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 (t1/2) 4.74 ± 1.80 h; elimination rate constant (Ke) 0.16 ± 0.06 h−1; apparent volume of distribution (Vd/F) 12.23 ± 8.69L • kg−1; 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 (AUC24) 4.29 ± 1.88 μg • mL−1 • h; AUC from time zero to infinity (AUC∞) 4.45 ± 1.81 μg • mL−1 • h; maximum plasma drug concentration (Cmax) 0.64 ± 0.27 μg • mL−1; and time to Cmax (tmax) 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.
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 400 mg 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 (t ½ ) 4.74 -1.80 h; elimination rate constant (K e ) 0.16 -0.06 h -1 ; apparent volume of distribution (Vd/F) 12.23 -8.69 L kg -1 ; apparent total clearance of the drug from plasma (CL/F) 1.63 -0.58 L h -1 kg -1 ; area under the plasma concentration-time curve (AUC) from time 0 to time 24 hours (AUC 24 ) 4.29 -1.88 mg mL -1 h; AUC from time zero to infinity (AUC ¥ ) 4.45 -1.81 mg mL -1 h; maximum plasma drug concentration (C max ) 0.64 -0.27 mg mL -1 ; and time to C max (t max ) 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.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.