• Je něco špatně v tomto záznamu ?

Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems

E. Mašková, M. Naiserová, K. Kubová, J. Mašek, S. Pavloková, M. Urbanová, J. Brus, J. Vysloužil, D. Vetchý,

. 2019 ; 2019 (-) : 8043415. [pub] 20190305

Jazyk angličtina Země Spojené státy americké

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc19034657

The aim of the present study was to investigate the suitability of insoluble Eudragit® water dispersions (NE, NM, RL, and RS) for direct high-shear granulation of very soluble levetiracetam in order to decrease its burst effect from HPMC K100M matrices. The process characteristics, ss-NMR analysis, in vitro dissolution behavior, drug release mechanism and kinetics, texture profile analysis of the gel layer, and PCA analysis were explored. An application of water dispersions directly on levetiracetam was feasible only in a multistep process. All prepared formulations exhibited a 12-hour sustained release profile characterized by a reduced burst effect in a concentration-dependent manner. No effect on swelling extent of HPMC K100M was observed in the presence of Eudragit®. Contrary, higher rigidity of formed gel layer was observed using combination of HPMC and Eudragit®. Not only the type and concentration of Eudragit®, but also the presence of the surfactant in water dispersions played a key role in the dissolution characteristics. The dissolution profile close to zero-order kinetic was achieved from the sample containing levetiracetam directly granulated by the water dispersion of Eudragit® NE (5% of solid polymer per tablet) with a relatively high amount of surfactant nonoxynol 100 (1.5%). The initial burst release of drug was reduced to 8.04% in 30 min (a 64.2% decrease) while the total amount of the released drug was retained (97.02%).

Citace poskytuje Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc19034657
003      
CZ-PrNML
005      
20200108081053.0
007      
ta
008      
191007s2019 xxu f 000 0|eng||
009      
AR
024    7_
$a 10.1155/2019/8043415 $2 doi
035    __
$a (PubMed)30949510
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a xxu
100    1_
$a Mašková, Eliška $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic. Department of Pharmacology and Immunotherapy, Veterinary Research Institute, Brno, Czech Republic.
245    10
$a Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems / $c E. Mašková, M. Naiserová, K. Kubová, J. Mašek, S. Pavloková, M. Urbanová, J. Brus, J. Vysloužil, D. Vetchý,
520    9_
$a The aim of the present study was to investigate the suitability of insoluble Eudragit® water dispersions (NE, NM, RL, and RS) for direct high-shear granulation of very soluble levetiracetam in order to decrease its burst effect from HPMC K100M matrices. The process characteristics, ss-NMR analysis, in vitro dissolution behavior, drug release mechanism and kinetics, texture profile analysis of the gel layer, and PCA analysis were explored. An application of water dispersions directly on levetiracetam was feasible only in a multistep process. All prepared formulations exhibited a 12-hour sustained release profile characterized by a reduced burst effect in a concentration-dependent manner. No effect on swelling extent of HPMC K100M was observed in the presence of Eudragit®. Contrary, higher rigidity of formed gel layer was observed using combination of HPMC and Eudragit®. Not only the type and concentration of Eudragit®, but also the presence of the surfactant in water dispersions played a key role in the dissolution characteristics. The dissolution profile close to zero-order kinetic was achieved from the sample containing levetiracetam directly granulated by the water dispersion of Eudragit® NE (5% of solid polymer per tablet) with a relatively high amount of surfactant nonoxynol 100 (1.5%). The initial burst release of drug was reduced to 8.04% in 30 min (a 64.2% decrease) while the total amount of the released drug was retained (97.02%).
650    _2
$a léky s prodlouženým účinkem $x farmakokinetika $x farmakologie $7 D003692
650    _2
$a uvolňování léčiv $7 D065546
650    12
$a deriváty hypromelózy $x chemie $x farmakokinetika $x farmakologie $7 D065347
650    _2
$a laktosa $x analogy a deriváty $x chemie $x farmakokinetika $x farmakologie $7 D007785
650    _2
$a methylcelulosa $x analogy a deriváty $x chemie $x farmakokinetika $x farmakologie $7 D008747
650    12
$a nonoxynol $x chemie $x farmakokinetika $x farmakologie $7 D017137
650    12
$a kyseliny polymethakrylové $x chemie $x farmakokinetika $x farmakologie $7 D011109
655    _2
$a časopisecké články $7 D016428
700    1_
$a Naiserová, Martina $7 xx0243541 $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic.
700    1_
$a Kubová, Kateřina $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic.
700    1_
$a Mašek, Josef $u Department of Pharmacology and Immunotherapy, Veterinary Research Institute, Brno, Czech Republic.
700    1_
$a Pavloková, Sylvie $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic.
700    1_
$a Urbanová, Martina $u Institute of Macromolecular Chemistry, Czech Academy of Sciences, Praha, Czech Republic.
700    1_
$a Brus, Jiří $u Institute of Macromolecular Chemistry, Czech Academy of Sciences, Praha, Czech Republic.
700    1_
$a Vysloužil, Jakub $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic.
700    1_
$a Vetchý, David $u Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic.
773    0_
$w MED00182164 $t BioMed research international $x 2314-6141 $g Roč. 2019, č. - (2019), s. 8043415
856    41
$u https://pubmed.ncbi.nlm.nih.gov/30949510 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y a $z 0
990    __
$a 20191007 $b ABA008
991    __
$a 20200108081422 $b ABA008
999    __
$a ok $b bmc $g 1451317 $s 1073207
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2019 $b 2019 $c - $d 8043415 $e 20190305 $i 2314-6141 $m BioMed research international $n Biomed Res Int $x MED00182164
LZP    __
$a Pubmed-20191007

Najít záznam

Citační ukazatele

    Možnosti archivace