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

Knöös, Patrik LU ; Onder, Sebla ; Pedersen, Lina ; Piculell, Lennart LU ; Ulvenlund, Stefan LU and Wahlgren, Marie (2013) In Results in Pharma Sciences 3. p.7-14
Abstract
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... (More)
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. (Less)
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author
; ; ; ; and
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Results in Pharma Sciences
volume
3
pages
7 - 14
publisher
Elsevier
external identifiers
  • scopus:84884932412
  • pmid:25755999
ISSN
2211-2863
DOI
10.1016/j.rinphs.2013.08.001
language
English
LU publication?
yes
id
e9f123f0-54b2-4980-ba39-0396379411c4 (old id 4250650)
date added to LUP
2016-04-01 13:45:47
date last changed
2023-12-11 19:39:36
@article{e9f123f0-54b2-4980-ba39-0396379411c4,
  abstract     = {{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.<br/><br>
<br/><br>
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.}},
  author       = {{Knöös, Patrik and Onder, Sebla and Pedersen, Lina and Piculell, Lennart and Ulvenlund, Stefan and Wahlgren, Marie}},
  issn         = {{2211-2863}},
  language     = {{eng}},
  pages        = {{7--14}},
  publisher    = {{Elsevier}},
  series       = {{Results in Pharma Sciences}},
  title        = {{Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)}},
  url          = {{http://dx.doi.org/10.1016/j.rinphs.2013.08.001}},
  doi          = {{10.1016/j.rinphs.2013.08.001}},
  volume       = {{3}},
  year         = {{2013}},
}