani di Tecnologie e Legislazioni Farmaceutiche
Year: 2013
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