Rivaroxaban crushed tablet suspension characteristics and relative bioavailability in healthy adults when administered orally or via nasogastric tube. Issue 4 (16th May 2014)

• Record Type: Journal Article
• Authors: Moore, Kenneth T.; Krook, Mark A.; Vaidyanathan, Seema; Sarich, Troy C.; Damaraju, C. V.; Fields, Larry E.
• Is Part Of: Clinical pharmacology in drug development. Volume 3:Issue 4(2014:Jul./Aug.)
• Page Start: 321
• Page End: 327
• Publication Date: 2014-05-16
• Subjects: Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.123
• Languages: English
• ISSNs: 2160-7648

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="cpdd123-sec-0001" sec-type="section"> <title>Purpose</title> <p>Because some patients have difficulty swallowing a whole tablet, we investigated the relative bioavailability of a crushed 20 mg rivaroxaban tablet and of 2 alternative crushed tablet dosing strategies.</p> </sec> <sec id="cpdd123-sec-0002" sec-type="section"> <title>Methods</title> <p>Stability and nasogastric (NG) tube adsorption characteristics of a crushed rivaroxaban tablet were assessed. Then, in 55 healthy adults, relative bioavailability of rivaroxaban administered orally as a whole tablet (<italic>Reference</italic> [<italic>Whole‐Oral</italic>]), crushed tablet in applesauce suspension (<italic>Crushed‐Oral</italic>), or crushed tablet in water suspension via NG tube (<italic>Crushed‐NG</italic>) were determined.</p> </sec> <sec id="cpdd123-sec-0003" sec-type="section"> <title>Results</title> <p>There were no significant changes in mean percent of non‐degraded rivaroxaban recovered over 4 hours from crushed tablet suspensions (>98.4% recovery across all suspensions and time points) or after NG tube exposure (recovery: 99.1% for silicone and 98.9% for polyvinyl chloride NG tubes). Relative bioavailability was similar between Crushed‐Oral and Reference dosing (C<sub>max</sub> and AUC<sub>∞</sub> were within the 80–125% bioequivalence limits). Relative bioavailability was also similar between the Crushed‐NG and Reference dosing (AUC<sub>∞</sub> was within bioequivalence limits; C<sub>max</sub> [90% CI range: 78.5–85.8%] was only slightly below the 80% lower bioequivalence limit).</p> </sec> <sec id="cpdd123-sec-0004" sec-type="section"> <title>Conclusions</title> <p>A crushed rivaroxaban tablet was stable and when administered orally or via NG tube, displayed similar relative bioavailability compared to a whole tablet administered orally.</p> </sec> </abstract>