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In the present research a salt of vincamine, a poorly bioavailable indole alkaloid derived from the leaves of Vinca minor L., was synthesized in the solid state by means of a mechanochemical process employing citric acid as a reagent. The mechanochemical process was adopted as a solvent-free alternative to classical citrate synthetic route that involves the use of solvents. Since the mechanochemical salification is little studied to date and presents the disadvantage of offering a low yield, in this work, the influence of three process and formulation variables on the percentage of vincamine citrate was studied. In particular, the time of mechanical treatment (in planetary mill Fritsch P5) and the amount of citric acid were varied in order to evaluate their effect on the yield of the process, and the introduction of a solid solvent, a common pharmaceutical excipient (sodium carboxymethylcellulose, NaCMC), was considered …
American Chemical Society
Publication date: 
7 Jan 2013

Dritan Hasa, Beatrice Perissutti, Cinzia Cepek, Sunil Bhardwaj, Elvio Carlino, Mario Grassi, Sergio Invernizzi, Dario Voinovich

Biblio References: 
Volume: 10 Issue: 1 Pages: 211-224
Molecular pharmaceutics