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Modeling drug release from hot-melt extruded mini-matrices with constant and non-constant diffusivities

Ellen Verhoeven UGent, F Siepmann, Thomas De Beer UGent, Denis Van Loo UGent, G. Van den Mooter, Jean Paul Remon UGent, J Siepmann and Chris Vervaet UGent (2009) EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS. 73(2). p.292-301
abstract
Non-disintegrating microcrystalline cellulose pellets (MCC) and disintegrating starch-based pellets were evaluated as new vaginal drug delivery forms and compared with a powder formulation. Pellets and powder were packed in a HPMC or hard gelatine capsule and vaginally administered to five series of five healthy volunteers. Distribution and retention of the multi-particulate formulation was monitored by colposcopy and swabbing. Capsule disintegration in the vagina was slow. MCC pellets clustered around the fornix 3 h after administration, and after 24 h only a few pellets were detected in the vaginal cavity. In contrast, starch-based pellets already started to disintegrate 6 h after administration, resulting in a complete coverage of the vaginal mucosa after 24 h in 8 out of 10 volunteers. The powder formulation had a better distribution after 6 h, although after 24 h almost no powder remained in the vagina. These results were confirmed by swabbing to determine the amount of riboflavin sodium phosphate (used as marker) distributed in the different vaginal regions.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
PHYSICOCHEMICAL PROPERTIES, LIPIDIC IMPLANTS, DELIVERY SYSTEMS, PROTEIN RELEASE, XANTHAN GUM, EXTRUSION, TABLETS, PELLETS, MECHANISMS, BIOAVAILABILITY
journal title
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Eur. J. Pharm. Biopharm.
volume
73
issue
2
pages
10 pages
publisher
Elsevier Science
place of publication
AMSTERDAM
Web of Science type
Article
Web of Science id
000271153300011
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
3.151 (2009)
JCR rank
70/236 (2009)
JCR quartile
2 (2009)
ISSN
0939-6411
DOI
10.1016/j.ejpb.2009.06.010
language
English
UGent publication?
yes
classification
A1
copyright statement
I don't know the status of the copyright for this publication
id
790723
handle
http://hdl.handle.net/1854/LU-790723
date created
2009-11-27 16:13:48
date last changed
2009-12-10 10:28:44
@article{790723,
  abstract     = {Non-disintegrating microcrystalline cellulose pellets (MCC) and disintegrating starch-based pellets were evaluated as new vaginal drug delivery forms and compared with a powder formulation. Pellets and powder were packed in a HPMC or hard gelatine capsule and vaginally administered to five series of five healthy volunteers. Distribution and retention of the multi-particulate formulation was monitored by colposcopy and swabbing. Capsule disintegration in the vagina was slow. MCC pellets clustered around the fornix 3 h after administration, and after 24 h only a few pellets were detected in the vaginal cavity. In contrast, starch-based pellets already started to disintegrate 6 h after administration, resulting in a complete coverage of the vaginal mucosa after 24 h in 8 out of 10 volunteers. The powder formulation had a better distribution after 6 h, although after 24 h almost no powder remained in the vagina. These results were confirmed by swabbing to determine the amount of riboflavin sodium phosphate (used as marker) distributed in the different vaginal regions.},
  author       = {Verhoeven, Ellen and Siepmann, F and De Beer, Thomas and Van Loo, Denis and Van den Mooter, G. and Remon, Jean Paul and Siepmann, J and Vervaet, Chris},
  issn         = {0939-6411},
  journal      = {EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS},
  keyword      = {PHYSICOCHEMICAL PROPERTIES,LIPIDIC IMPLANTS,DELIVERY SYSTEMS,PROTEIN RELEASE,XANTHAN GUM,EXTRUSION,TABLETS,PELLETS,MECHANISMS,BIOAVAILABILITY},
  language     = {eng},
  number       = {2},
  pages        = {292--301},
  publisher    = {Elsevier Science},
  title        = {Modeling drug release from hot-melt extruded mini-matrices with constant and non-constant diffusivities},
  url          = {http://dx.doi.org/10.1016/j.ejpb.2009.06.010},
  volume       = {73},
  year         = {2009},
}

Chicago
Verhoeven, Ellen, F Siepmann, Thomas De Beer, Denis Van Loo, G. Van den Mooter, Jean Paul Remon, J Siepmann, and Chris Vervaet. 2009. “Modeling Drug Release from Hot-melt Extruded Mini-matrices with Constant and Non-constant Diffusivities.” European Journal of Pharmaceutics and Biopharmaceutics 73 (2): 292–301.
APA
Verhoeven, E., Siepmann, F., De Beer, T., Van Loo, D., Van den Mooter, G., Remon, J. P., Siepmann, J., et al. (2009). Modeling drug release from hot-melt extruded mini-matrices with constant and non-constant diffusivities. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 73(2), 292–301.
Vancouver
1.
Verhoeven E, Siepmann F, De Beer T, Van Loo D, Van den Mooter G, Remon JP, et al. Modeling drug release from hot-melt extruded mini-matrices with constant and non-constant diffusivities. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS. AMSTERDAM: Elsevier Science; 2009;73(2):292–301.
MLA
Verhoeven, Ellen, F Siepmann, Thomas De Beer, et al. “Modeling Drug Release from Hot-melt Extruded Mini-matrices with Constant and Non-constant Diffusivities.” EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS 73.2 (2009): 292–301. Print.