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

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F19%3A43877714" target="_blank" >RIV/62157124:16370/19:43877714 - isvavai.cz</a>

Výsledek na webu

<a href="https://www.hindawi.com/journals/bmri/2019/8043415/" target="_blank" >https://www.hindawi.com/journals/bmri/2019/8043415/</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1155/2019/8043415" target="_blank" >10.1155/2019/8043415</a>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

The aim of the present study was to investigate the suitability of insoluble Eudragit (R) 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 (R). Contrary, higher rigidity of formed gel layer was observed using combination of HPMC and Eudragit (R). Not only the type and concentration of Eudragit (R), 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 (R) 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%).

Název v anglickém jazyce

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

Popis výsledku anglicky

The aim of the present study was to investigate the suitability of insoluble Eudragit (R) 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 (R). Contrary, higher rigidity of formed gel layer was observed using combination of HPMC and Eudragit (R). Not only the type and concentration of Eudragit (R), 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 (R) 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%).

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2019

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Biomed Research International

ISSN

2314-6133

e-ISSN

—

Svazek periodika

2019

Číslo periodika v rámci svazku

ID8043415

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

13

Strana od-do

—

Kód UT WoS článku

000461616600001

EID výsledku v databázi Scopus

2-s2.0-85063271286