BIOAVAILABILITY OF ITAZIGREL IN DOGS AFTER ORAL-ADMINISTRATION OF SOFT ELASTIC CAPSULES

The effect of Tween 80, a solubilizing agent, on gastrointestinal abso rption was investigated in dogs after oral administration of soft elas tic capsules (SEC) of itazigrel with respect to bioavailability. The b ioavailability was determined from the area under the curve (AUC) of p lasma itazigrel concentration after drug administration. In spite of i ts known low water solubility (less than 100 ng/ml), the mean absolute bioavailability of itazigrel was about 90% in six dogs under fasting conditions. Furthermore, the absolute bioavailability was also about 8 5% when measured 30 min after standard food was given to the dogs. The high bioavailability observed in this oral study is believed to be du e to Tween 80 contained in SEC which apparently caused complete dissol ution in the gastrointestinal tract.