Retrospective population-based analysis of the dose-response (fecal fat excretion) relationship of orlistat in normal and obese volunteers.

摘要: Orlistat, an inhibitor of gastrointestinal lipases, limits the absorption ingested fat and could become a potential treatment for obesity. This analysis was performed to elucidate relationship between orlistat dose intensity inhibition dietary (assessed by measuring fecal excretion). In 11 phase I double-blind, placebo-controlled, parallel-group randomized studies, total 171 subjects received oral daily doses that ranged from 30 1200 mg or matching placebo three times day 9 10 days. The results mean excretion percentage (relative fat) were correlated dose. A simple maximum-effect model included basal value used fit dose-response all evaluable subjects. maximum excreted in feces approximately 32% during administration compared with 5% administration. produced 50% effect 98 mg/day. model-fitting suggests existence steep portion curve up 400 mg/day, subsequent tendency plateau at higher doses. Such instrumental identifying appropriate be therapeutic trials weight loss obese patients.