K. Yamamoto et al., ENHANCED RECTAL ABSORPTION OF ITAZIGREL FORMULATED WITH POLYSORBATE-80 MICELLE VEHICLE IN RAT - ROLE OF CO-ADMINISTERED ESTERASE, Journal of Pharmacy and Pharmacology, 46(7), 1994, pp. 608-611
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.