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Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability
In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409573/ https://www.ncbi.nlm.nih.gov/pubmed/30717471 http://dx.doi.org/10.3390/pharmaceutics11020067 |
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author | Han, Fei Zhang, Wei Wang, Ying Xi, Ziyue Chen, Lu Li, Sanming Xu, Lu |
author_facet | Han, Fei Zhang, Wei Wang, Ying Xi, Ziyue Chen, Lu Li, Sanming Xu, Lu |
author_sort | Han, Fei |
collection | PubMed |
description | In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The PXRD and DSC results suggested that the amorphous form of IBU was maintained in the solid dispersions. Furthermore, in vitro dissolution and in vivo pharmacokinetic (PK) studies in rats were also performed. The dissolution performance of the SCF-prepared IBU dispersions was significantly improved compared to that of the physical mixtures of crystalline IBU and a polymer. In addition, the PK results revealed that the SCF-prepared IBU dispersions produced remarkably high blood drug concentrations (both the AUC and C(max)) and a rapid absorption rate (T(max)). Finally, molecular modeling was used to evaluate the binding energy of interactions between IBU and the polymers. The negative binding energy suggests a relatively stable system. Hence, SCF technology can be used as a very effective approach to prepare IBU solid dispersions with good physical stability and enhanced in vitro and in vivo performance. |
format | Online Article Text |
id | pubmed-6409573 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-64095732019-03-29 Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability Han, Fei Zhang, Wei Wang, Ying Xi, Ziyue Chen, Lu Li, Sanming Xu, Lu Pharmaceutics Article In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The PXRD and DSC results suggested that the amorphous form of IBU was maintained in the solid dispersions. Furthermore, in vitro dissolution and in vivo pharmacokinetic (PK) studies in rats were also performed. The dissolution performance of the SCF-prepared IBU dispersions was significantly improved compared to that of the physical mixtures of crystalline IBU and a polymer. In addition, the PK results revealed that the SCF-prepared IBU dispersions produced remarkably high blood drug concentrations (both the AUC and C(max)) and a rapid absorption rate (T(max)). Finally, molecular modeling was used to evaluate the binding energy of interactions between IBU and the polymers. The negative binding energy suggests a relatively stable system. Hence, SCF technology can be used as a very effective approach to prepare IBU solid dispersions with good physical stability and enhanced in vitro and in vivo performance. MDPI 2019-02-03 /pmc/articles/PMC6409573/ /pubmed/30717471 http://dx.doi.org/10.3390/pharmaceutics11020067 Text en © 2019 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Han, Fei Zhang, Wei Wang, Ying Xi, Ziyue Chen, Lu Li, Sanming Xu, Lu Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability |
title | Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability |
title_full | Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability |
title_fullStr | Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability |
title_full_unstemmed | Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability |
title_short | Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability |
title_sort | applying supercritical fluid technology to prepare ibuprofen solid dispersions with improved oral bioavailability |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409573/ https://www.ncbi.nlm.nih.gov/pubmed/30717471 http://dx.doi.org/10.3390/pharmaceutics11020067 |
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