Ghent University Academic Bibliography

Advanced

Preparation and evaluation of sustained-release matrix tablets based on metoprolol and an acrylic carrier using injection moulding

Thomas Quinten, GP Andrews, Thomas De Beer UGent, Lien Saerens UGent, Wim Bouquet-Geerardyn, DS Jones, P Hornsby, Jean Paul Remon UGent and Chris Vervaet UGent (2012) AAPS PHARMSCITECH. 13(4). p.1197-1211
abstract
Sustained-release matrix tablets based on Eudragit RL and RS were manufactured by injection moulding. The influence of process temperature; matrix composition; drug load, plasticizer level; and salt form of metoprolol: tartrate (MPT), fumarate (MPF) and succinate (MPS) on ease of processing and drug release were evaluated. Formulations composed of 70/30% Eudragit RL/MPT showed the fastest drug release, substituting part of Eudragit RL by RS resulted in slower drug release, all following first-order release kinetics. Drug load only affected drug release of matrices composed of Eudragit RS: a higher MPT concentration yielded faster release rates. Adding triethyl citrate enhanced the processability, but was detrimental to long-term stability. The process temperature and plasticizer level had no effect on drug release, whereas metoprolol salt form significantly influenced release properties. The moulded tablets had a low porosity and a smooth surface morphology. A plasticizing effect of MPT, MPS and MPF on Eudragit RS and Eudragit RL was observed via DSC and DMA. Solubility parameter assessment, thermal analysis and X-ray diffraction demonstrated the formation of a solid solution immediately after production, in which H-bonds were formed between metoprolol and Eudragit as evidenced by near-infrared spectroscopy. However, high drug loadings of MPS and MPF showed a tendency to recrystallise during storage. The in vivo performance of injection-moulded tablets was strongly dependent upon drug loading.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
sustained release, solid state, tablet, WATER-SOLUBLE DRUGS, physicochemical properties, metoprolol, matrix, injection moulding, drug release, drug polymer interaction, acrylates, controlled release, SOLUBILITY PARAMETERS, SOLID DISPERSIONS, MELT EXTRUSION, POLYMERS, DELIVERY, PERMEABILITY, COPOLYMERS, RS, RL
journal title
AAPS PHARMSCITECH
AAPS PharmSciTech
volume
13
issue
4
pages
1197 - 1211
Web of Science type
Article
Web of Science id
000313500500019
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
1.584 (2012)
JCR rank
173/259 (2012)
JCR quartile
3 (2012)
ISSN
1530-9932
DOI
10.1208/s12249-012-9848-6
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
4142918
handle
http://hdl.handle.net/1854/LU-4142918
date created
2013-09-23 16:02:22
date last changed
2016-12-19 15:46:03
@article{4142918,
  abstract     = {Sustained-release matrix tablets based on Eudragit RL and RS were manufactured by injection moulding. The influence of process temperature; matrix composition; drug load, plasticizer level; and salt form of metoprolol: tartrate (MPT), fumarate (MPF) and succinate (MPS) on ease of processing and drug release were evaluated. Formulations composed of 70/30\% Eudragit RL/MPT showed the fastest drug release, substituting part of Eudragit RL by RS resulted in slower drug release, all following first-order release kinetics. Drug load only affected drug release of matrices composed of Eudragit RS: a higher MPT concentration yielded faster release rates. Adding triethyl citrate enhanced the processability, but was detrimental to long-term stability. The process temperature and plasticizer level had no effect on drug release, whereas metoprolol salt form significantly influenced release properties. The moulded tablets had a low porosity and a smooth surface morphology. A plasticizing effect of MPT, MPS and MPF on Eudragit RS and Eudragit RL was observed via DSC and DMA. Solubility parameter assessment, thermal analysis and X-ray diffraction demonstrated the formation of a solid solution immediately after production, in which H-bonds were formed between metoprolol and Eudragit as evidenced by near-infrared spectroscopy. However, high drug loadings of MPS and MPF showed a tendency to recrystallise during storage. The in vivo performance of injection-moulded tablets was strongly dependent upon drug loading.},
  author       = {Quinten, Thomas and Andrews, GP and De Beer, Thomas and Saerens, Lien and Bouquet-Geerardyn, Wim and Jones, DS and Hornsby, P and Remon, Jean Paul and Vervaet, Chris},
  issn         = {1530-9932},
  journal      = {AAPS PHARMSCITECH},
  keyword      = {sustained release,solid state,tablet,WATER-SOLUBLE DRUGS,physicochemical properties,metoprolol,matrix,injection moulding,drug release,drug polymer interaction,acrylates,controlled release,SOLUBILITY PARAMETERS,SOLID DISPERSIONS,MELT EXTRUSION,POLYMERS,DELIVERY,PERMEABILITY,COPOLYMERS,RS,RL},
  language     = {eng},
  number       = {4},
  pages        = {1197--1211},
  title        = {Preparation and evaluation of sustained-release matrix tablets based on metoprolol and an acrylic carrier using injection moulding},
  url          = {http://dx.doi.org/10.1208/s12249-012-9848-6},
  volume       = {13},
  year         = {2012},
}

Chicago
Quinten, Thomas, GP Andrews, Thomas De Beer, Lien Saerens, Wim Bouquet-Geerardyn, DS Jones, P Hornsby, Jean Paul Remon, and Chris Vervaet. 2012. “Preparation and Evaluation of Sustained-release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding.” Aaps Pharmscitech 13 (4): 1197–1211.
APA
Quinten, T., Andrews, G., De Beer, T., Saerens, L., Bouquet-Geerardyn, W., Jones, D., Hornsby, P., et al. (2012). Preparation and evaluation of sustained-release matrix tablets based on metoprolol and an acrylic carrier using injection moulding. AAPS PHARMSCITECH, 13(4), 1197–1211.
Vancouver
1.
Quinten T, Andrews G, De Beer T, Saerens L, Bouquet-Geerardyn W, Jones D, et al. Preparation and evaluation of sustained-release matrix tablets based on metoprolol and an acrylic carrier using injection moulding. AAPS PHARMSCITECH. 2012;13(4):1197–211.
MLA
Quinten, Thomas, GP Andrews, Thomas De Beer, et al. “Preparation and Evaluation of Sustained-release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding.” AAPS PHARMSCITECH 13.4 (2012): 1197–1211. Print.