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A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets
Etoricoxib, as a model drug, has a poor solubility and dissolution rate. Cyclodextrin derivatives can be used to solve such a problem. A comparative study was run on three cyclodextrin derivatives, namely β-CD, HP β-CD, and SBE β-CD, to solve the drug problem through the formulation of solid dispers...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10525456/ https://www.ncbi.nlm.nih.gov/pubmed/37760881 http://dx.doi.org/10.3390/biomedicines11092440 |
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author | Elsegaie, Doaa El-Nabarawi, Mohamed A. Mahmoud, Hanaa Abdelmonem Teaima, Mahmoud Louis, Dina |
author_facet | Elsegaie, Doaa El-Nabarawi, Mohamed A. Mahmoud, Hanaa Abdelmonem Teaima, Mahmoud Louis, Dina |
author_sort | Elsegaie, Doaa |
collection | PubMed |
description | Etoricoxib, as a model drug, has a poor solubility and dissolution rate. Cyclodextrin derivatives can be used to solve such a problem. A comparative study was run on three cyclodextrin derivatives, namely β-CD, HP β-CD, and SBE β-CD, to solve the drug problem through the formulation of solid dispersions and their preparation into fast-dissolving tablets. Preparations utilized different (1:1, 1:2, and 1:4) drug:carrier ratios. Nine fast-dissolving tablets (containing 1:4 drug: carrier) were formulated using Prosolv ODT(®) and/or F-melt(®) type C as super-disintegrants. Optimized formulation was chosen based on a 3(2) factorial design. The responses chosen were the outcomes of the in vitro evaluation tests. The optimized formulation that had the highest desirability (0.86) was found to be SD-HP3, which was prepared from etoricoxib: HP β-CD at a 1:4 ratio using equal amounts of Prosolv ODT(®) and F-melt(®) type C. An in vivo evaluation of SD-HP3 on a rabbit model revealed its superiority over the marketed product Arcoxia(®). SD-HP3 showed a significantly lower Tmax (13.3 min) and a significantly higher Cmax (9122.156 μg/mL), as well as a significantly higher AUC, than Arcoxia(®). Thus, the solubility, dissolution, and bioavailability of etoricoxib were significantly enhanced. |
format | Online Article Text |
id | pubmed-10525456 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-105254562023-09-28 A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets Elsegaie, Doaa El-Nabarawi, Mohamed A. Mahmoud, Hanaa Abdelmonem Teaima, Mahmoud Louis, Dina Biomedicines Article Etoricoxib, as a model drug, has a poor solubility and dissolution rate. Cyclodextrin derivatives can be used to solve such a problem. A comparative study was run on three cyclodextrin derivatives, namely β-CD, HP β-CD, and SBE β-CD, to solve the drug problem through the formulation of solid dispersions and their preparation into fast-dissolving tablets. Preparations utilized different (1:1, 1:2, and 1:4) drug:carrier ratios. Nine fast-dissolving tablets (containing 1:4 drug: carrier) were formulated using Prosolv ODT(®) and/or F-melt(®) type C as super-disintegrants. Optimized formulation was chosen based on a 3(2) factorial design. The responses chosen were the outcomes of the in vitro evaluation tests. The optimized formulation that had the highest desirability (0.86) was found to be SD-HP3, which was prepared from etoricoxib: HP β-CD at a 1:4 ratio using equal amounts of Prosolv ODT(®) and F-melt(®) type C. An in vivo evaluation of SD-HP3 on a rabbit model revealed its superiority over the marketed product Arcoxia(®). SD-HP3 showed a significantly lower Tmax (13.3 min) and a significantly higher Cmax (9122.156 μg/mL), as well as a significantly higher AUC, than Arcoxia(®). Thus, the solubility, dissolution, and bioavailability of etoricoxib were significantly enhanced. MDPI 2023-09-01 /pmc/articles/PMC10525456/ /pubmed/37760881 http://dx.doi.org/10.3390/biomedicines11092440 Text en © 2023 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 Elsegaie, Doaa El-Nabarawi, Mohamed A. Mahmoud, Hanaa Abdelmonem Teaima, Mahmoud Louis, Dina A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets |
title | A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets |
title_full | A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets |
title_fullStr | A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets |
title_full_unstemmed | A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets |
title_short | A Comparative Study on Cyclodextrin Derivatives in Improving Oral Bioavailability of Etoricoxib as a Model Drug: Formulation and Evaluation of Solid Dispersion-Based Fast-Dissolving Tablets |
title_sort | comparative study on cyclodextrin derivatives in improving oral bioavailability of etoricoxib as a model drug: formulation and evaluation of solid dispersion-based fast-dissolving tablets |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10525456/ https://www.ncbi.nlm.nih.gov/pubmed/37760881 http://dx.doi.org/10.3390/biomedicines11092440 |
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