PREPARATION AND EVALUATION OF ARTEMISININ PREPARATIONS WITH ENHANCED BIOA V AILABILITY
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Date
2010-02
Authors
EL HASSAN, GAMAL OSMAN
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Abstract
The present study was conducted to investigate the effect of different polymeric
carriers to enhance the solubility and hence oral bioavailability of artemisinin, a
poorly water-soluble drug, through different techniques, namely, spray drying, solid
dispersion and freeze drying. The phase solubility of artemisinin-PVP K-25 spray
dried powder and artemisinin solid dispersion with Gelucire 44/14 or PEGs (1500,
4000 and 6000), showed that these preparations were not capable of increasing the
solubility of artemisinin significantly.
However, the artemisinin freeze dried with PVP K-25, PEG 6000 and dextrin using
different solvents were successfully prepared at different ratios. In vitro studies
showed that the aqueous solubility of artemisinin was increased significantly for the
preparation containing artemisinin-dextrin at a ratio of 1: 4. The incorporation of
different co-carriers (citric acid or mannitol) into artemisinin-dextrin at different
ratios was evaluated. A significant increase in the solubility and dissolution rate of
artemisinin was obtained for the preparation of artemisinin-dextrin-citric acid at a
ratio of 1: 3: L
A liquid chromatography tandem mass spectrometry method was successfully
developed for determining plasma concentration of artemisinin. The method is
simple, sensitive and specific and it applied to evaluate the bioavailability of the
freeze dried product of artemisinin-dextrin-citric acid (at a ratio of 1: 3: 1 )o
In vivo study conducted usmg Sprague-Dawley rats revealed that the above
preparation was capable of increasing the oral bioavailability of artemisinin by
approximately 3A fold compared to the aqueous suspension of pure artemisinino
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Keywords
PREPARATION AND EVALUATION OF ARTEMISININ PREPARATIONS