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Oral-based controlled release formulations using poly(acrylic acid) microgels.

Wahlgren, M LU ; Christensen, Karin Löwenstein; Jørgensen, Erik Valentin; Svensson, Anna and Ulvenlund, S LU (2009) In Drug Development and Industrial Pharmacy 35. p.922-929
Abstract
Aim: To investigate the release of hydrophobic and hydrophilic substances from tablets containing Pemulen and Carbopol as excipients. Method: The dissolution patterns of a hydrophobic (diazepam) and a hydrophilic active substance (midodrine-HCl) from different tablet formulations containing a nonmodified polyacrylic microgel (Carbopol 981 F) or a hydrophobically modified polyacrylic microgel (Pemulen(R)) have been studied. Possible differences in dissolution in phosphate buffer (pH 6.8) and in 0.1 M HCl between tablets produced using wet granulation and direct compression were also investigated. Results: Tablets produced by wet granulation had a greater effect on the release of active substance from the tablets. No major differences were... (More)
Aim: To investigate the release of hydrophobic and hydrophilic substances from tablets containing Pemulen and Carbopol as excipients. Method: The dissolution patterns of a hydrophobic (diazepam) and a hydrophilic active substance (midodrine-HCl) from different tablet formulations containing a nonmodified polyacrylic microgel (Carbopol 981 F) or a hydrophobically modified polyacrylic microgel (Pemulen(R)) have been studied. Possible differences in dissolution in phosphate buffer (pH 6.8) and in 0.1 M HCl between tablets produced using wet granulation and direct compression were also investigated. Results: Tablets produced by wet granulation had a greater effect on the release of active substance from the tablets. No major differences were observed in the release patterns of the hydrophilic substance midodrine-HCl from wet granulated tablets based on Carbopol and Pemulen. However, the release pattern of the more hydrophobic drug substance, diazepam, differed considerably between the two polymers. Wet granulation gave reproducible release patterns. The release patterns from the polymers differed considerably at pH 6.8 but were similar at low pH. Conclusions: The release of the diazepam from the hydrophobic polymer Pemulen was very slow, and the release was close to zero order. (Less)
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Drug Development and Industrial Pharmacy
volume
35
pages
8 pages
publisher
Marcel Dekker
external identifiers
  • wos:000268879400004
  • pmid:19466881
  • scopus:70350683737
ISSN
0363-9045
DOI
10.1080/03639040802698810
language
English
LU publication?
yes
id
68bfdf4f-b801-43a3-9088-6d033dd3df9a (old id 1412036)
date added to LUP
2009-06-11 09:00:15
date last changed
2017-02-05 03:27:46
@article{68bfdf4f-b801-43a3-9088-6d033dd3df9a,
  abstract     = {Aim: To investigate the release of hydrophobic and hydrophilic substances from tablets containing Pemulen and Carbopol as excipients. Method: The dissolution patterns of a hydrophobic (diazepam) and a hydrophilic active substance (midodrine-HCl) from different tablet formulations containing a nonmodified polyacrylic microgel (Carbopol 981 F) or a hydrophobically modified polyacrylic microgel (Pemulen(R)) have been studied. Possible differences in dissolution in phosphate buffer (pH 6.8) and in 0.1 M HCl between tablets produced using wet granulation and direct compression were also investigated. Results: Tablets produced by wet granulation had a greater effect on the release of active substance from the tablets. No major differences were observed in the release patterns of the hydrophilic substance midodrine-HCl from wet granulated tablets based on Carbopol and Pemulen. However, the release pattern of the more hydrophobic drug substance, diazepam, differed considerably between the two polymers. Wet granulation gave reproducible release patterns. The release patterns from the polymers differed considerably at pH 6.8 but were similar at low pH. Conclusions: The release of the diazepam from the hydrophobic polymer Pemulen was very slow, and the release was close to zero order.},
  author       = {Wahlgren, M and Christensen, Karin Löwenstein and Jørgensen, Erik Valentin and Svensson, Anna and Ulvenlund, S},
  issn         = {0363-9045},
  language     = {eng},
  pages        = {922--929},
  publisher    = {Marcel Dekker},
  series       = {Drug Development and Industrial Pharmacy},
  title        = {Oral-based controlled release formulations using poly(acrylic acid) microgels.},
  url          = {http://dx.doi.org/10.1080/03639040802698810},
  volume       = {35},
  year         = {2009},
}