Powder Technology, Vol.347, 85-92, 2019
Precompression of dry vegetal bioactive agents to optimize density and compactness: Case of Peschiera fuchsiaefolia powdered materials
Natural products of vegetable origin, some of them manufactured as extracts, are largely used for treatment of several pathologies. This report describes an extract of Peschiera fuchsiaefolia (Pf) developed for treatment of malaria. This Pf extract contains low soluble indolic alkaloids. To improve its solubility, the Pf extract was complexed by spray-drying coprocessing with carboxymethylcellulose (CMC), obtaining the CMC-Pf complex. The ionic complexation of Pf cationic alkaloids with the highly soluble anionic CMC improved the Pf solubility favoring its bioavailability and absorption. The spray-dried powder was light, fluffy and voluminous. These features may constitute a major difficulty during the compression of tablets at micro-pilot or at industrial scale with punches for multi-compression. The aim of this report was to investigate the precompression conditions of such low-density powdered materials (i.e. CMC-Pf complex), prior to further processing, for final tablet compression. A moderate force exerted on the powder (25 Kg/g of sample) provoked the removal of air trapped in Pf granules by breaking down spheroidal morphology. Also, the powder volume was reduced favoring the fill-up the powder mixture in the die of the automatic press for further tablet compression. This adjustment provided a good compactness and uniform distribution of powders. The method seems appropriate for various bioactive agents. Except the morphology, no significant changes of structural characteristics (functional group, solubility, stability), neither of the biological activity of CMC-Pf, were found. Furthermore, no significant differences in terms of release kinetic profiles from tablets formulated with uncompressed or with precompressed CMC-Pf, were detected. This precompression method is not expensive, and is simple, fast and easy to apply. It is worth to mention that no extra ingredients were added in the formulation. (C) 2019 Elsevier B.V. All rights reserved.
Keywords:Peschiera fuchsiaefolia compactness;Alkaloid extract densification;Fluffy powder volume reduction;Drug release kinetics;Powder precompression;Tablet manufacturing process