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

IF 0.8 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
Liqing Zhu, Yimei Wang, Lang Liu, Yuan Wei, Minghao De, Hengli Yu, Jianghai Li, Xue Fu
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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.

Abstract Image

塞来昔布三元固体分散体的设计以改善其溶解度和稳定性
塞来昔布(CXB)是一种非甾体抗炎药,但其低水溶性和生物利用度限制了其临床应用。本研究采用三元固体分散技术(以PVP K30/胆酸钠为载体)结合旋转蒸发法制备CXB固体分散体,以提高溶解性能。结果表明,PVP K30和胆酸钠的加入显著提高了CXB的溶解度,药物-聚合物-表面活性剂比为1:1:1.13时,CXB的溶解度和溶出率最高。新型三元固体分散体的溶解度提高了约4.63倍,溶解速度加快了14.48倍(在120分钟内)。x射线粉末衍射(XRD)和傅里叶变换红外光谱(FT-IR)分析证实了CXB的非晶态色散和与载流子的氢键相互作用。差示扫描量热法(DSC)显示玻璃化转变温度(Tg)升高,表明系统稳定性增强。接触角实验表明,载体明显改善了药物的润湿性。此外,在室温下保存三个月后,CXB三元固体分散体的稳定性相对较好。本研究为开发高效的CXB配方提供了一种新的策略。
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来源期刊
CiteScore
1.40
自引率
22.20%
发文量
252
审稿时长
2-4 weeks
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.
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