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Gamal Osman Elhassan*, Yuen Kah Hay, Wong Jia Woei, Jiyauddin Khan, Khalid Omer Alfarouk and Jawed Akhter


Artemisinin (ART) is an oral antimalarial agent with poor aqueous
solubilityand low oral bioavailability. The present study describes the
preparation of artemisinin freeze dried powder using different carriers
(polyvinyl pyrolidone K-25 (PVP K-25), hydroxyl propyl cellulose
(HPC) and dextrin) designed to enhance the solubility of artemisinin.
and hence oral bioavailability of artemisinin, a poorly water-soluble
Drug.,Artemisinin freeze dried powders were prepared by dissolving
different carriers (PVP K-25, HPC and dextrin) in water followed by
the addition of artemisinin at a ratio of 1:4. The resultant products were
evaluated using the solubility and dissolution studies, differential
scanning calorimeter (DSC) and scanning electron microscopic (SEM).
Relative bioavailability studies were conducted in Sprague-Dawely rats using the optimized
formulation against the reference suspension. The in vitro studies showed that the aqueous
solubility of artemisinin has increased significantly for the preparation containing
artemisinin-dextrin at a ratio of 1:4. Further, the effect of incorporation of different cocarriers
(citric acid or mannitol) to artemisinin-dextrin freeze-dried powder at different ratio
was evaluated. There was a significant increase in the solubility and dissolution rate of
artemisinin was obtained with the artemisinin-dextrin-citric acid freeze-dried powder at a
ratio of 1:3:1. In addition, there was statistically significant increase in the oral bioavailabilityof freeze dried artemisinin-dextrin-citric acid mixture compared to reference suspension. The rate and extent of absorption were enhanced by 3.4 folds. In conclusion freeze, dried product of artemisinin was able to increase the solubility, dissolution and therefore, the oral bioavailability.

Keywords: Artemisinin, freeze dried, solubility, dissolution, oral bioavailability.

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