Oral ileocolonic drug delivery by the colopulse-system: a bioavailability study in healthy volunteers

Abstract

The release profile of a novel oral ileocolonic drug delivery technology (ColoPulse-technology) was assessed by a combination of conventional kinetics of a marker substance in blood and site-specific signaling by stable isotope technology. Since ileocolonic delivery involves the drug release in a region in which bacteria are highly present, a prolonged lag time should coincide with proven bacterial enzyme activity. The latter can be tested using 13C-urea as the marker substance. The study was designed as a two period (uncoated versus coated capsule) crossover single dose bioavailability study in healthy subjects. The 13C-recovery data after oral administration of 13C-urea using the ColoPulse delivery system showed a delayed sigmoid release in all subjects with a lag time of > 3h (median: 330 min). Release was achieved in a urease-containing intestinal segment in all healthy subjects. Complete release in the ileocolonic region was achieved in 10 of 11 subjects. The ColoPulse-technology therefore enables specific and reliable drug delivery in the ileocolonic region in healthy volunteers.