Enhanced Oral Bioavailability of Vinpocetine Through Mechanochemical Salt Formation: Physico-Chemical Characterization and In Vivo Studies

dc.cclicenceCC-BY-NCen
dc.contributor.authorHasa, Dritanen
dc.contributor.authorVoinovich, Darioen
dc.contributor.authorPerissutti, Beatriceen
dc.contributor.authorGrassi, Marioen
dc.contributor.authorBonifacio, Aloisen
dc.contributor.authorSergo, Valteren
dc.contributor.authorCepek, Cinziaen
dc.contributor.authorChierotti, Michele R.en
dc.contributor.authorGobetto, Robertoen
dc.contributor.authorDall’Acqua, Stefanoen
dc.contributor.authorInvernizzi, Sergioen
dc.date.accessioned2017-04-28T10:12:24Z
dc.date.available2017-04-28T10:12:24Z
dc.date.issued2011-03-19
dc.descriptionThe file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.en
dc.description.abstractPurpose Enhancing oral bioavailability of vinpocetine by forming its amorphous citrate salt through a solvent-free mechanochemical process, in presence of micronised crospovidone and citric acid. Methods The impact of formulation and process variables (amount of polymer and citric acid, and milling time) on vinpocetine solubilization kinetics from the coground was studied through an experimental design. The best performing samples were characterized by employing a multidisciplinary approach, involving Differential scanning calorimetry, X-ray diffraction, Raman imaging/spectroscopy, X-ray photoelectron spectroscopy, solid-state NMR spectroscopy, porosimetry and in vivo studies on rats to ascertain the salt formation, their solidstate characteristics and oral bioavailability in comparison to vinpocetine citrate salt (Oxopocetine®). Results The analyses attested that the mechanochemical process is a viable way to produce in absence of solvents vinpocetine citrate salt in an amorphous state. Conclusion From the in vivo studies on rats the obtained salt was four times more bioavailable than its physical mixture and bioequivalent to the commercial salt produced by conventional synthetic process implying the use of solvent.en
dc.funderN/Aen
dc.identifier.citationHasa, D. et al. (2011) Enhanced Oral Bioavailability of Vinpocetine Through Mechanochemical Salt Formation: Physico-Chemical Characterization and In Vivo Studies. Pharmaceutical Research, 28 (8), pp. 1870-1883en
dc.identifier.doihttps://doi.org/10.1007/s11095-011-0415-8
dc.identifier.urihttp://hdl.handle.net/2086/14119
dc.peerreviewedYesen
dc.projectidN/Aen
dc.publisherSpringeren
dc.researchinstituteLeicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)en
dc.subjectmechanochemical reaction/activationen
dc.subjectoral absorptionen
dc.subjectphysico-chemical characterizationen
dc.subjectsolvent-free processen
dc.subjectvinpocetine citrateen
dc.titleEnhanced Oral Bioavailability of Vinpocetine Through Mechanochemical Salt Formation: Physico-Chemical Characterization and In Vivo Studiesen
dc.typeArticleen

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