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Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design

Context: Microcrystalline cellulose (MCC) is the most widely used excipient for the production of pellets but it retards the release of poorly water soluble drugs. Objective: The present investigation reports incorporation of camphor, cross carmellose sodium (CCS) and spray dried lactose (SDL) into...

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Detalles Bibliográficos
Autores principales: Patel, Hetal, Patel, Hiral, Gohel, Mukesh, Tiwari, Sanjay
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5059835/
https://www.ncbi.nlm.nih.gov/pubmed/27752231
http://dx.doi.org/10.1016/j.jsps.2015.03.007
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author Patel, Hetal
Patel, Hiral
Gohel, Mukesh
Tiwari, Sanjay
author_facet Patel, Hetal
Patel, Hiral
Gohel, Mukesh
Tiwari, Sanjay
author_sort Patel, Hetal
collection PubMed
description Context: Microcrystalline cellulose (MCC) is the most widely used excipient for the production of pellets but it retards the release of poorly water soluble drugs. Objective: The present investigation reports incorporation of camphor, cross carmellose sodium (CCS) and spray dried lactose (SDL) into MCC pellets to enhance the dissolution rate of telmisartan. Materials and methods: A full factorial design (3(2)) was used in the study. Concentration of camphor and CCS was selected as independent variables whereas percentage porosity and percentage drug release at 60 min were selected as dependent variables. Pellets were produced by extrusion–spheronization technique and evaluated for percentage yield, particle size analysis, flow characteristics, percentage porosity, drug content and in vitro drug release. Contour plots and 3-D surface plots were presented for graphical expression of the results. Results and discussion: Pellet formulations exhibited acceptable morphological, flow and mechanical properties. As against to 38.54% drug release after 60 min with MCC pellets, pellets prepared with optimized formulation, composed of proper combination of MCC, SDL, camphor and CCS, released 100% drug after 60 min. Conclusion: Our study underlines the fact that dissolution of telmisartan from MCC pellets can be successfully enhanced by incorporating water soluble excipient, disintegrant and pore formers.
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spelling pubmed-50598352016-10-17 Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design Patel, Hetal Patel, Hiral Gohel, Mukesh Tiwari, Sanjay Saudi Pharm J Original Article Context: Microcrystalline cellulose (MCC) is the most widely used excipient for the production of pellets but it retards the release of poorly water soluble drugs. Objective: The present investigation reports incorporation of camphor, cross carmellose sodium (CCS) and spray dried lactose (SDL) into MCC pellets to enhance the dissolution rate of telmisartan. Materials and methods: A full factorial design (3(2)) was used in the study. Concentration of camphor and CCS was selected as independent variables whereas percentage porosity and percentage drug release at 60 min were selected as dependent variables. Pellets were produced by extrusion–spheronization technique and evaluated for percentage yield, particle size analysis, flow characteristics, percentage porosity, drug content and in vitro drug release. Contour plots and 3-D surface plots were presented for graphical expression of the results. Results and discussion: Pellet formulations exhibited acceptable morphological, flow and mechanical properties. As against to 38.54% drug release after 60 min with MCC pellets, pellets prepared with optimized formulation, composed of proper combination of MCC, SDL, camphor and CCS, released 100% drug after 60 min. Conclusion: Our study underlines the fact that dissolution of telmisartan from MCC pellets can be successfully enhanced by incorporating water soluble excipient, disintegrant and pore formers. Elsevier 2016-09 2015-03-23 /pmc/articles/PMC5059835/ /pubmed/27752231 http://dx.doi.org/10.1016/j.jsps.2015.03.007 Text en © 2015 The Authors 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
Patel, Hetal
Patel, Hiral
Gohel, Mukesh
Tiwari, Sanjay
Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design
title Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design
title_full Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design
title_fullStr Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design
title_full_unstemmed Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design
title_short Dissolution rate improvement of telmisartan through modified MCC pellets using 3(2) full factorial design
title_sort dissolution rate improvement of telmisartan through modified mcc pellets using 3(2) full factorial design
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5059835/
https://www.ncbi.nlm.nih.gov/pubmed/27752231
http://dx.doi.org/10.1016/j.jsps.2015.03.007
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AT tiwarisanjay dissolutionrateimprovementoftelmisartanthroughmodifiedmccpelletsusing32fullfactorialdesign