The 2nd International Conference on Drug Discovery & Therapy: Dubai, February 1 - 4, 2010


Poster Presenter

Enhanced oral bioavailability of etodolac by self-emulsifying systems
Nahla salah barakat
Saudi Arabia

This study focuses on the enhancement of the dissolution and oral absorption of poorly water-soluble etodolac. Self-emulsifying drug delivery system (SEDDS) composed of oil, surfactant, and co surfactant for oral administration was formulated. The SEDDS formulations were optimized by evaluating their ability to self-emulsifying when introduced to an aqueous medium under gentle agitation, and by determination of particle size of the resulting emulsion. Optimized formulation of SEDDS was selected for bioavailability assessment in rabbits. Also, the anti-inflammatory effect of SEDDS formulation was determined in rats, compared with powder drug and etodolac suspension in water (50 mg kg-1).

The peak plasma concentration of 16.4 1.07 g mL-1 appeared after 1.3 0.2 h, whereas with powder drug and etodolac suspension the values were 7.5 0.5 and 10.6 0.7 g mL-1 appeared at 4.2 0.4 and 2.4 0.2 h, respectively. The AUC 0-8 of the etodolac SEDDS formulation was 2.3 times as that of the pure drug and 2.1 times as much as that of the suspension form. There was no significant change in the elimination rate constant and the elimination half-life. Thus, the extent of oral absorption is improved significantly from SEDDS formulation. The anti-inflammatory activity of SEDDS formulation was compared with etodolac suspended in water at a dose 20 mg kg-1, by carrageenan induced rat paw oedema model. SEDDS formulation, exhibits 25% increase in paw thickness while upon oral administration of etodolac suspension, the increase in paw thickness reached 39% after 4 h using the same dose of the drug. The result indicating the utility of dispersed lipid-based formulation for the oral delivery of etodolac, and potentially other lipophilic drugs.













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