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Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects

Oral solid formulations based on Angelica gigas Nakai (AGN) and Soluplus were prepared by the hot-melting extrusion (HME) method. AGN was pulverized into coarse and ultrafine particles, and their particle size and morphology were investigated. Ultrafine AGN particles were used in the HME process wit...

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Autores principales: Piao, Jingpei, Lee, Jae-Young, Weon, Jin Bae, Ma, Choong Je, Ko, Hyun-Jeong, Kim, Dae-Duk, Kang, Wie-Soo, Cho, Hyun-Jong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4411051/
https://www.ncbi.nlm.nih.gov/pubmed/25915423
http://dx.doi.org/10.1371/journal.pone.0124447
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author Piao, Jingpei
Lee, Jae-Young
Weon, Jin Bae
Ma, Choong Je
Ko, Hyun-Jeong
Kim, Dae-Duk
Kang, Wie-Soo
Cho, Hyun-Jong
author_facet Piao, Jingpei
Lee, Jae-Young
Weon, Jin Bae
Ma, Choong Je
Ko, Hyun-Jeong
Kim, Dae-Duk
Kang, Wie-Soo
Cho, Hyun-Jong
author_sort Piao, Jingpei
collection PubMed
description Oral solid formulations based on Angelica gigas Nakai (AGN) and Soluplus were prepared by the hot-melting extrusion (HME) method. AGN was pulverized into coarse and ultrafine particles, and their particle size and morphology were investigated. Ultrafine AGN particles were used in the HME process with high shear to produce AGN-based formulations. In simulated gastrointestinal fluids (pH 1.2 and pH 6.8) and water, significantly higher amounts of the major active components of AGN, decursin (D) and decursinol angelate (DA), were extracted from the HME-processed AGN/Soluplus (F8) group than the AGN EtOH extract (ext) group (p < 0.05). Based on an in vivo pharmacokinetic study in rats, the relative oral bioavailability of decursinol (DOH), a hepatic metabolite of D and DA, in F8-administered mice was 8.75-fold higher than in AGN EtOH ext-treated group. In scopolamine-induced memory-impaired mice, F8 exhibited a more potent cognitive enhancing effect than AGN EtOH ext in both a Morris water maze test and a passive avoidance test. These findings suggest that HME-processed AGN/Soluplus formulation (F8) could be a promising therapeutic candidate for memory impairment.
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spelling pubmed-44110512015-05-07 Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects Piao, Jingpei Lee, Jae-Young Weon, Jin Bae Ma, Choong Je Ko, Hyun-Jeong Kim, Dae-Duk Kang, Wie-Soo Cho, Hyun-Jong PLoS One Research Article Oral solid formulations based on Angelica gigas Nakai (AGN) and Soluplus were prepared by the hot-melting extrusion (HME) method. AGN was pulverized into coarse and ultrafine particles, and their particle size and morphology were investigated. Ultrafine AGN particles were used in the HME process with high shear to produce AGN-based formulations. In simulated gastrointestinal fluids (pH 1.2 and pH 6.8) and water, significantly higher amounts of the major active components of AGN, decursin (D) and decursinol angelate (DA), were extracted from the HME-processed AGN/Soluplus (F8) group than the AGN EtOH extract (ext) group (p < 0.05). Based on an in vivo pharmacokinetic study in rats, the relative oral bioavailability of decursinol (DOH), a hepatic metabolite of D and DA, in F8-administered mice was 8.75-fold higher than in AGN EtOH ext-treated group. In scopolamine-induced memory-impaired mice, F8 exhibited a more potent cognitive enhancing effect than AGN EtOH ext in both a Morris water maze test and a passive avoidance test. These findings suggest that HME-processed AGN/Soluplus formulation (F8) could be a promising therapeutic candidate for memory impairment. Public Library of Science 2015-04-27 /pmc/articles/PMC4411051/ /pubmed/25915423 http://dx.doi.org/10.1371/journal.pone.0124447 Text en © 2015 Piao et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Piao, Jingpei
Lee, Jae-Young
Weon, Jin Bae
Ma, Choong Je
Ko, Hyun-Jeong
Kim, Dae-Duk
Kang, Wie-Soo
Cho, Hyun-Jong
Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects
title Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects
title_full Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects
title_fullStr Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects
title_full_unstemmed Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects
title_short Angelica gigas Nakai and Soluplus-Based Solid Formulations Prepared by Hot-Melting Extrusion: Oral Absorption Enhancing and Memory Ameliorating Effects
title_sort angelica gigas nakai and soluplus-based solid formulations prepared by hot-melting extrusion: oral absorption enhancing and memory ameliorating effects
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4411051/
https://www.ncbi.nlm.nih.gov/pubmed/25915423
http://dx.doi.org/10.1371/journal.pone.0124447
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