Indomethacin co-crystals and their parent mixtures: does the intestinal barrier recognize them differently?

Molecular Pharmaceutics
Valeria FerrettiBarbara Pavan

Abstract

Co-crystals are crystalline complexes of two or more molecules bound together in crystal lattices through noncovalent interactions. The solubility and dissolution properties of co-crystals can allow to increase the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). It is currently believed that the co-crystallization strategy should not induce changes on the pharmacological profile of the APIs, even if it is not yet clear whether a co-crystal would be defined as a physical mixture or as a new chemical entity. In order to clarify these aspects, we chose indomethacin as guest poorly aqueous soluble molecule and compared its properties with those of its co-crystals obtained with 2-hydroxy-4-methylpyridine (co-crystal 1), 2-methoxy-5-nitroaniline (co-crystal 2), and saccharine (co-crystal 3). In particular, we performed a systematic comparison among indomethacin, its co-crystals, and their parent physical mixtures by evaluating via HPLC analysis the API dissolution profile, its ability to permeate across intestinal cell monolayers (NCM460), and its oral bioavailability in rat. The indomethacin dissolution profile was not altered by the presence of co-crystallizing agents as physical mixtures, whereas ...Continue Reading

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Citations

Jun 6, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Paolo MarchettiAlessandro Dalpiaz
Jun 21, 2016·Chemical & Pharmaceutical Bulletin·Ken-Ichi IzutsuEtsuo Yonemochi
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Dec 29, 2019·Pharmaceutics·Reynaldo Salas-ZúñigaDea Herrera-Ruiz
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Dec 8, 2020·Expert Opinion on Drug Delivery·Yingxi ZhangHongzhuo Liu
Jul 25, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ilma Nugrahani, Rismaya Desti Parwati

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