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Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers
Gastroretentive raft-forming formulations were developed in liquid and chewable tablet dosage forms to achieve prolonged delivery of quercetin in the stomach. The formulations contained a solid dispersion of quercetin and polyvinylpyrrolidone (PVP K 30) at a 1:10 w/w ratio to improve the solubility...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8523354/ https://www.ncbi.nlm.nih.gov/pubmed/34703368 http://dx.doi.org/10.1016/j.jsps.2021.08.005 |
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author | Bunlung, Suputra Nualnoi, Teerapat Issarachot, Ousanee Wiwattanapatapee, Ruedeekorn |
author_facet | Bunlung, Suputra Nualnoi, Teerapat Issarachot, Ousanee Wiwattanapatapee, Ruedeekorn |
author_sort | Bunlung, Suputra |
collection | PubMed |
description | Gastroretentive raft-forming formulations were developed in liquid and chewable tablet dosage forms to achieve prolonged delivery of quercetin in the stomach. The formulations contained a solid dispersion of quercetin and polyvinylpyrrolidone (PVP K 30) at a 1:10 w/w ratio to improve the solubility of the flavonoid. The formulations also contained sodium alginate as a gel forming agent, calcium carbonate as a calcium source and carbon dioxide producer and hydroxypropyl methylcellulose K100M as a drug release retarding polymer. The chewable tablets incorporated mannitol as a diluent. Both liquid and chewable tablet formulations exhibited rapid floating behaviour (lag time < 1 min) and long floating duration (>24 h) in 0.1 N HCl. The optimized liquid formulation showed superior characteristics based on high raft strength (10.4 g) and sustained release of quercetin (93 % over 8 h) whereas the optimized chewable tablet formulation exhibited lower raft strength (7.2 g) and lower drug release (79 % in 8 h). The optimized liquid and chewable tablet formulations were found to induce anti-inflammatory activity in cell culture using RAW 264.7 cells macrophages and enhance the migration of human gastric adenocarcinoma (AGS) epithelial cells in vitro, indicating wound healing potential for treatment of gastric ulcers. |
format | Online Article Text |
id | pubmed-8523354 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-85233542021-10-25 Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers Bunlung, Suputra Nualnoi, Teerapat Issarachot, Ousanee Wiwattanapatapee, Ruedeekorn Saudi Pharm J Original Article Gastroretentive raft-forming formulations were developed in liquid and chewable tablet dosage forms to achieve prolonged delivery of quercetin in the stomach. The formulations contained a solid dispersion of quercetin and polyvinylpyrrolidone (PVP K 30) at a 1:10 w/w ratio to improve the solubility of the flavonoid. The formulations also contained sodium alginate as a gel forming agent, calcium carbonate as a calcium source and carbon dioxide producer and hydroxypropyl methylcellulose K100M as a drug release retarding polymer. The chewable tablets incorporated mannitol as a diluent. Both liquid and chewable tablet formulations exhibited rapid floating behaviour (lag time < 1 min) and long floating duration (>24 h) in 0.1 N HCl. The optimized liquid formulation showed superior characteristics based on high raft strength (10.4 g) and sustained release of quercetin (93 % over 8 h) whereas the optimized chewable tablet formulation exhibited lower raft strength (7.2 g) and lower drug release (79 % in 8 h). The optimized liquid and chewable tablet formulations were found to induce anti-inflammatory activity in cell culture using RAW 264.7 cells macrophages and enhance the migration of human gastric adenocarcinoma (AGS) epithelial cells in vitro, indicating wound healing potential for treatment of gastric ulcers. Elsevier 2021-10 2021-08-09 /pmc/articles/PMC8523354/ /pubmed/34703368 http://dx.doi.org/10.1016/j.jsps.2021.08.005 Text en © 2021 The Author(s) https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Original Article Bunlung, Suputra Nualnoi, Teerapat Issarachot, Ousanee Wiwattanapatapee, Ruedeekorn Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
title | Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
title_full | Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
title_fullStr | Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
title_full_unstemmed | Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
title_short | Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
title_sort | development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8523354/ https://www.ncbi.nlm.nih.gov/pubmed/34703368 http://dx.doi.org/10.1016/j.jsps.2021.08.005 |
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