Relative Bioavailability of Apixaban Solution or Crushed Tablet Formulations Administered by Mouth or Nasogastric Tube in Healthy Subjects

摘要: Abstract Purpose Crushed tablet and solution formulations of apixaban administered orally or via a nasogastric tube (NGT) may be useful in patients unable to swallow solid dose formulations. It is important understand whether new and/or methods administration impact bioavailability pharmacokinetic properties. These studies evaluated the relative (F rel ) orally; oral NGT flushed with either 5% dextrose water (D 5 W) infant formula; nutritional supplement; crushed suspended D W NGT. Methods Three open-label, randomized, crossover were conducted healthy adults (study 1: 10-mg [reference] versus solution, both PO; study 2: 5-mg PO 3: supplement NGT). Point estimates 90% CIs geometric mean ratios (GMRs; test/reference) generated for C max AUC. Adverse events recorded throughout each study. Findings F was 105% tablet, flush, formula supplement, 96.7%, 92.2%, 81.3%, 95.1%, respectively. The GMRs all AUCs met bioequivalence criterion except that (0.766–0.863). corresponding 0.977, 0.953, 0.805, 0.682, 0.884. For criterion. Apixaban well tolerated 3 studies; most adverse mild. Implications Comparable observed formula, suspension. Exposure less when supplement. results support several alternative administering certain clinical situations. ClinicalTrials.gov identifiers: NCT02034565, NCT02034578, NCT02034591.