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Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide

This study aims to develop a powder formulation for the Korean red ginseng extract (RGE) and to evaluate its in vitro and in vivo formulation characteristics. The solid dispersion of RGE was prepared with hydrophilic carriers using a freeze-drying method. After conducting the water sorption–desorpti...

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Autores principales: Jin, Sojeong, Lee, Chul Haeng, Lim, Dong Yu, Lee, Jaehyeok, Park, Soo-Jin, Song, Im-Sook, Choi, Min-Koo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8309041/
https://www.ncbi.nlm.nih.gov/pubmed/34371714
http://dx.doi.org/10.3390/pharmaceutics13071022
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author Jin, Sojeong
Lee, Chul Haeng
Lim, Dong Yu
Lee, Jaehyeok
Park, Soo-Jin
Song, Im-Sook
Choi, Min-Koo
author_facet Jin, Sojeong
Lee, Chul Haeng
Lim, Dong Yu
Lee, Jaehyeok
Park, Soo-Jin
Song, Im-Sook
Choi, Min-Koo
author_sort Jin, Sojeong
collection PubMed
description This study aims to develop a powder formulation for the Korean red ginseng extract (RGE) and to evaluate its in vitro and in vivo formulation characteristics. The solid dispersion of RGE was prepared with hydrophilic carriers using a freeze-drying method. After conducting the water sorption–desorption isothermogram (relative humidity between 30 and 70% RH), differential scanning calorimetry thermal behavior, dissolution test, and intestinal permeation study, a solid dispersion formulation of RGE and silicon dioxide (RGE-SiO(2)) was selected. RGE-SiO(2) formulation increased intestinal permeability of ginsenoside Rb1 (GRb1), GRb2, GRc, and GRd by 1.6-fold in rat jejunal segments as measured by the Ussing chamber system. A 1.6- to 1.8-fold increase in plasma exposure of GRb1, GRb2, GRc, and GRd in rats was observed following oral administration of RGE-SiO(2) (375 mg/kg as RGE). No significant difference was observed in the time to reach maximum concentration (T(max)) and half-life in comparison to those in RGE administered rats (375 mg/kg). In conclusion, formulating solid dispersion of RGE with amorphous SiO(2), the powder formulation of RGE was successfully formulated with improved hygroscopicity, increased intestinal permeability, and enhanced oral bioavailability and is therefore suitable for processing solid formulations of RGE product.
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spelling pubmed-83090412021-07-25 Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide Jin, Sojeong Lee, Chul Haeng Lim, Dong Yu Lee, Jaehyeok Park, Soo-Jin Song, Im-Sook Choi, Min-Koo Pharmaceutics Article This study aims to develop a powder formulation for the Korean red ginseng extract (RGE) and to evaluate its in vitro and in vivo formulation characteristics. The solid dispersion of RGE was prepared with hydrophilic carriers using a freeze-drying method. After conducting the water sorption–desorption isothermogram (relative humidity between 30 and 70% RH), differential scanning calorimetry thermal behavior, dissolution test, and intestinal permeation study, a solid dispersion formulation of RGE and silicon dioxide (RGE-SiO(2)) was selected. RGE-SiO(2) formulation increased intestinal permeability of ginsenoside Rb1 (GRb1), GRb2, GRc, and GRd by 1.6-fold in rat jejunal segments as measured by the Ussing chamber system. A 1.6- to 1.8-fold increase in plasma exposure of GRb1, GRb2, GRc, and GRd in rats was observed following oral administration of RGE-SiO(2) (375 mg/kg as RGE). No significant difference was observed in the time to reach maximum concentration (T(max)) and half-life in comparison to those in RGE administered rats (375 mg/kg). In conclusion, formulating solid dispersion of RGE with amorphous SiO(2), the powder formulation of RGE was successfully formulated with improved hygroscopicity, increased intestinal permeability, and enhanced oral bioavailability and is therefore suitable for processing solid formulations of RGE product. MDPI 2021-07-04 /pmc/articles/PMC8309041/ /pubmed/34371714 http://dx.doi.org/10.3390/pharmaceutics13071022 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Jin, Sojeong
Lee, Chul Haeng
Lim, Dong Yu
Lee, Jaehyeok
Park, Soo-Jin
Song, Im-Sook
Choi, Min-Koo
Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide
title Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide
title_full Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide
title_fullStr Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide
title_full_unstemmed Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide
title_short Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide
title_sort improved hygroscopicity and bioavailability of solid dispersion of red ginseng extract with silicon dioxide
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8309041/
https://www.ncbi.nlm.nih.gov/pubmed/34371714
http://dx.doi.org/10.3390/pharmaceutics13071022
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