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Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits

The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1–F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (...

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Autores principales: Razavi, Mahboubeh, Karimian, Hamed, Yeong, Chai Hong, Chung, Lip Yong, Nyamathulla, Shaik, Noordin, Mohamed Ibrahim
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4532171/
https://www.ncbi.nlm.nih.gov/pubmed/26273196
http://dx.doi.org/10.2147/DDDT.S86263
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author Razavi, Mahboubeh
Karimian, Hamed
Yeong, Chai Hong
Chung, Lip Yong
Nyamathulla, Shaik
Noordin, Mohamed Ibrahim
author_facet Razavi, Mahboubeh
Karimian, Hamed
Yeong, Chai Hong
Chung, Lip Yong
Nyamathulla, Shaik
Noordin, Mohamed Ibrahim
author_sort Razavi, Mahboubeh
collection PubMed
description The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1–F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm(2)O(3)) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics.
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spelling pubmed-45321712015-08-13 Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits Razavi, Mahboubeh Karimian, Hamed Yeong, Chai Hong Chung, Lip Yong Nyamathulla, Shaik Noordin, Mohamed Ibrahim Drug Des Devel Ther Original Research The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1–F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm(2)O(3)) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics. Dove Medical Press 2015-08-06 /pmc/articles/PMC4532171/ /pubmed/26273196 http://dx.doi.org/10.2147/DDDT.S86263 Text en © 2015 Razavi et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Razavi, Mahboubeh
Karimian, Hamed
Yeong, Chai Hong
Chung, Lip Yong
Nyamathulla, Shaik
Noordin, Mohamed Ibrahim
Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
title Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
title_full Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
title_fullStr Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
title_full_unstemmed Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
title_short Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
title_sort gamma scintigraphic evaluation of floating gastroretentive tablets of metformin hcl using a combination of three natural polymers in rabbits
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4532171/
https://www.ncbi.nlm.nih.gov/pubmed/26273196
http://dx.doi.org/10.2147/DDDT.S86263
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