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.
|