Purpose <p>Cocrystals of Carvedilol (CAV) were developed using nicotinamide (NTA) as a co-former to study their effect on crystalline properties and dissolution behavior.</p> Method <p>Cocrystals of CAV-NTA in a 1:1 molar ratio was prepared using the Ultrasound Assisted Solution Crystallization (USSC) technique. The prepared cocrystals were characterized by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), and Powder X-ray Diffraction (P-XRD). Morphological analysis was performed using Scanning Electron Microscopy (SEM) to confirm cocrystal formation. Further, saturation solubility and in-vitro dissolution studies were conducted to compare the solubility profile of CAV-NTA cocrystals with that of pure CAV.</p> Result <p>SEM analysis of CAV and CAV–NTA cocrystals were used to compare crystal habit and surface morphology. Pure CAV showed irregular, non-uniform crystals with a rough surface. In contrast, CAV–NTA cocrystals exhibited regular, needle to spherical shaped but comparatively smoother surface crystal morphology, indicating successful cocrystal formation. The prepared cocrystals exhibited a 10.13-fold increase in solubility compared to pure CAV.</p> Conclusion <p>The study concludes that the Ultrasound Assisted Solution Crystallization (USSC) technique is an effective approach to enhance the solubility of poorly water-soluble BCS Class-II drugs like Carvedilol.</p>

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Exploring Ultrasound-Assisted Solvent Co-crystallization (USSC) Technique to Enhance Solubility of Carvedilol

  • Meenaxi Maste,
  • Krantisinha Randive,
  • Amolkumar Kempwade,
  • Anagha Patil

摘要

Purpose

Cocrystals of Carvedilol (CAV) were developed using nicotinamide (NTA) as a co-former to study their effect on crystalline properties and dissolution behavior.

Method

Cocrystals of CAV-NTA in a 1:1 molar ratio was prepared using the Ultrasound Assisted Solution Crystallization (USSC) technique. The prepared cocrystals were characterized by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), and Powder X-ray Diffraction (P-XRD). Morphological analysis was performed using Scanning Electron Microscopy (SEM) to confirm cocrystal formation. Further, saturation solubility and in-vitro dissolution studies were conducted to compare the solubility profile of CAV-NTA cocrystals with that of pure CAV.

Result

SEM analysis of CAV and CAV–NTA cocrystals were used to compare crystal habit and surface morphology. Pure CAV showed irregular, non-uniform crystals with a rough surface. In contrast, CAV–NTA cocrystals exhibited regular, needle to spherical shaped but comparatively smoother surface crystal morphology, indicating successful cocrystal formation. The prepared cocrystals exhibited a 10.13-fold increase in solubility compared to pure CAV.

Conclusion

The study concludes that the Ultrasound Assisted Solution Crystallization (USSC) technique is an effective approach to enhance the solubility of poorly water-soluble BCS Class-II drugs like Carvedilol.