Exploring Ultrasound-Assisted Solvent Co-crystallization (USSC) Technique to Enhance Solubility of Carvedilol
摘要
Cocrystals of Carvedilol (CAV) were developed using nicotinamide (NTA) as a co-former to study their effect on crystalline properties and dissolution behavior.
MethodCocrystals 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.
ResultSEM 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.
ConclusionThe 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.