Formulation optimization of solid dispersion of candesartan cilexetil

Abstract

Context: Antihypertensive effects were achieved by quickly hydrolyzing candesartan cilexetil (CC), an inactive prodrug of candesartan, into active candesartan during absorption in the gastrointestinal tract. Due to its weak water solubility, CC has an inadequate intestinal absorption and a low oral bioavailability. Aim: The goal of this study was to make the medication CC more soluble in water. Materials and Methods: Low viscosity hydroxypropyl methylcellulose (HPMC) E5LV was used to prepare the solid dispersions through spray drying. Results: Study of dissolution, Fourier transform infrared spectroscopy, scanning electron microscopy (SEM), differential scanning calorimeter (DSC), and X-ray diffraction characterized the prepared solid dispersions. CC amorphized from its crystallized state, as shown by the findings from the SEM, DSC, and X-ray powder diffraction experiments. Comparing pure CC and solid dispersion, the dissolution rate was higher with the former. The surfactant and wetting property of HPMC E5LV slowed devitrification and had an anti-plasticization impact, increasing the solubility and stability of the solid dispersion. Conclusion: The final results indicated that the CC, a weakly water-soluble medication, dissolved much better in the solid dispersions.