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Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF
[Image: see text] This study focused on improving the physicochemical characteristics of aprepitant with poor water solubility by preparing solid dispersion (SD). To prepare the SD with HPMCAS-LF, the solvent evaporation method was applied. Based on dissolution analysis, the dissolution rate of SD i...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9647728/ https://www.ncbi.nlm.nih.gov/pubmed/36385804 http://dx.doi.org/10.1021/acsomega.2c04021 |
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author | Liu, Jinwen Li, Yongji Ao, Wuliji Xiao, Yingge Bai, Meirong Li, Shuyan |
author_facet | Liu, Jinwen Li, Yongji Ao, Wuliji Xiao, Yingge Bai, Meirong Li, Shuyan |
author_sort | Liu, Jinwen |
collection | PubMed |
description | [Image: see text] This study focused on improving the physicochemical characteristics of aprepitant with poor water solubility by preparing solid dispersion (SD). To prepare the SD with HPMCAS-LF, the solvent evaporation method was applied. Based on dissolution analysis, the dissolution rate of SD increased by five times compared with aprepitant. In addition, scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC) results suggested the presence of amorphous-form aprepitant inside SD. According to Fourier transform infrared (FTIR) spectroscopy, intermolecular hydrogen bonds were detected between polymer and aprepitant. The Caco-2 cell experiment proved that SD did not lower the transepithelial electrical resistance (TEER) values but improved the permeation amount of aprepitant. Additionally, the SD of aprepitant displayed excellent stability. |
format | Online Article Text |
id | pubmed-9647728 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-96477282022-11-15 Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF Liu, Jinwen Li, Yongji Ao, Wuliji Xiao, Yingge Bai, Meirong Li, Shuyan ACS Omega [Image: see text] This study focused on improving the physicochemical characteristics of aprepitant with poor water solubility by preparing solid dispersion (SD). To prepare the SD with HPMCAS-LF, the solvent evaporation method was applied. Based on dissolution analysis, the dissolution rate of SD increased by five times compared with aprepitant. In addition, scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC) results suggested the presence of amorphous-form aprepitant inside SD. According to Fourier transform infrared (FTIR) spectroscopy, intermolecular hydrogen bonds were detected between polymer and aprepitant. The Caco-2 cell experiment proved that SD did not lower the transepithelial electrical resistance (TEER) values but improved the permeation amount of aprepitant. Additionally, the SD of aprepitant displayed excellent stability. American Chemical Society 2022-10-24 /pmc/articles/PMC9647728/ /pubmed/36385804 http://dx.doi.org/10.1021/acsomega.2c04021 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Liu, Jinwen Li, Yongji Ao, Wuliji Xiao, Yingge Bai, Meirong Li, Shuyan Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF |
title | Preparation and Characterization of Aprepitant Solid
Dispersion with HPMCAS-LF |
title_full | Preparation and Characterization of Aprepitant Solid
Dispersion with HPMCAS-LF |
title_fullStr | Preparation and Characterization of Aprepitant Solid
Dispersion with HPMCAS-LF |
title_full_unstemmed | Preparation and Characterization of Aprepitant Solid
Dispersion with HPMCAS-LF |
title_short | Preparation and Characterization of Aprepitant Solid
Dispersion with HPMCAS-LF |
title_sort | preparation and characterization of aprepitant solid
dispersion with hpmcas-lf |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9647728/ https://www.ncbi.nlm.nih.gov/pubmed/36385804 http://dx.doi.org/10.1021/acsomega.2c04021 |
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