Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium
Aluminometasilicate Oral Matrices Based on NMR Solid-State
Spectroscopy and Dynamic Characteristics of Gel Layer

J 2018

Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer

NAISEROVÁ, M., Kateřina KUBOVÁ, Jakub VYSLOUŽIL, Sylvie PAVLOKOVÁ, David VETCHÝ et. al.

Základní údaje

Originální název

Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer

Autoři

NAISEROVÁ, M. (203 Česká republika), Kateřina KUBOVÁ (203 Česká republika), Jakub VYSLOUŽIL (203 Česká republika, domácí), Sylvie PAVLOKOVÁ (203 Česká republika), David VETCHÝ (203 Česká republika), M. URBANOVÁ (203 Česká republika), J. BRUS (203 Česká republika), Jan VYSLOUŽIL (203 Česká republika, domácí) a P. KULICH (203 Česká republika)

Vydání

AAPS PHARMSCITECH, NEW YORK, SPRINGER, 2018, 1530-9932

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Odkazy

URL

Impakt faktor

Impact factor: 2.608

Kód RIV

RIV/00216224:14310/18:00102251

Organizační jednotka

Přírodovědecká fakulta

DOI

http://dx.doi.org/10.1208/s12249-017-0870-6

UT WoS

000423720400017

Klíčová slova anglicky

matrix tablets HPMC Eudragit® NE30D Neusilin® US2 gel layer Levetiracetam Burst effect thermal treatment multivariate data analysis

Změněno: 23. 4. 2024 10:58, Mgr. Michal Petr

Anotace

V originále

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.

Citovat

NAISEROVÁ, M., Kateřina KUBOVÁ, Jakub VYSLOUŽIL, Sylvie PAVLOKOVÁ, David VETCHÝ, M. URBANOVÁ, J. BRUS, Jan VYSLOUŽIL a P. KULICH. Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer. AAPS PHARMSCITECH. NEW YORK: SPRINGER, 2018, roč. 19, č. 2, s. 681-692. ISSN 1530-9932. Dostupné z: https://dx.doi.org/10.1208/s12249-017-0870-6.

@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 a 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, roč.~19, č.~2, s.~681-692. ISSN~1530-9932. Dostupné z: https://dx.doi.org/10.1208/s12249-017-0870-6.

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