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Mechanochemically induced disordered structures of vincamine: the different mediation of two cross-linked polymers
Hasa, Dritan (Avtor), Perissutti, Beatrice (Avtor), Chierotti, Michele Remo (Avtor), Gobetto, Roberto (Avtor), Grabnar, Iztok (Avtor), Bonifacio, Alois (Avtor), Dall'Acqua, Stefano (Avtor), Invernizzi, Sergio (Avtor), Voinovich, Dario (Avtor)

URLURL - Predstavitvena datoteka, za dostop obiščite http://www.sciencedirect.com/science/article/pii/S0378517312006229 Povezava se odpre v novem oknu

Izvleček
The aims of this research were to prepare highly bioavailable binary cogrounds(vincamine-AcDiSolŽ or PVP-Cl) by means of a mechanochemical process and to study the mediation of each polymer in the induction of physical transformations of the drug. From a set of fifteen cogrounds for each cross linked polymer, two samples were selected in each group on the basis of the AUC of in vitro dissolution profiles with the help of a statistical comparison. The chosen samples were analysed by means of TEM, XRPD, Raman-spectroscopy/imaging, SSNMR, also including the study of 1H spin-latticerelaxation times. The research encompassed in vivo oral absorption studies in rats, pharmacokinetic analysis and physical stability studies during 1 year. An intimate drug-polymer mixing was found in the coground samples with domain average dimensions smaller than 100 Å; this reflected in a remarkable enhancement of the in vitro and in vivo bioavailability. Different disordered states were detected in the coground samples as a function of cogrinding time and the type and amount of polymer used. Though both crosslinked polymers produced a remarkable enhancement of the oral bioavailability, coground systems based on AcDiSol are preferable interms of pharmacokinetic performance and physical stability.

Jezik:Angleški jezik
Ključne besede:vincamine, mechanochemical activation, cross-linked polymers, physico-chemical characterisation, bioavailability, physical stability
Vrsta gradiva:Delo ni kategorizirano (r6)
Tipologija:1.01 - Izvirni znanstveni članek
Organizacija:FFA - Fakulteta za farmacijo
Leto izida:2012
Št. strani:str. 41-57
Številčenje:Vol. 436, no. 1-2
UDK:543.9:615
ISSN pri članku:0378-5173
DOI:10.1016/j.ijpharm.2012.06.024 Povezava se odpre v novem oknu
COBISS.SI-ID:3273329 Povezava se odpre v novem oknu
Število ogledov:549
Število prenosov:294
Metapodatki:XML RDF-CHPDL DC-XML DC-RDF
 
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Naslov:International journal of pharmaceutics
Skrajšan naslov:Int. j. pharm.
Založnik:Elsevier/North-Holland
ISSN:0378-5173
COBISS.SI-ID:3087631 Povezava se odpre v novem oknu

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