A Dose Dumping Study with a Sustained-Release Formulation of Bunazosin (E1015) in Healthy Volunteers

The pharmacokinetics of a single oral dose of sustained-release bunazosin 6mg were compared under fasting and nonfasting conditions in 12 healthy volunteers. Following ingestion of a high fat (59g) meal, the extent of gastrointestinal absorption of bunazosin was significantly reduced in comparison with that obtained in the fasting state (mean peak plasma bunazosin concentration 5.6 ± 2.1 vs 12.8 ± 4.5 μg/L; mean area under the bunazosin concentration-time curve 85.1 ± 34.1 vs 114.9 ± 41.6 μg/L·h), whereas the rate of bunazosin absorption was not significantly modified (mean time to peak plasma concentration 4.9 ± 1.2 vs 5.8 ± 1.9 hours).