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.; Kateřina KUBOVÁ ; Jakub VYSLOUŽIL ; Sylvie PAVLOKOVÁ ; David VETCHÝ; M. URBANOVÁ; J. BRUS; Jan VYSLOUŽIL a P. KULICH

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

Označené pro přenos do RIV

Ano

Kód RIV

RIV/00216224:14310/18:00102251

Organizační jednotka

Přírodovědecká fakulta

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://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 = {https://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://doi.org/10.1208/s12249-017-0870-6.

Přehled o publikaci