Preliminary pharmacokinetics of a new anthelmintic agent, CDRI-81/470 in healthy subjects

  • Nagaraja N
  • Singh S
  • Paliwal J
 et al. 
  • 5


    Mendeley users who have this article in their library.
  • 0


    Citations of this article.


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.

Author-supplied keywords

  • Benzimidazole anthelmintic
  • CDRI-81/470
  • Clinical pharmacokinetics
  • Human
  • Oral
  • Single-dose

Get free article suggestions today

Mendeley saves you time finding and organizing research

Sign up here
Already have an account ?Sign in

Find this document


Cite this document

Choose a citation style from the tabs below

Save time finding and organizing research with Mendeley

Sign up for free