Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Bunlung, Suputra, Nualnoi, Teerapat, Issarachot, Ousanee, Wiwattanapatapee, Ruedeekorn
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
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
_version_ 1784585284686446592
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
work_keys_str_mv AT bunlungsuputra developmentofraftformingliquidandchewabletabletformulationsincorporatingquercetinsoliddispersionsfortreatmentofgastriculcers
AT nualnoiteerapat developmentofraftformingliquidandchewabletabletformulationsincorporatingquercetinsoliddispersionsfortreatmentofgastriculcers
AT issarachotousanee developmentofraftformingliquidandchewabletabletformulationsincorporatingquercetinsoliddispersionsfortreatmentofgastriculcers
AT wiwattanapatapeeruedeekorn developmentofraftformingliquidandchewabletabletformulationsincorporatingquercetinsoliddispersionsfortreatmentofgastriculcers