Document Detail

Synthesis and disposition of 14C-labelled 81/470, a new anthelminthic agent in rats.
MedLine Citation:
PMID:  9403350     Owner:  NLM     Status:  MEDLINE    
CDRI compound 81/470 (AH) is a new broad-spectrum anthelminthic agent under development for clinical and veterinary application. We herewith report the synthesis of 14C-labelled AH, and a study of the tissue distribution and excretion of radioactivity after administering a single 1 mg/kg p.o. or i.v. dose in young male rats. After oral administration of the dose, percent radioactivity recovered in 24-h urine, faeces and tissues were 17.9, 59.7 and 22.9 respectively. The levels were below detection limit in brain and gonads up to 24 h. In bile-duct-cannulated rats, the majority (37.8 +/- 2.8 and 43.8 +/- 6.4) of the radioactivity was excreted in the bile within 24 h of p.o. and i.v. administration, respectively. After an oral dose (1 mg/kg), the urinary excretion of radioactivity in rats was found to be approximately one-half (21 +/- 5.7, 18.3 +/- 2.1) of that obtained by i.v. administration of an equal dose (40.2 +/- 3.1 and 35 +/- 1.3), in bile-duct-intact and cannulated rats respectively.
J K Paliwal; D Ramesh; R C Gupta
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  International journal of clinical pharmacology research     Volume:  17     ISSN:  0251-1649     ISO Abbreviation:  Int J Clin Pharmacol Res     Publication Date:  1997  
Date Detail:
Created Date:  1998-01-27     Completed Date:  1998-01-27     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  8110183     Medline TA:  Int J Clin Pharmacol Res     Country:  SWITZERLAND    
Other Details:
Languages:  eng     Pagination:  23-30     Citation Subset:  IM    
Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Lucknow, India.
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MeSH Terms
Administration, Oral
Anthelmintics / administration & dosage,  chemical synthesis*,  pharmacokinetics*
Benzimidazoles / administration & dosage,  chemical synthesis*,  pharmacokinetics*
Bile / chemistry
Carbamates / administration & dosage,  chemical synthesis*,  pharmacokinetics*
Carbon Radioisotopes / pharmacokinetics
Feces / chemistry
Rats, Sprague-Dawley
Tissue Distribution
Reg. No./Substance:
0/Anthelmintics; 0/Benzimidazoles; 0/Carbamates; 0/Carbon Radioisotopes; 93522-20-4/CDRI 81-470

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