Formation of ultrafine deferasirox particles via rapid expansion of supercritical solution (RESS process) using Taguchi approach

International Journal of Pharmaceutics
Iman Asghari, Feridun Esmaeilzadeh

Abstract

The poor water solubility of many drugs is a challenge in pharmaceutical research. Recently, there have been great interests in finding environmentally friendly methods producing fine particles of pharmaceutical products for applications in pharmaceutical engineering. A promising method to improve the bioavailability of pharmaceutical agents is the rapid expansion of supercritical solutions. Deferasirox (DFS), a tridentate chelator, requires two molecules for iron (III) coordination. The bioavailability (the percentage of the drug absorbed compared to its initial dosage) is limited by this insolubility. The effect of four different RESS parameters including, extraction temperature (308-318K), extraction pressure (140-200 bar), effective nozzle diameter (500-1200 μm), with and without cosolvents were investigated on the size and morphology of the precipitated particles of deferasirox based on Taguchi design. The results show great reduction in the size of the precipitated particles of deferasirox (50 nm-5 μm) via RESS process compared with the original particles of deferasirox (5-500 μm).

References

Mar 1, 1993·Journal of Biopharmaceutical Statistics·K E Peace, G G Koch
Jun 7, 2000·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·C Leuner, J Dressman
Jun 26, 2004·Current Drug Targets·Rubiana M Mainardes, Luciano P Silva
Sep 2, 2004·Nature Reviews. Drug Discovery·Barrett E Rabinow

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Citations

Oct 10, 2013·BioMed Research International·Rakesh K Tekade, Mahavir B Chougule
Sep 17, 2021·International Journal of Pharmaceutics·Rahul KumarPranava Chaudhari

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