4.5 Article

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

Journal

JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 109, Issue 3, Pages 1242-1252

Publisher

ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2019.11.019

Keywords

solid dispersion; curcumin; hot-melt extrusion; dissolution; sustained-release

Funding

  1. National Natural Science Foundation of China, China [30801552, 81274095]
  2. Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, China [ZDXM-3-10, 021062001001]
  3. Postgraduate Research & Practice Innovation Program of Jiangsu Province, China [BK20161403]

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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. (C) 2020 Published by Elsevier Inc. on behalf of the American Pharmacists Association.

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