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Concentrations of cefotetan in the intestinal wall of patients with Crohn's disease were investigated with the method of tissue homogenates with the aim to evaluate the effects of inflammation on tissue distribution. Twenty-four patients who underwent surgery were treated with a 2-gram single dose of cefotetan intravenously before the operation. The mean tissue levels in inflamed intestinal wall were constantly higher than in normal wall, but the difference was statistically significant only in samples taken more than 2 h after cefotetan administration (31.0 +/- 17.8 vs 14.7 +/- 11.4 mg/kg; p less than 0.05). The mean residence time was 284.3 min for inflamed tissue and 123.9 min for normal. The areas under the curve were significantly higher in inflamed wall than in normal, with mean values of 4,789 and 3,020.2 mg/l.h, respectively (p less than 0.05). Inflammation seems to facilitate the penetration of cefotetan into the intestinal wall of patients with Crohn's disease but above all, it increases the mean residence time in inflamed tissue.