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Development and evaluation of injection-moulded sustained-release tablets containing ethylcellulose and polyethylene oxide

Thomas Quinten UGent, Thomas De Beer UGent, Ana Almeida UGent, Jelle Vlassenbroeck UGent, Luc Van Hoorebeke UGent and Jean Paul Remon UGent (2011) DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY. 37(2). p.149-159
abstract
It was the aim of the present study to develop sustained-release matrix tablets by means of injection moulding of ethylcellulose and polyethyleneoxide mixtures and to evaluate the influence of process temperature, matrix composition and viscosity grade of ethylcellulose and polyethyleneoxide on processability and drug release. Formulations consisting of metoprolol tartrate (MPT, concentration: 30%), ethylcellulose (EC) plasticized by dibutylsebacate and polyethyleneoxide (PEO) were extruded and consequently injection moulded into tablets. The influence of process temperature (120 and 140°C), matrix compostition, viscosity grade of ethylcellulose (4, 10, 20, 45 and 100mPa.s) and polyethyleneoxide (7.106, 1. 106 and 1.105 10 Mw) on processability and drug release was determined. Formulations consisting of 70% EC and 30% MPT showed incomplete drug release, whereas drug release was too fast for formulations without EC. Higher PEO concentrations increased drug release. Formulations containing 30% metoprolol, EC and different concentrations of PEO showed first-order release rates with limited burst release. Drug release from directed compressed tablets showed faster drug release rates compared to IM formulations. There was no clear relationship between the molecular weight of EC and drug release. The melting endotherm (113.9°C) of metoprolol tartrate observed in the DSC18 thermogram of the tablets indicated that a solid dispersion was formed which was confirmed by X-RD. X-ray tomography demonstrated a difference in pore structure between tablets processed at 120 and 140°C. It was concluded that injection moulding can be applied successfully to develop sustained release PEO/EC matrix tablets.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
ethylcellulose, injection molding, metoprolol tartrate, melt extrusion, matrix tablet, injection moulding, solid dispersion, sustained release, viscosity grade, polyethylene oxide
journal title
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Drug Dev. Ind. Pharm.
volume
37
issue
2
pages
149 - 159
Web of Science type
Article
Web of Science id
000286522400004
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
1.494 (2011)
JCR rank
183/259 (2011)
JCR quartile
3 (2011)
ISSN
0363-9045
DOI
10.3109/03639045.2010.498426
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
979570
handle
http://hdl.handle.net/1854/LU-979570
date created
2010-06-16 17:13:10
date last changed
2011-07-26 10:28:10
@article{979570,
  abstract     = {It was the aim of the present study to develop sustained-release matrix tablets by means of injection moulding of ethylcellulose and polyethyleneoxide mixtures and to evaluate the influence of process temperature, matrix composition and viscosity grade of ethylcellulose and polyethyleneoxide on processability and drug release. Formulations consisting of metoprolol tartrate (MPT, concentration: 30\%), ethylcellulose (EC) plasticized by dibutylsebacate and polyethyleneoxide (PEO) were extruded and consequently injection moulded into tablets. The influence of process temperature (120 and 140{\textdegree}C), matrix compostition, viscosity grade of ethylcellulose (4, 10, 20, 45 and 100mPa.s) and polyethyleneoxide (7.106, 1. 106 and 1.105 10 Mw) on processability and drug release was determined. Formulations consisting of 70\% EC and 30\% MPT showed incomplete drug release, whereas drug release was too fast for formulations without EC. Higher PEO concentrations increased drug release. Formulations containing 30\% metoprolol, EC and different concentrations of PEO showed first-order release rates with limited burst release.
Drug release from directed compressed tablets showed faster drug release rates compared to IM formulations. There was no clear relationship between the molecular weight of EC and drug release. The melting endotherm (113.9{\textdegree}C) of metoprolol tartrate observed in the DSC18 thermogram of the tablets indicated that a solid dispersion was formed which was confirmed by X-RD. X-ray tomography demonstrated a difference in pore structure between tablets processed at 120 and 140{\textdegree}C. It was concluded that injection moulding can be applied successfully to develop sustained release PEO/EC matrix tablets.},
  author       = {Quinten, Thomas and De Beer, Thomas and Almeida, Ana and Vlassenbroeck, Jelle and Van Hoorebeke, Luc and Remon, Jean Paul},
  issn         = {0363-9045},
  journal      = {DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY},
  keyword      = {ethylcellulose,injection molding,metoprolol tartrate,melt extrusion,matrix tablet,injection moulding,solid dispersion,sustained release,viscosity grade,polyethylene oxide},
  language     = {eng},
  number       = {2},
  pages        = {149--159},
  title        = {Development and evaluation of injection-moulded sustained-release tablets containing ethylcellulose and polyethylene oxide},
  url          = {http://dx.doi.org/10.3109/03639045.2010.498426},
  volume       = {37},
  year         = {2011},
}

Chicago
Quinten, Thomas, Thomas De Beer, Ana Almeida, Jelle Vlassenbroeck, Luc Van Hoorebeke, and Jean Paul Remon. 2011. “Development and Evaluation of Injection-moulded Sustained-release Tablets Containing Ethylcellulose and Polyethylene Oxide.” Drug Development and Industrial Pharmacy 37 (2): 149–159.
APA
Quinten, T., De Beer, T., Almeida, A., Vlassenbroeck, J., Van Hoorebeke, L., & Remon, J. P. (2011). Development and evaluation of injection-moulded sustained-release tablets containing ethylcellulose and polyethylene oxide. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 37(2), 149–159.
Vancouver
1.
Quinten T, De Beer T, Almeida A, Vlassenbroeck J, Van Hoorebeke L, Remon JP. Development and evaluation of injection-moulded sustained-release tablets containing ethylcellulose and polyethylene oxide. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY. 2011;37(2):149–59.
MLA
Quinten, Thomas, Thomas De Beer, Ana Almeida, et al. “Development and Evaluation of Injection-moulded Sustained-release Tablets Containing Ethylcellulose and Polyethylene Oxide.” DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY 37.2 (2011): 149–159. Print.