Abstract <p>Celecoxib (CXB) is a non-steroidal anti-inflammatory drug, but its low aqueous solubility and bioavailability limit its clinical application. This study employed ternary solid dispersion technology (using PVP K30/sodium cholate as carriers) combined with rotary evaporation to prepare CXB solid dispersions for enhancing dissolution performance. Results demonstrated that the addition of PVP K30 and sodium cholate significantly improved the solubility of CXB, with the drug-polymer-surfactant ratio of 1 : 1 : 1.13 exhibiting maximum solubility and dissolution rate. The novel ternary solid dispersion achieved approximately 4.63-fold enhancement in solubility and 14.48-fold acceleration in dissolution rate (within 120 min). X-Ray powder diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) analyses confirmed the amorphous state dispersion of CXB and hydrogen bonding interactions with carriers. differential scanning calorimetry (DSC) revealed an elevated glass transition temperature (<i>T</i><sub>g</sub>), indicating enhanced system stability. Contact angle experiments demonstrated significantly improved drug wettability by the carriers. In addition, after being stored at room temperature for three months, the stability of the CXB ternary solid dispersion is relatively good. This research provides a novel strategy for developing high-efficiency CXB formulations.</p>

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Design of Ternary Solid Dispersions of Celecoxib to Improve Solubility and Stability Properties

  • Liqing Zhu,
  • Yimei Wang,
  • Lang Liu,
  • Yuan Wei,
  • Minghao De,
  • Hengli Yu,
  • Jianghai Li,
  • Xue Fu

摘要

Abstract

Celecoxib (CXB) is a non-steroidal anti-inflammatory drug, but its low aqueous solubility and bioavailability limit its clinical application. This study employed ternary solid dispersion technology (using PVP K30/sodium cholate as carriers) combined with rotary evaporation to prepare CXB solid dispersions for enhancing dissolution performance. Results demonstrated that the addition of PVP K30 and sodium cholate significantly improved the solubility of CXB, with the drug-polymer-surfactant ratio of 1 : 1 : 1.13 exhibiting maximum solubility and dissolution rate. The novel ternary solid dispersion achieved approximately 4.63-fold enhancement in solubility and 14.48-fold acceleration in dissolution rate (within 120 min). X-Ray powder diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) analyses confirmed the amorphous state dispersion of CXB and hydrogen bonding interactions with carriers. differential scanning calorimetry (DSC) revealed an elevated glass transition temperature (Tg), indicating enhanced system stability. Contact angle experiments demonstrated significantly improved drug wettability by the carriers. In addition, after being stored at room temperature for three months, the stability of the CXB ternary solid dispersion is relatively good. This research provides a novel strategy for developing high-efficiency CXB formulations.