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

(2012) AAPS PHARMSCITECH. 13(4). p.1197-1211
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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.
Keywords
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

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MLA
Quinten, Thomas, et al. “Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding.” AAPS PHARMSCITECH, vol. 13, no. 4, 2012, pp. 1197–211, doi:10.1208/s12249-012-9848-6.
APA
Quinten, T., Andrews, G., De Beer, T., Saerens, L., Bouquet-Geerardyn, W., Jones, D., … Vervaet, C. (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. https://doi.org/10.1208/s12249-012-9848-6
Chicago author-date
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. https://doi.org/10.1208/s12249-012-9848-6.
Chicago author-date (all authors)
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. doi:10.1208/s12249-012-9848-6.
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.
IEEE
[1]
T. Quinten et al., “Preparation and evaluation of sustained-release matrix tablets based on metoprolol and an acrylic carrier using injection moulding,” AAPS PHARMSCITECH, vol. 13, no. 4, pp. 1197–1211, 2012.
@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}},
  keywords     = {{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://doi.org/10.1208/s12249-012-9848-6}},
  volume       = {{13}},
  year         = {{2012}},
}

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