Surfactants modify the release from tablets made of hydrophobically modified poly (acrylic acid)
(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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/4250650
- author
- Knöös, Patrik LU ; Onder, Sebla ; Pedersen, Lina ; Piculell, Lennart LU ; Ulvenlund, Stefan LU and Wahlgren, Marie
- organization
- publishing date
- 2013
- 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}}, }