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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...

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Autores principales: Liu, Jinwen, Li, Yongji, Ao, Wuliji, Xiao, Yingge, Bai, Meirong, Li, Shuyan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
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.
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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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