Single dose pharmacokinetic study of CDRI-81/470, a new broad spectrum anthelmintic agent, was carried out in 12 healthy human subjects after a single 375-mg oral dose. The serum, saliva and urine samples were analyzed by HPLC. The compound attained peak serum levels of 15.1±4.6 μg/ml in 2.6±1.1 h and could be measured up to 5 days. Mean serum AUC was 195±69 μg per h/ml. The compound showed a mean apparent elimination half-life of 12.1±4.5 h while mean residence time (MRT) was found to be 11.1±1.7 h. Extent of urinary excretion of CDRI-81/470 (2.3±0.7%) was less than that of its decarboxylate metabolite (5.3±2.2%) up to 10 h post dose. In vivo protein binding in serum was 93.1±1.2% and remained constant over in vivo concentration range. The salivary levels of CDRI-81/470 were higher than the corresponding unbound serum levels. There was a significant correlation between serum and salivary levels of CDRI-81/470, with a mean ratio of saliva to unbound serum levels of 2.04±0.24, indicating the possibility of predicting serum concentrations of CDRI-81/470 from non-invasive salivary sampling technique. Copyright (C) 1998 Elsevier Science B.V.
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