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Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()

Many novel pharmaceutically active substances are characterized by a high hydrophobicity and a low water solubility, which present challenges for their delivery as drugs. Tablets made from cross-linked hydrophobically modified poly (acrylic acid) (CLHMPAA), commercially available as Pemulen™, have p...

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Autores principales: Knöös, Patrik, Onder, Sebla, Pedersen, Lina, Piculell, Lennart, Ulvenlund, Stefan, Wahlgren, Marie
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3940118/
https://www.ncbi.nlm.nih.gov/pubmed/25755999
http://dx.doi.org/10.1016/j.rinphs.2013.08.001
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author Knöös, Patrik
Onder, Sebla
Pedersen, Lina
Piculell, Lennart
Ulvenlund, Stefan
Wahlgren, Marie
author_facet Knöös, Patrik
Onder, Sebla
Pedersen, Lina
Piculell, Lennart
Ulvenlund, Stefan
Wahlgren, Marie
author_sort Knöös, Patrik
collection PubMed
description Many novel pharmaceutically active substances are characterized by a high hydrophobicity and a low water solubility, which present challenges for their delivery as drugs. Tablets made from cross-linked hydrophobically modified poly (acrylic acid) (CLHMPAA), commercially available as Pemulen™, have previously shown promising abilities to control the release of hydrophobic model substances. This study further investigates the possibility to use CLHMPAA in tablet formulations using ibuprofen as a model substance. Furthermore, surfactants were added to the dissolution medium in order to simulate the presence of bile salts in the intestine. The release of ibuprofen is strongly affected by the presence of surfactant and/or buffer in the dissolution medium, which affect both the behaviour of CLHMPAA and the swelling of the gel layer that surrounds the disintegrating tablets. Two mechanisms of tablet disintegration were observed under shear, namely conventional dissolution of a soluble tablet matrix and erosion of swollen insoluble gel particles from the tablet. The effects of surfactant in the surrounding medium can be circumvented by addition of surfactant to the tablet. With added surfactant, tablets that may be insusceptible to the differences in bile salt level between fasted or fed states have been produced, thus addressing a central problem in controlled delivery of hydrophobic drugs. In other words CLHMPAA is a potential candidate to be used in tablet formulations for controlled release with poorly soluble drugs.
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spelling pubmed-39401182015-03-09 Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)() Knöös, Patrik Onder, Sebla Pedersen, Lina Piculell, Lennart Ulvenlund, Stefan Wahlgren, Marie Results Pharma Sci Article Many novel pharmaceutically active substances are characterized by a high hydrophobicity and a low water solubility, which present challenges for their delivery as drugs. Tablets made from cross-linked hydrophobically modified poly (acrylic acid) (CLHMPAA), commercially available as Pemulen™, have previously shown promising abilities to control the release of hydrophobic model substances. This study further investigates the possibility to use CLHMPAA in tablet formulations using ibuprofen as a model substance. Furthermore, surfactants were added to the dissolution medium in order to simulate the presence of bile salts in the intestine. The release of ibuprofen is strongly affected by the presence of surfactant and/or buffer in the dissolution medium, which affect both the behaviour of CLHMPAA and the swelling of the gel layer that surrounds the disintegrating tablets. Two mechanisms of tablet disintegration were observed under shear, namely conventional dissolution of a soluble tablet matrix and erosion of swollen insoluble gel particles from the tablet. The effects of surfactant in the surrounding medium can be circumvented by addition of surfactant to the tablet. With added surfactant, tablets that may be insusceptible to the differences in bile salt level between fasted or fed states have been produced, thus addressing a central problem in controlled delivery of hydrophobic drugs. In other words CLHMPAA is a potential candidate to be used in tablet formulations for controlled release with poorly soluble drugs. Elsevier 2013-09-13 /pmc/articles/PMC3940118/ /pubmed/25755999 http://dx.doi.org/10.1016/j.rinphs.2013.08.001 Text en © 2013 The Authors http://creativecommons.org/licenses/by-nc-nd/3.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial-No Derivative Works License, which permits non-commercial use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Article
Knöös, Patrik
Onder, Sebla
Pedersen, Lina
Piculell, Lennart
Ulvenlund, Stefan
Wahlgren, Marie
Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
title Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
title_full Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
title_fullStr Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
title_full_unstemmed Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
title_short Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
title_sort surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)()
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3940118/
https://www.ncbi.nlm.nih.gov/pubmed/25755999
http://dx.doi.org/10.1016/j.rinphs.2013.08.001
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