ENHANCED RECTAL ABSORPTION OF ITAZIGREL FORMULATED WITH POLYSORBATE-80 MICELLE VEHICLE IN RAT - ROLE OF CO-ADMINISTERED ESTERASE

We investigated the effect of esterase on rectal absorption in the rat of itazigrel using polysorbate 80 (PS-80) micelle as a vehicle to ove rcome the poor aqueous solubility of itazigrel. The itazigrel formulat ion prepared with PS-80 increased the absorption compared with a 0.25% carmellose sodium suspension, probably by supplying the itazigrel sol ute to keep a high concentration at the epithelial surface. When ester ase was co-administered with the formulations containing PS-80, the ab sorption of itazigrel from rat rectum was accelerated further, by rapi d release of itazigrel from the micelle vehicle after enzymatic degrad ation of the PS-80 micelle.