Cargando…

Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics

The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and also to reduce the side effects in upper gastrointestinal tract. Direct compression method was used to...

Descripción completa

Detalles Bibliográficos
Autores principales: Vemula, Sateesh Kumar, Bontha, Vijaya Kumar
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3821905/
https://www.ncbi.nlm.nih.gov/pubmed/24260738
http://dx.doi.org/10.1155/2013/287919
_version_ 1782290367607996416
author Vemula, Sateesh Kumar
Bontha, Vijaya Kumar
author_facet Vemula, Sateesh Kumar
Bontha, Vijaya Kumar
author_sort Vemula, Sateesh Kumar
collection PubMed
description The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and also to reduce the side effects in upper gastrointestinal tract. Direct compression method was used to prepare flurbiprofen core tablets, and they were compression coated with guar gum. Then the tablets were optimized with the support of in vitro dissolution studies, and further it was proved by pharmacokinetic studies. The optimized formulation (F4) showed almost complete drug release in the colon (99.86%) within 24 h without drug loss in the initial lag period of 5 h (only 6.84% drug release was observed during this period). The pharmacokinetic estimations proved the capability of guar gum compression coated tablets to achieve colon targeting. The C (max) of colon targeted tablets was 11956.15 ng/mL at T (max) of 10 h whereas it was 15677.52 ng/mL at 3 h in case of immediate release tablets. The area under the curve for the immediate release and compression coated tablets was 40385.78 and 78214.50 ng-h/mL and the mean resident time was 3.49 and 10.78 h, respectively. In conclusion, formulation of guar gum compression coated tablets was appropriate for colon targeting of flurbiprofen.
format Online
Article
Text
id pubmed-3821905
institution National Center for Biotechnology Information
language English
publishDate 2013
publisher Hindawi Publishing Corporation
record_format MEDLINE/PubMed
spelling pubmed-38219052013-11-20 Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics Vemula, Sateesh Kumar Bontha, Vijaya Kumar Biomed Res Int Clinical Study The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and also to reduce the side effects in upper gastrointestinal tract. Direct compression method was used to prepare flurbiprofen core tablets, and they were compression coated with guar gum. Then the tablets were optimized with the support of in vitro dissolution studies, and further it was proved by pharmacokinetic studies. The optimized formulation (F4) showed almost complete drug release in the colon (99.86%) within 24 h without drug loss in the initial lag period of 5 h (only 6.84% drug release was observed during this period). The pharmacokinetic estimations proved the capability of guar gum compression coated tablets to achieve colon targeting. The C (max) of colon targeted tablets was 11956.15 ng/mL at T (max) of 10 h whereas it was 15677.52 ng/mL at 3 h in case of immediate release tablets. The area under the curve for the immediate release and compression coated tablets was 40385.78 and 78214.50 ng-h/mL and the mean resident time was 3.49 and 10.78 h, respectively. In conclusion, formulation of guar gum compression coated tablets was appropriate for colon targeting of flurbiprofen. Hindawi Publishing Corporation 2013 2013-10-24 /pmc/articles/PMC3821905/ /pubmed/24260738 http://dx.doi.org/10.1155/2013/287919 Text en Copyright © 2013 S. K. Vemula and V. K. Bontha. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Clinical Study
Vemula, Sateesh Kumar
Bontha, Vijaya Kumar
Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics
title Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics
title_full Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics
title_fullStr Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics
title_full_unstemmed Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics
title_short Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics
title_sort colon targeted guar gum compression coated tablets of flurbiprofen: formulation, development, and pharmacokinetics
topic Clinical Study
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3821905/
https://www.ncbi.nlm.nih.gov/pubmed/24260738
http://dx.doi.org/10.1155/2013/287919
work_keys_str_mv AT vemulasateeshkumar colontargetedguargumcompressioncoatedtabletsofflurbiprofenformulationdevelopmentandpharmacokinetics
AT bonthavijayakumar colontargetedguargumcompressioncoatedtabletsofflurbiprofenformulationdevelopmentandpharmacokinetics