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Polymer leaching from film coating: Effects on the coating transport properties.

Marucci, Mariagrazia LU ; Ragnarsson, Gert; von Corswant, Christian; Welinder, Anette; Jarke, Annica; Iselau, Frida and Axelsson, Anders LU (2011) In International Journal of Pharmaceutics 411. p.43-48
Abstract
The release mechanism of metoprolol succinate pellets coated with a blend of a water-insoluble polymer, ethyl cellulose (EC), and a water-soluble polymer, hydroxypropyl cellulose (HPC) is mechanistically explained. The kinetics of drug release and HPC leaching were followed for drug doses. The coating was initially not permeable to the drug, and release started only after a critical amount of the HPC had been leached out. Drug release occurred mainly through pores created in the coating by the HPC dissolution. Single-pellet release experiments were also performed. The coating thickness and size of each pellet were measured. In order to quantitatively characterize the transport properties of the coating of the individual pellets, and to... (More)
The release mechanism of metoprolol succinate pellets coated with a blend of a water-insoluble polymer, ethyl cellulose (EC), and a water-soluble polymer, hydroxypropyl cellulose (HPC) is mechanistically explained. The kinetics of drug release and HPC leaching were followed for drug doses. The coating was initially not permeable to the drug, and release started only after a critical amount of the HPC had been leached out. Drug release occurred mainly through pores created in the coating by the HPC dissolution. Single-pellet release experiments were also performed. The coating thickness and size of each pellet were measured. In order to quantitatively characterize the transport properties of the coating of the individual pellets, and to determine the effective diffusion coefficient (D(e)) of the drug in the coating, a mechanistic model was used to fit the single-pellet release data. It was found that D(e) increased with time due to an increase in the amount of HPC leached. It was also found that D(e) was dependent on the coating thickness, and increased more slowly with a thicker coating. This agreed well with the finding that the HPC leaching rate decreased with increasing film thickness. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
International Journal of Pharmaceutics
volume
411
pages
43 - 48
publisher
Elsevier
external identifiers
  • wos:000291507400006
  • pmid:21421031
  • scopus:79955961861
ISSN
1873-3476
DOI
10.1016/j.ijpharm.2011.03.022
language
English
LU publication?
yes
id
ddbb826c-132d-4ef9-9335-7bfe45ca51bf (old id 1883691)
date added to LUP
2011-04-20 08:43:07
date last changed
2017-09-24 03:14:39
@article{ddbb826c-132d-4ef9-9335-7bfe45ca51bf,
  abstract     = {The release mechanism of metoprolol succinate pellets coated with a blend of a water-insoluble polymer, ethyl cellulose (EC), and a water-soluble polymer, hydroxypropyl cellulose (HPC) is mechanistically explained. The kinetics of drug release and HPC leaching were followed for drug doses. The coating was initially not permeable to the drug, and release started only after a critical amount of the HPC had been leached out. Drug release occurred mainly through pores created in the coating by the HPC dissolution. Single-pellet release experiments were also performed. The coating thickness and size of each pellet were measured. In order to quantitatively characterize the transport properties of the coating of the individual pellets, and to determine the effective diffusion coefficient (D(e)) of the drug in the coating, a mechanistic model was used to fit the single-pellet release data. It was found that D(e) increased with time due to an increase in the amount of HPC leached. It was also found that D(e) was dependent on the coating thickness, and increased more slowly with a thicker coating. This agreed well with the finding that the HPC leaching rate decreased with increasing film thickness.},
  author       = {Marucci, Mariagrazia and Ragnarsson, Gert and von Corswant, Christian and Welinder, Anette and Jarke, Annica and Iselau, Frida and Axelsson, Anders},
  issn         = {1873-3476},
  language     = {eng},
  pages        = {43--48},
  publisher    = {Elsevier},
  series       = {International Journal of Pharmaceutics},
  title        = {Polymer leaching from film coating: Effects on the coating transport properties.},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2011.03.022},
  volume       = {411},
  year         = {2011},
}