The Preparation of Curcumin Sustained-Release Solid Dispersion by Hot Melt Extrusion—Ⅰ. Optimization of the Formulation

• Published in: Journal of pharmaceutical sciences Vol. 109; no. 3; pp. 1242 - 1252
• Main Authors: Fan, Wenling, Zhu, Wenjing, Zhang, Xinyi, Di, Liuqing
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.03.2020
• Subjects: curcumin; dissolution; hot-melt extrusion; solid dispersion; sustained-release; hot-melt extrusion; solid dispersion; dissolution; sustained-release; curcumin
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1016/j.xphs.2019.11.019

The purpose of this study was to optimize the formulation for developing curcumin sustained-release solid dispersion to increase the solubility of curcumin, delay drug release by hot-melt extrusion, and to explore the possibility of hot-melt extrusion for one-step preparation of insoluble drug sustained-release solid dispersion. The miscibility of curcumin and Eudragit RSPO and Eudragit RLPO were assessed by solubility parameter and melting point depression. Orthogonal test was used to optimize the formulation, based on the results of single-factor experiment, and the final optimal formulation: the ratio of the sustained-release carrier material RS/RL was 1:3, the ratio of drug and carrier was 1:6, and the porogen was used in an amount of 40% of the sustained-release carrier material. The curcumin solid dispersion of the best formulation had been prepared and had a significant sustained-release effect compared to the curcumin and the physical mixture.