Effect of Food on the Bioavailability of Captopril in Healthy Subjects

: 14C‐Captopril was administered as 100‐mg tablets to 12 subjects in a two‐way crossover study in which subjects were either fasted or were given a standard meal immediately prior to dosing. Based on blood level and urinary excretion data, both the absorption of total radioactivity and the bioavailability of captopril were decreased approximately 35 to 40 per cent after a meal. Whether this moderate decrease in the absorption and the bioavailability of captopril caused by food is of clinical significance has not yet been determined.