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Enhanced Dissolution and Bioavailability of Etoricoxib in Solid Dispersion Systems: An Investigation into the Role of Carrier Matrix on Stability, In vitro and In vivo Performance

Abstract

Etoricoxib (ECB) is a large, lipophilic molecule that is practically insoluble in water and exhibit an exceedingly slow dissolution rate making it a Class II compound in Bio pharmaceutics Classification System. In the present article, the higher solubility advantage of ECB in solid dispersion is explored. More specifically, solid dispersion of ECB within different water soluble polymers such as polyethylene glycol 6000, polyvinyl pyrrolidone K40 and dextrin were prepared with different drug loadings by using solvent evaporation and fusion method, and the physicochemical properties, stability and in vitro and in vivo performance of the dispersions were evaluated. The pharmacokinetic studies were carried out by using Wistar rats. The solid dispersion prepared with dextrin exhibited improved aqueous solubility. The D60 (percentage drug release after 60 minutes) value for pure drug and optimized formulation (F10; Drug: Dextrin, 1:2) were found to 5.06 ± 3.0 and 16.43 ± 0.18 respectively. The Cmax of pure drug and F10 were found to be 7.2 ± 1.32 μg/ml and 15.5 ± 2.67 μg/ml respectively. These results indicated the improved systemic exposure of ECB following dissolution from solid dispersions

Gopal Venkatesh Shavi, Usha Yogendra Nayak, Ramesh Raghavendra, Shrawan B and Meka Sreenivasa Reddy

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