Bioavailability and Gastrointestinal Toxicity Study of Hexamethylene Bisacetamide (HMBA: NSC-95580) in Beagle Dogs

摘要

Four beagle dogs received intravenous doses (400 mg/kg) and oral doses (400 mg/kg) of HMBA in a crossover study to assess bioavailability. Doses were well tolerated with little or no evidence of toxicity. Bioavailability of orally administered doses was estimated to be 97.5 plus or minus 14.3 percent. The biological half-life of HMBA was 1.8 plus or minus 0.2 hours. Four additional dogs received gastric gavage doses of 200 mg/kg every 4 hours during a 120 hour dose period (total of 31 doses/dog). Convulsions were noted in all four dogs. Males appeared to be more sensitive to HMBA-induced convulsions than females. No evidence of gastrointestional (GI) toxicity or GI lesions were detected.