Degradation of Bromazepam by the Intestinal Microflora(Pharmaceutical,Chemical)

概要

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Degradation of four benzodiazepines, i.e. bromazepam, diazepam, desmethyidiazepam, and 7-bromo-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2(1H)-one, in a broth containing human feces was studied. Degradation of bromazepam was also investigated in a fecal medium, a homogenate of the liver and a homogenate of intestinal epithelial cells of rat. More than 80% of bromazepam, which contains a pyridine ring in its structure, was degraded in the broth containing 8% human feces under both anaerobic and aerobic conditions. The major degradation product of bromazepam was identified as 2-(2-amino-5-bromobenzoyl)pyridine by means of thin layer chromatography and gas chromatography-mass spectra analyses. About 70, 90, and 90% of bromazepam remained in the fecal medium, homogenate of the liver and homogenate of intestinal epithelial cells of rat, respectively, after incubation for 5 h at 37℃. Therefore, degradation of bromazepam by the intestinal microflora may be considered to be one of the major factors influencing the bioavailability after oral administration to man.
社団法人日本薬学会の論文
1987-10-25