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Area of Science:

  • Pharmaceutical Science
  • Drug Discovery
  • Materials Science

Background:

  • Poor aqueous solubility of new chemical entities presents a major hurdle in drug discovery, necessitating high exposures for essential studies.
  • Pharmaceutical cocrystals offer a promising approach to enhance physicochemical properties and in vivo performance of poorly soluble drugs.
  • Physical instability of cocrystals in supersaturated formulations is a significant concern for their application in preclinical research.

Purpose of the Study:

  • To review the thermodynamic and kinetic factors influencing the physical stability of cocrystals in preclinical formulations.
  • To examine the impact of surfactants, polymeric excipients, and pH on cocrystal stability.
  • To discuss the in vivo performance of cocrystals and propose strategies for developing stable preclinical formulations.

Main Methods:

  • Literature review focusing on thermodynamic and kinetic contributions to cocrystal physical stability.
  • Analysis of the role of excipients (surfactants, polymers) and pH in formulation stability.
  • Discussion of in vivo performance data and formulation strategies.

Main Results:

  • Physical instability, particularly in supersaturated states, remains a key challenge for cocrystal formulations in preclinical studies.
  • Surfactants, polymeric excipients, and pH significantly influence the thermodynamic and kinetic stability of cocrystals.
  • Strategies for developing physically stable cocrystal formulations are crucial for successful preclinical evaluation.

Conclusions:

  • Addressing the physical instability of pharmaceutical cocrystals is critical for their effective use in drug discovery.
  • Careful selection of excipients and control of formulation parameters like pH are essential for enhancing cocrystal stability.
  • Further research into stable cocrystal formulations will facilitate their translation into preclinical and clinical applications.