• Je něco špatně v tomto záznamu ?

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

M. Naiserová, K. Kubová, J. Vysloužil, S. Pavloková, D. Vetchý, M. Urbanová, J. Brus, J. Vysloužil, P. Kulich,

. 2018 ; 19 (2) : 681-692. [pub] 20171002

Jazyk angličtina Země Spojené státy americké

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc18033687

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.

Citace poskytuje Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc18033687
003      
CZ-PrNML
005      
20200108081148.0
007      
ta
008      
181008s2018 xxu f 000 0|eng||
009      
AR
024    7_
$a 10.1208/s12249-017-0870-6 $2 doi
035    __
$a (PubMed)28971441
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a xxu
100    1_
$a Naiserová, Martina $7 xx0243541 $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 61242, Brno, Czech Republic.
245    10
$a Investigation of Dissolution Behavior HPMC/Eudragit®/Magnesium Aluminometasilicate Oral Matrices Based on NMR Solid-State Spectroscopy and Dynamic Characteristics of Gel Layer / $c M. Naiserová, K. Kubová, J. Vysloužil, S. Pavloková, D. Vetchý, M. Urbanová, J. Brus, J. Vysloužil, P. Kulich,
520    9_
$a 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.
650    _2
$a aplikace orální $7 D000284
650    _2
$a sloučeniny hliníku $x aplikace a dávkování $x chemie $x metabolismus $7 D017607
650    _2
$a léky s prodlouženým účinkem $x aplikace a dávkování $x chemie $x metabolismus $7 D003692
650    _2
$a uvolňování léčiv $7 D065546
650    _2
$a pomocné látky $x chemie $7 D005079
650    _2
$a gely $7 D005782
650    _2
$a sloučeniny hořčíku $x aplikace a dávkování $x chemie $x metabolismus $7 D017616
650    _2
$a magnetická rezonanční spektroskopie $x metody $7 D009682
650    _2
$a velikost částic $7 D010316
650    _2
$a kyseliny polymethakrylové $x aplikace a dávkování $x chemie $x metabolismus $7 D011109
650    _2
$a silikáty $x aplikace a dávkování $x chemie $x metabolismus $7 D017640
650    _2
$a rozpustnost $7 D012995
655    _2
$a časopisecké články $7 D016428
700    1_
$a Kubová, K $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 61242, Brno, Czech Republic. kubovak@vfu.cz.
700    1_
$a Vysloužil, J $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 61242, Brno, Czech Republic.
700    1_
$a Pavloková, Sylvie $7 xx0238422 $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 61242, Brno, Czech Republic.
700    1_
$a Vetchý, D $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 61242, Brno, Czech Republic.
700    1_
$a Urbanová, M $u Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Prague 1, Czech Republic.
700    1_
$a Brus, J $u Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Prague 1, Czech Republic.
700    1_
$a Vysloužil, J $u Department of Biochemistry, Faculty of Science, Masaryk University, Brno, Czech Republic.
700    1_
$a Kulich, P $u Department of Chemistry and Toxicology, Veterinary Research Institute, Brno, Czech Republic.
773    0_
$w MED00008281 $t AAPS PharmSciTech $x 1530-9932 $g Roč. 19, č. 2 (2018), s. 681-692
856    41
$u https://pubmed.ncbi.nlm.nih.gov/28971441 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y a $z 0
990    __
$a 20181008 $b ABA008
991    __
$a 20200108081516 $b ABA008
999    __
$a ok $b bmc $g 1339554 $s 1030681
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2018 $b 19 $c 2 $d 681-692 $e 20171002 $i 1530-9932 $m AAPS PharmSciTech $n AAPS PharmSciTech $x MED00008281
LZP    __
$a Pubmed-20181008

Najít záznam

Citační ukazatele

Možnosti archivace