Liqing Zhu, Yimei Wang, Lang Liu, Yuan Wei, Minghao De, Hengli Yu, Jianghai Li, Xue Fu
{"title":"Design of Ternary Solid Dispersions of Celecoxib to Improve Solubility and Stability Properties","authors":"Liqing Zhu, Yimei Wang, Lang Liu, Yuan Wei, Minghao De, Hengli Yu, Jianghai Li, Xue Fu","doi":"10.1134/S1070363225601644","DOIUrl":null,"url":null,"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>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 9","pages":"2445 - 2456"},"PeriodicalIF":0.8000,"publicationDate":"2025-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of General Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1070363225601644","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
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.
期刊介绍:
Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.