Gastro-intestinal blood loss with high dose tilcotil (Ro 12-0068) and aspirin: an open crossover clinical trial and pharmacokinetic assessment in normal volunteers.
An open crossover study was carried out in 8 normal volunteer subjects to compare faecal blood loss resulting from tilcotil (Ro12-0068), a new anti-inflammatory agent, and from enteric-coated aspirin. After a 1-week run-in period, subjects were allocated at random to receive treatment for 2 weeks with either 40 mg tilcotil as a single dose per day or aspirin, 900 mg 4-times daily, reduced if necessary to a maximum tolerated dose. Subjects were then crossed over to the alternative treatment for a further 2 weeks. The results showed that tilcotil produced less blood loss, assessed by a radioactive labelling method, and was better tolerated than aspirin. Plasma concentrations of tilcotil showed that the drug's half-life was approximately 50 hours, compatible with once daily dosage, and steady state concentrations on multiple dosing were reached after 10 to 12 days.
D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects; D001241:Aspirin / Q000008:administration & dosage* / Q000009:adverse effects; D002986:Clinical Trials as Topic; D004305:Dose-Response Relationship, Drug; D005260:Female; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced*; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D010894:Piroxicam / Q000031:analogs & derivatives*; D011897:Random Allocation; D013843:Thiazines / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013843:Thiazines; D010894:Piroxicam; D001241:Aspirin; C032801:tenoxicam