PURPOSE: To determine the bioavailability and pharmacokinetic profile of lumiracoxib from different sites in the gastrointestinal tract. METHODS: Subjects (11 healthy adult males) were randomized to receive a 100 mg lumiracoxib dose, via a site-specific radiolabeled delivery capsule, to the stomach (internal reference), proximal small bowel, distal small bowel, or ascending colon. Gamma scintigraphy was used for real-time visualization of capsule location, and a radiofrequency signal was used to activate capsules at target site. RESULTS:Ten subjects completed the study. The mean capsule activation times for the stomach, proximal small bowel, distal small bowel, and ascending colon were 0.22, 1.52, 3.43, and 11.46 h post dose, respectively. Lumiracoxib was well absorbed from the proximal and distal small bowel, with AUC(0-infinity) ratios 104% (86, 127)% and 110% (89, 136)%, respectively. The highest Cmax (2413 ng/ml) and AUC(0-infinity) for lumiracoxib were in the distal small bowel (6842 ng x h/ml). Effective absorption was observed from the ascending colon, with an AUC(0-infinity) ratio of 85% (69, 104)% vs. the reference. CONCLUSIONS:Lumiracoxib is rapidly and efficiently absorbed throughout the gastrointestinal tract.
RCT Entities:
PURPOSE: To determine the bioavailability and pharmacokinetic profile of lumiracoxib from different sites in the gastrointestinal tract. METHODS: Subjects (11 healthy adult males) were randomized to receive a 100 mg lumiracoxib dose, via a site-specific radiolabeled delivery capsule, to the stomach (internal reference), proximal small bowel, distal small bowel, or ascending colon. Gamma scintigraphy was used for real-time visualization of capsule location, and a radiofrequency signal was used to activate capsules at target site. RESULTS: Ten subjects completed the study. The mean capsule activation times for the stomach, proximal small bowel, distal small bowel, and ascending colon were 0.22, 1.52, 3.43, and 11.46 h post dose, respectively. Lumiracoxib was well absorbed from the proximal and distal small bowel, with AUC(0-infinity) ratios 104% (86, 127)% and 110% (89, 136)%, respectively. The highest Cmax (2413 ng/ml) and AUC(0-infinity) for lumiracoxib were in the distal small bowel (6842 ng x h/ml). Effective absorption was observed from the ascending colon, with an AUC(0-infinity) ratio of 85% (69, 104)% vs. the reference. CONCLUSIONS:Lumiracoxib is rapidly and efficiently absorbed throughout the gastrointestinal tract.
Authors: James B Mangold; Helen Gu; Lolita C Rodriguez; Johanne Bonner; Janet Dickson; Christiane Rordorf Journal: Drug Metab Dispos Date: 2004-05 Impact factor: 3.922