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Model drug release from matrix tablets composed of HPMC with different substituent heterogeneity

Viriden, Anna; Larsson, Anette; Schagerlöf, Herje LU and Wittgren, Bengt (2010) In International Journal of Pharmaceutics 401(1-2). p.60-67
Abstract
The release of a model drug substance, methylparaben, was studied in matrix tablets composed of hydroxypropyl methylcellulose (HPMC) batches of the USP 2208 grade that had different chemical compositions. It was found that chemically heterogeneous HPMC batches with longer sections of low substituted regions and lower hydroxypropoxy content facilitated the formation of reversible gel structures at a temperature as low as 37 degrees C. Most importantly, these structures were shown to affect the release of the drug from matrix tablets, where the drug release decreased with increased heterogeneity and a difference in T80 values of 7 h was observed between the compositions. This could be explained by the much lower erosion rate of the... (More)
The release of a model drug substance, methylparaben, was studied in matrix tablets composed of hydroxypropyl methylcellulose (HPMC) batches of the USP 2208 grade that had different chemical compositions. It was found that chemically heterogeneous HPMC batches with longer sections of low substituted regions and lower hydroxypropoxy content facilitated the formation of reversible gel structures at a temperature as low as 37 degrees C. Most importantly, these structures were shown to affect the release of the drug from matrix tablets, where the drug release decreased with increased heterogeneity and a difference in T80 values of 7 h was observed between the compositions. This could be explained by the much lower erosion rate of the heterogeneous HPMC batches, which decreased the drug release rate and also released the drug with a more diffusion based release mechanism compared to the less heterogeneous batches. It can therefore be concluded that the drug release from matrix tablets is very sensitive to variations in the chemical heterogeneity of HPMC. (C) 2010 Elsevier B.V. All rights reserved. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
methylcellulose, Hydroxypropyl, Hydrophilic matrix tablets, Drug release, Batch-to-batch variation, Chemical heterogeneous
in
International Journal of Pharmaceutics
volume
401
issue
1-2
pages
60 - 67
publisher
Elsevier
external identifiers
  • wos:000285222700009
  • scopus:78049297947
ISSN
1873-3476
DOI
10.1016/j.ijpharm.2010.09.017
language
English
LU publication?
yes
id
9aef33f3-0cc7-4ca9-99a5-69548fa862c8 (old id 1773469)
date added to LUP
2011-02-01 15:51:22
date last changed
2018-05-29 09:19:53
@article{9aef33f3-0cc7-4ca9-99a5-69548fa862c8,
  abstract     = {The release of a model drug substance, methylparaben, was studied in matrix tablets composed of hydroxypropyl methylcellulose (HPMC) batches of the USP 2208 grade that had different chemical compositions. It was found that chemically heterogeneous HPMC batches with longer sections of low substituted regions and lower hydroxypropoxy content facilitated the formation of reversible gel structures at a temperature as low as 37 degrees C. Most importantly, these structures were shown to affect the release of the drug from matrix tablets, where the drug release decreased with increased heterogeneity and a difference in T80 values of 7 h was observed between the compositions. This could be explained by the much lower erosion rate of the heterogeneous HPMC batches, which decreased the drug release rate and also released the drug with a more diffusion based release mechanism compared to the less heterogeneous batches. It can therefore be concluded that the drug release from matrix tablets is very sensitive to variations in the chemical heterogeneity of HPMC. (C) 2010 Elsevier B.V. All rights reserved.},
  author       = {Viriden, Anna and Larsson, Anette and Schagerlöf, Herje and Wittgren, Bengt},
  issn         = {1873-3476},
  keyword      = {methylcellulose,Hydroxypropyl,Hydrophilic matrix tablets,Drug release,Batch-to-batch variation,Chemical heterogeneous},
  language     = {eng},
  number       = {1-2},
  pages        = {60--67},
  publisher    = {Elsevier},
  series       = {International Journal of Pharmaceutics},
  title        = {Model drug release from matrix tablets composed of HPMC with different substituent heterogeneity},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2010.09.017},
  volume       = {401},
  year         = {2010},
}