<p>Non-covalent interactions (NCIs), such as hydrogen bonding and π-π stacking, play a pivotal role in modulating the physicochemical properties of drug molecules through non-covalent derivatives (NCDs), including co-crystals and eutectics. This review highlights the advances in the design and development of non-covalent derivatives (NCDs) for antipsychotic drugs such as aripiprazole, olanzapine, risperidone, and others, which often suffer from poor aqueous solubility and low oral bioavailability. A range of pharmaceutically acceptable coformers, along with various preparation techniques, have been employed for the development of multicomponent systems. Their formation, structural integrity, and stability are typically confirmed through comprehensive characterization methods, including thermal analysis, spectroscopy, powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), and single-crystal X-ray diffraction (SCXRD). The improved solubility and dissolution rates in these NCDs can enhance absorption and bioavailability, which are critical for achieving optimal therapeutic efficacy. Therefore, these non-covalent strategies hold significant promise in improving drug performance and clinical outcomes in the treatment of psychotic disorders.</p>

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Crystal structural insights into non-covalent derivatives of antipsychotic drugs with improved performance: a comprehensive overview

  • Shweta Kamboj,
  • Saara,
  • Dimpy Rani

摘要

Non-covalent interactions (NCIs), such as hydrogen bonding and π-π stacking, play a pivotal role in modulating the physicochemical properties of drug molecules through non-covalent derivatives (NCDs), including co-crystals and eutectics. This review highlights the advances in the design and development of non-covalent derivatives (NCDs) for antipsychotic drugs such as aripiprazole, olanzapine, risperidone, and others, which often suffer from poor aqueous solubility and low oral bioavailability. A range of pharmaceutically acceptable coformers, along with various preparation techniques, have been employed for the development of multicomponent systems. Their formation, structural integrity, and stability are typically confirmed through comprehensive characterization methods, including thermal analysis, spectroscopy, powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), and single-crystal X-ray diffraction (SCXRD). The improved solubility and dissolution rates in these NCDs can enhance absorption and bioavailability, which are critical for achieving optimal therapeutic efficacy. Therefore, these non-covalent strategies hold significant promise in improving drug performance and clinical outcomes in the treatment of psychotic disorders.