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Metabolism and Disposition of Tribendimidine and Its Metabolites in Healthy Chinese Volunteers.
- Source :
- Drugs in R&D; 2010, Vol. 10 Issue 2, p83-90, 8p, 1 Diagram, 1 Chart, 4 Graphs
- Publication Year :
- 2010
-
Abstract
- Background: Tribendimidine is a new anthelmintic agent synthesized by Chinese scientists. It is a broad spectrum agent with high activity against parasites. However, its disposition and metabolism remain unknown. Objective: To investigate the metabolism, disposition, and metabolites of tribendimidine in healthy human volunteers. Methods: Twelve healthy Chinese volunteers were chosen after clinical assessment of health status and laboratory tests. They received single oral doses of tribendimidine 400mg enteric-coated tablets. Blood and urine samples were collected at scheduled timepoints. Samples were qualitatively and quantitatively analyzed by liquid chromatography-mass spectrometric (LC-MS) and high performance liquid chromatography (HPLC) methods, respectively. Results: Tribendimidine was rapidly and completely broken down to p-(1-dimethylamino ethylimino) aniline (dADT) and terephthalaldehyde (TPAL). Furthermore, dADT was partially transformed to acetylated dADT, and TPAL completely transformed to terephalic acid (TPAC). The main pharmacokinetic parameters (± SD) of dADT were as follows: elimination half life (t½) 4.74 ± 1.80 h; elimination rate constant (K<subscript>e</subscript>) 0.16 ± 0.06 h<superscript>-1</superscript>; apparent volume of distribution (Vd/F) 12.23 ± 8.69L · kg<superscript>-1</superscript>; apparent total clearance of the drug from plasma (CL/F) 1.63 ± 0.58L · h-1 kg-1; area under the plasma concentration-time curve (AUC) from time 0 to time 24 hours (AUC<subscript>24</subscript>) 4.29 ± 1.88 µg · mL<superscript>-1</superscript> · h; AUC from time zero to infinity (AUC∞) 4.45 ± 1.81 µg · mL<superscript>-1</superscript> h; maximum plasma drug concentration (C<subscript>max</subscript>) 0.64 ± 0.27 µg · mL<superscript>-1</superscript>; and time to C<subscript>max</subscript> (t<subscript>max</subscript>) 4.20 ± 0.71 h. A total of 35.28% dADT and 28.50% TPAC were excreted through the urine within 24 hours after tribendimidine administration. Conclusion: These results reveal the disposition, metabolism, and main metabolites of tribendimidine in healthy Chinese volunteers. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 11745886
- Volume :
- 10
- Issue :
- 2
- Database :
- Complementary Index
- Journal :
- Drugs in R&D
- Publication Type :
- Academic Journal
- Accession number :
- 66916820
- Full Text :
- https://doi.org/10.2165/11539320-000000000-00000