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采用热熔挤出法制备虎杖提取物固体分散体以提高白藜芦醇的口服生物利用度。

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

机构信息

College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.

Jiangsu Provincial Technology Engineering Research Center of TCM Health Preservation, Nanjing 210023, China.

出版信息

Molecules. 2023 Jan 11;28(2):737. doi: 10.3390/molecules28020737.

Abstract

The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in extract (PCE) by hot melt extrusion (HME). In addition, the role of the auxiliary substances in PCE was also studied. The solid dispersion of extract 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 of extract 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.

摘要

本研究旨在通过热熔挤出(HME)提高白藜芦醇(RES-SD)固体分散体在虎杖提取物(PCE)中的溶解度、生物利用度和稳定性。此外,还研究了 PCE 中辅助物质的作用。采用热熔挤出法制备虎杖提取物的固体分散体。通过单因素设计和正交试验选择最佳配方。最佳配方为:机筒温度 140°C,螺杆转速 40rpm/min,PCE 与 HPMCAS 的比例为 1:2。溶出度试验表明,PCE-SD 使 RES 的溶出度从 46.75±0.47%提高到 130.06±0.12%。大鼠药代动力学曲线表明,PCE-SD 使 RES 的 AUC0-t 从 111,471.22±11.4%增加到 160,458.968±15.7%,表明吸收增加了约 1.44 倍。此外,PCE-SD 螺杆的转速小于 RES-SD 螺杆的转速。PCE-SD 的生物利用度略优于 RES-SD。PCE-SD 比 RES-SD 更吸湿。PCE-SD 提高了 RES 的溶解度和口服生物利用度。虎杖提取物中的辅助物质对其制备技术、稳定性和生物利用度有影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ba8/9865168/a71191737c6c/molecules-28-00737-g001.jpg

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