Show simple item record Szabó Zoltán-István Gál Réka Gáll Zsolt Vancea Szende Rédai Emőke Fülöp Ibolya Sipos Emese Donáth-Nagy Gabriella Noszál Béla Tóth Gergő 2018-02-21T14:27:41Z 2018-02-21T14:27:41Z 2017
dc.identifier 85018407930
dc.identifier.citation pagination=43-52; journalVolume=88; journalIssueNumber=1; journalTitle=JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY;
dc.identifier.uri doi:10.1007/s10847-017-0710-z
dc.description.abstract Rufinamide (RUF) was characterized in terms of cyclodextrin (CD) complexation in order to improve its aqueous solubility. Binary systems of RUF with three CDs—β-cyclodextrin (β-CD), randomly methylated-β-cyclodextrin (RAMEB) and sulfobutylether-β-cyclodextrin (SBE-β-CD)—were characterized with a wide variety of analytical techniques. Liquid state characterization was carried out by complementary techniques such as nuclear magnetic resonance spectroscopy (NMR), capillary electrophoresis (CE), mass spectrometry (MS) and phase solubility studies. The latter revealed that the stability of the complexes decreased in the order of RAMEB > β-CD > SBE-β-CD. AL-type diagrams were obtained in all cases, characteristic of 1:1 stoichiometry, with a maximum of over 15-fold increase in RUF solubility, when complexed with RAMEB. NMR Job plot and MS studies confirmed phase solubility results, regarding the binding stoichiometry. 1H NMR and 2D ROESY investigations revealed the inclusion of the triazole moiety of RUF, confirmed by molecular modeling. Solid state complexation in 1:1 molar ratio was carried out by kneading method and investigated by differential scanning calorimetry (DSC) and infrared spectroscopy (IR). Comparative dissolution studies indicated an over two-fold improvement in dissolution efficacy of the kneaded products, when compared to the pure drug. Results of the present study might pave the way for a drug formulation with improved bioavailability.
dc.relation.ispartof urn:issn:1388-3127
dc.title Cyclodextrin complexation improves aqueous solubility of the antiepileptic drug, rufinamide: solution and solid state characterization of compound-cyclodextrin binary systems
dc.type Journal Article 2018-02-21T14:17:07Z
dc.language.rfc3066 en
dc.identifier.mtmt 3222506
dc.contributor.department SE/GYTK/Gyógyszerészi Kémiai Intézet

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