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Statements

Subject Item
n2:RIV%2F61389013%3A_____%2F15%3A00439661%21RIV15-GA0-61389013
rdf:type
n4:Vysledek skos:Concept
dcterms:description
New drug formulations are sought for poorly water-soluble substances because there is a risk of compromised bioavailability if such substances are administered orally. Such active pharmaceutical ingredients can be reformulated as solid dispersions with suitable water-soluble polymers. In this contribution, formulation of a novel and physically stable dispersion of Simvastatin in poly(2-hydroxypropyl) methacrylamide (pHPMA) is demonstrated. Due to the limited water sorption of pHPMA and a high Tg, the prepared dispersion is more suited for oral administration and storage compared with neat amorphous Simvastatin. Surprisingly, the rate of global reorientation and the internal motion of Simvastatin molecules were enhanced and exhibited dynamical heterogeneities when incorporated into the pHPMA matrix. As revealed by solid-state nuclear magnetic resonance combined with Raman spectroscopy exploiting the fluorescence phenomenon the mobility of the ester and lactone components increased considerably, whereas the naphthalene ring remained rigid. Furthermore, the solid dispersion was found to be nano-heterogeneous with nanometer-sized Simvastatin domains. The presence of these clusters had no impact on the dynamics of the rigid pHPMA chains. Thus, the diffusion of Simvastatin molecules through the glassy pHPMA walls and the subsequent transformation of the clusters into larger crystallites were prevented. No crystallization was detected for more than two years. New drug formulations are sought for poorly water-soluble substances because there is a risk of compromised bioavailability if such substances are administered orally. Such active pharmaceutical ingredients can be reformulated as solid dispersions with suitable water-soluble polymers. In this contribution, formulation of a novel and physically stable dispersion of Simvastatin in poly(2-hydroxypropyl) methacrylamide (pHPMA) is demonstrated. Due to the limited water sorption of pHPMA and a high Tg, the prepared dispersion is more suited for oral administration and storage compared with neat amorphous Simvastatin. Surprisingly, the rate of global reorientation and the internal motion of Simvastatin molecules were enhanced and exhibited dynamical heterogeneities when incorporated into the pHPMA matrix. As revealed by solid-state nuclear magnetic resonance combined with Raman spectroscopy exploiting the fluorescence phenomenon the mobility of the ester and lactone components increased considerably, whereas the naphthalene ring remained rigid. Furthermore, the solid dispersion was found to be nano-heterogeneous with nanometer-sized Simvastatin domains. The presence of these clusters had no impact on the dynamics of the rigid pHPMA chains. Thus, the diffusion of Simvastatin molecules through the glassy pHPMA walls and the subsequent transformation of the clusters into larger crystallites were prevented. No crystallization was detected for more than two years.
dcterms:title
Structural insight into the physical stability of amorphous Simvastatin dispersed in pHPMA: enhanced dynamics and local clustering as evidenced by solid-state NMR and Raman spectroscopy Structural insight into the physical stability of amorphous Simvastatin dispersed in pHPMA: enhanced dynamics and local clustering as evidenced by solid-state NMR and Raman spectroscopy
skos:prefLabel
Structural insight into the physical stability of amorphous Simvastatin dispersed in pHPMA: enhanced dynamics and local clustering as evidenced by solid-state NMR and Raman spectroscopy Structural insight into the physical stability of amorphous Simvastatin dispersed in pHPMA: enhanced dynamics and local clustering as evidenced by solid-state NMR and Raman spectroscopy
skos:notation
RIV/61389013:_____/15:00439661!RIV15-GA0-61389013
n5:aktivita
n16:I n16:P
n5:aktivity
I, P(GA14-03636S), P(LD14010)
n5:cisloPeriodika
2
n5:dodaniDat
n8:2015
n5:domaciTvurceVysledku
n11:6934404 n11:5021197 n11:1926284 n11:2613549
n5:druhVysledku
n15:J
n5:duvernostUdaju
n14:S
n5:entitaPredkladatele
n17:predkladatel
n5:idSjednocenehoVysledku
443
n5:idVysledku
RIV/61389013:_____/15:00439661
n5:jazykVysledku
n6:eng
n5:klicovaSlova
solid dispersions; simvastatin; pharmaceuticals
n5:klicoveSlovo
n12:pharmaceuticals n12:simvastatin n12:solid%20dispersions
n5:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n5:kontrolniKodProRIV
[76EEB562B2D6]
n5:nazevZdroje
International Journal of Pharmaceutics
n5:obor
n13:CD
n5:pocetDomacichTvurcuVysledku
4
n5:pocetTvurcuVysledku
4
n5:projekt
n9:GA14-03636S n9:LD14010
n5:rokUplatneniVysledku
n8:2015
n5:svazekPeriodika
478
n5:tvurceVysledku
Kredatusová, Jana Šturcová, Adriana Urbanová, Martina Brus, Jiří
s:issn
0378-5173
s:numberOfPages
12
n18:doi
10.1016/j.ijpharm.2014.12.007