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

التفاصيل البيبلوغرافية
العنوان: Enhanced Oral Bioavailability of Vinpocetine Through Mechanochemical Salt Formation: Physico-Chemical Characterization and In Vivo Studies
المؤلفون: Valter Sergo, Alois Bonifacio, Mario Grassi, Dritan Hasa, Michele R. Chierotti, Roberto Gobetto, Dario Voinovich, Beatrice Perissutti, Cinzia Cepek, Sergio Invernizzi, Stefano Dall'Acqua
المساهمون: Hasa, Dritan, Voinovich, Dario, Perissutti, Beatrice, Grassi, Mario, Bonifacio, Aloi, Sergo, Valter, Cepek, C., Chierotti, M. R., Gobetto, R., Dall'Acqua, S., Invernizzi, Sergio
المصدر: Pharmaceutical research (Dordr., Online) 28 (2011): 1870–1883. doi:10.1007/s11095-011-0415-8
info:cnr-pdr/source/autori:Dritan Hasa, Dario Voinovich, Beatrice Perissutti, Mario Grassi, Alois Bonifacio, Valter Sergo, Cinzia Cepek, Michele R. Chierotti, Roberto Gobetto, Stefano Dall'Acqua, Sergio Invernizzi/titolo:Enhanced Oral Bioavailability of Vinpocetine Through Mechanochemical Salt Formation: Physico-Chemical Characterization and In Vivo Studies/doi:10.1007%2Fs11095-011-0415-8/rivista:Pharmaceutical research (Dordr., Online)/anno:2011/pagina_da:1870/pagina_a:1883/intervallo_pagine:1870–1883/volume:28
سنة النشر: 2011
مصطلحات موضوعية: Magnetic Resonance Spectroscopy, Chemistry, Pharmaceutical, Kinetics, Inorganic chemistry, Pharmaceutical Science, Salt (chemistry), Administration, Oral, Biological Availability, Spectrum Analysis, Raman, Citric Acid, Rats, Sprague-Dawley, chemistry.chemical_compound, Differential scanning calorimetry, Vinpocetine, X-Ray Diffraction, solvent-free proce, oral absorption, medicine, Animals, mechanochemical reaction/activation, Pharmacology (medical), Solubility, Particle Size, Vinca Alkaloids, Pharmacology, chemistry.chemical_classification, solvent-free process, Calorimetry, Differential Scanning, physico-chemical characterization, Photoelectron Spectroscopy, Organic Chemistry, Povidone, vinpocetine citrate, Bioavailability, Rats, Solvent, chemistry, Molecular Medicine, Citric acid, Biotechnology, Nuclear chemistry, medicine.drug
الوصف: The 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. Purpose 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.
وصف الملف: application/msword; STAMPA
اللغة: English
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe6ec907402613bb7230315763fb540c
http://hdl.handle.net/2318/91385
حقوق: OPEN
رقم الأكسشن: edsair.doi.dedup.....fe6ec907402613bb7230315763fb540c
قاعدة البيانات: OpenAIRE