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Pharmacokinetics of huperzine A following oral administration to human volunteers


The objective of the present study was to investigate the in vivo pharmacokinetics of huperzine A in healthy human volunteers. Twelve subjects (M 6, F 6; age ranged from 20 ∼ 25 years) participated in the study. Huperzine A was administered in tablet form at a single dose of 0.4 mg. Following oral administration, the presence of huperzine A started to appear in the plasma at 5—10 min, and reached the peak concentrations with a Cmax of 2.59±0.37 ng/ml at 58.33±3.89 min (time to reach peak level, Tmax). The area under plasma vs time curve (AUC0−t) and the area under plasma from zero to infinity (AUC0−∞) for huperzine A were found to be 1986.96± 164.57 μg/1-min and 2450.34±233.32 μg/1-min, respectively. The results of this study indicated that the pharmacokinetics of huperzine A conformed to a two-compartmental open model. The mean values of α and the β half-life were 21.13±7.28 min and 716.25±130.18 min respectively, and snowed a biphasic profile with rapid distribution followed by a slower elimination rate.

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Li, Y.X., Zhang, R.Q., Li, C.R. et al. Pharmacokinetics of huperzine A following oral administration to human volunteers. Eur. J. Drug Metabol. Pharmacokinet. 32, 183–187 (2007).

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