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@article{1406170,
author = {Naiserová, M. and Kubová, Kateřina and Vysloužil, Jakub and Pavloková, Sylvie and Vetchý, David and Urbanová, M. and Brus, J. and Vysloužil, Jan and Kulich, P.},
article_location = {NEW YORK},
article_number = {2},
doi = {http://dx.doi.org/10.1208/s12249-017-0870-6},
keywords = {matrix tablets HPMC Eudragit® NE30D Neusilin® US2 gel layer Levetiracetam Burst effect thermal treatment multivariate data analysis},
language = {eng},
issn = {1530-9932},
journal = {AAPS PHARMSCITECH},
title = {Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer},
url = {http://dx.doi.org/10.1208/s12249-017-0870-6},
volume = {19},
year = {2018}
}
TY - JOUR
ID - 1406170
AU - Naiserová, M. - Kubová, Kateřina - Vysloužil, Jakub - Pavloková, Sylvie - Vetchý, David - Urbanová, M. - Brus, J. - Vysloužil, Jan - Kulich, P.
PY - 2018
TI - Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer
JF - AAPS PHARMSCITECH
VL - 19
IS - 2
SP - 681-692
EP - 681-692
PB - SPRINGER
SN - 15309932
KW - matrix tablets HPMC Eudragit® NE30D Neusilin® US2 gel layer Levetiracetam Burst effect thermal treatment multivariate data analysis
UR - http://dx.doi.org/10.1208/s12249-017-0870-6
N2 - Burst drug release is often considered a negative phenomenon resulting in unexpected toxicity or tissue irritation. Optimal release of a highly soluble active pharmaceutical ingredient (API) from hypromellose (HPMC) matrices is technologically impossible; therefore, a combination of polymers is required for burst effect reduction. Promising variant could be seen in combination of HPMC and insoluble Eudragits® as water dispersions. These can be applied only on API/insoluble filler mixture as over-wetting prevention. The main hurdle is a limited water absorption capacity (WAC) of filler. Therefore, the object of this study was to investigate the dissolution behavior of levetiracetam from HPMC/Eudragit®NE matrices using magnesium aluminometasilicate (Neusilin® US2) as filler with excellent WAC. Part of this study was also to assess influence of thermal treatment on quality parameters of matrices. The use of Neusilin® allowed the application of Eudragit® dispersion to API/Neusilin® mixture in one step during high-shear wet granulation. HPMC was added extragranularly. Obtained matrices were investigated for qualitative characteristics, NMR solid-state spectroscopy (ssNMR), gel layer dynamic parameters, SEM, and principal component analysis (PCA). Decrease in burst effect (max. of 33.6%) and dissolution rate, increase in fitting to zero-order kinetics, and paradoxical reduction in gel layer thickness were observed with rising Eudragit® NE concentration. The explanation was done by ssNMR, which clearly showed a significant reduction of the API particle size (150–500 nm) in granules as effect of surfactant present in dispersion in dependence on Eudragit®NE amount. This change in API particle size resulted in a significantly larger interface between these two entities. Based on ANOVA and PCA, thermal treatment was not revealed as a useful procedure for this system.
ER -
NAISEROVÁ, M., Kateřina KUBOVÁ, Jakub VYSLOUŽIL, Sylvie PAVLOKOVÁ, David VETCHÝ, M. URBANOVÁ, J. BRUS, Jan VYSLOUŽIL and P. KULICH. Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer. \textit{AAPS PHARMSCITECH}. NEW YORK: SPRINGER, 2018, vol.~19, No~2, p.~681-692. ISSN~1530-9932. Available from: https://dx.doi.org/10.1208/s12249-017-0870-6.
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