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Pharmacokinetics and tissue distribution of a water-soluble flavonol triglycoside, CTN986, in mice.

The pharmacokinetics and bioavailability of CTN986, a highly water-soluble flavonol triglycoside that has shown interesting antidepressant effects, were determined in mice after intravenous ( I. V.), intraperitoneal ( I. P.) and oral administrations. Concentrations of CTN986 in the biological samples were determined by a validated LC/MS/MS method. Non-compartmental methods were used to perform pharmacokinetic data analysis. The dose-dependent pharmacokinetics of CTN986 was characterized after I. V. administrations (0.16, 0.4 and 1.0 mg/kg) to mice. There was no significant difference in clearance (CL) with increasing dose [252.66 +/- 42.82 mL/h (0.16 mg/kg) versus 241.73 +/- 14.93 mL/h (1.0 mg/kg)] after I. V. administrations. The absolute bioavailability of CTN986 after I. P. and oral administrations was 96.57 % and 1.31 %, respectively. CTN986 was found to distribute widely in the internal organs of mice 10 min after oral dosage, with tissue concentrations in the order of duodenum, stomach, small intestine, kidney, lung, liver, brain, heart and spleen (from the highest to the lowest). In conclusion, CTN986 could be absorbed and extensively distributed into tissues as its intact form in mice.