Evaluation of Crushed Tablet for Oral Administration and the Effect of Food on Apixaban Pharmacokinetics in Healthy Adults.

摘要: Abstract Purpose These studies evaluate the relative bioavailability of crushed apixaban tablets and effect food on pharmacokinetic properties. Methods An open-label, randomized, crossover study in 33 healthy adults compared 2 × 5-mg administered whole (reference), suspended 30 mL water, mixed with g applesauce. A second 22 1 tablet when fasted (reference) or immediately after consumption a high-fat, high-calorie meal. Point estimates 90% CIs for geometric mean ratios were generated C max , AUC 0–∞ 0–t . Findings met bioequivalence criteria water. decreased by 21.1% 16.4%, respectively, lower bound falling below Similarly, administration meal reduced 14.9% 20.1%, respectively. The exposure reductions both considered not clinically significant. Implications Apixaban can be whole, without food. results these alternative methods support their use patients who have difficulty swallowing tablets. ClinicalTrials.gov identifiers: NCT02101112 NCT01437839.