Objective <p>This review focuses on the crystallization and cocrystallization of BCS Class II drug indomethacin (IMC), a common nonsteroidal anti-inflammatory drug (NSAID). In particular, it highlights the liquid antisolvent method as a viable strategy for creating IMC cocrystals with improved characteristics.</p> Significance of review <p>Indomethacin has a low bioavailability and poor water solubility, despite its therapeutic effectiveness. Cocrystallization has been a prominent approach to overcome these challenges. The liquid antisolvent method is thoroughly reviewed in this review, along with the physicochemical properties of indomethacin, together with other co-crystallization strategies to improve the physicochemical performance of IMC in pharmaceutical formulations.</p> Key findings <p>The review emphasizes that, in comparison to raw IMC, the crystals prepared by&#xa0;liquid antisolvent approach is a useful for enhancing IMC's crystal habit, solubility, dissolving rate, and bioavailability. Various solid forms, polymorphs, and cocrystal structures created throughout the process are also examined.</p> Conclusion <p>This review emphasizes the importance of cocrystallization and solid-form engineering, particularly the antisolvent approach, in enhancing the physicochemical properties. Solvents and coformers play a critical function. Integrating advanced characterization tools allows for optimizing formulations that helps poorly soluble medications get closer to improved bioavailability, clinical efficacy, and possible industrial use.</p>

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Indomethacin cocrystals: a critical review of antisolvent-mediated strategies

  • Soham M. Deshmukh,
  • Manishkumar D. Yadav

摘要

Objective

This review focuses on the crystallization and cocrystallization of BCS Class II drug indomethacin (IMC), a common nonsteroidal anti-inflammatory drug (NSAID). In particular, it highlights the liquid antisolvent method as a viable strategy for creating IMC cocrystals with improved characteristics.

Significance of review

Indomethacin has a low bioavailability and poor water solubility, despite its therapeutic effectiveness. Cocrystallization has been a prominent approach to overcome these challenges. The liquid antisolvent method is thoroughly reviewed in this review, along with the physicochemical properties of indomethacin, together with other co-crystallization strategies to improve the physicochemical performance of IMC in pharmaceutical formulations.

Key findings

The review emphasizes that, in comparison to raw IMC, the crystals prepared by liquid antisolvent approach is a useful for enhancing IMC's crystal habit, solubility, dissolving rate, and bioavailability. Various solid forms, polymorphs, and cocrystal structures created throughout the process are also examined.

Conclusion

This review emphasizes the importance of cocrystallization and solid-form engineering, particularly the antisolvent approach, in enhancing the physicochemical properties. Solvents and coformers play a critical function. Integrating advanced characterization tools allows for optimizing formulations that helps poorly soluble medications get closer to improved bioavailability, clinical efficacy, and possible industrial use.