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Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol

Journal 2023 · IF 4.6 · 28(2): 737 · 发表于 2023 年 1 月 11 日
作者: Wenling Fan,Jiali Wu,Meiqi Gao,Xiaotong Zhang,Wenjing Zhu
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摘要

The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion inPolygonum cuspidatumextract (PCE) by hot melt extrusion (HME). In addition, the role of the auxiliary substances in PCE was also studied. The solid dispersion ofPolygonum cuspidatumextract was prepared by hot-melt extrusion. The optimum formula was selected by single factor design and orthogonal test. The optimum formula was barrel temperature 140 °C, screw rotation speed 40 rpm/min, and the ratio ofPolygonum cuspidatumextract to HPMCAS was 1:2. The dissolution test showed that PCE-SD increased the dissolution of RES from 46.75 ± 0.47% to 130.06 ± 0.12%. The pharmacokinetics curve of rats showed that PCE-SD increased AUC0-t of RES from 111,471.22 ± 11.4% to 160,458.968 ± 15.7%, indicating an approximately 1.44-fold increase in absorption. In addition, the rotation speed of PCE-SD screw is less than that of RES-SD screw. The bioavailability of PCE-SD was slightly better than that of RES-SD. PCE-SD is more hygroscopic than RES-SD. PCE-SD increased the solubility and oral bioavailability of RES. The auxiliary substances in Polygonum cuspidatum extract have influence on its preparation technology, stability, and bioavailability.Keywords:resveratrol;polygonum cuspidatum extract;hot-melt extrusion;solid dispersion;attendant substances

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