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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Liu J.S., Zhu Y.L., Zhou Y.Z., Han Y.Y., Wu F.W., Qi B.F., (1986): The structure of huperzine A and B, two new alkaloids exhibiting marked anticholinesterase activity. Can. J. Chem. 64, 837–839.
Tang X.C., Han Y.F., Chen X.P., Zhu X.D., (1986): Effects of huperzine A on learning and retrieval processes of discrimination performance in rats. Acta Pharmacol. Sin. 7, 507–511.
Tang X.C., De S.P., Sugaya K., Giacobini E., (1989): Effect of huperzine A, a new Cholinesterase inhibitor, on the central cholinergic system of the rat. J. Neur. Res. 24, 276–285.
Tang X.C., (1996): Huperzine A (Shuangyiping): a promising drug for Alzhemimer’s disease. Zhongguo Yaoli Xuebao 17, 481–484.
Zangara A., (2003): The psychopharmacology of huperzine A: an alkaloid with cognitive enhancing and neuroprotective properties of interest in the treatment of Alzheimer’s disease. Pharmacol. Biochem. Behav. 75, 675–686.
Qian B.C., Wang M., Zhou Z.F., (1995): Pharmacokinetics of tablet huperzine A in six volunteers. Acta Pharmacol. Sin. 16, 396–398.
Wang Y.E., Feng J., Lu W.H., (1988): Pharmaceutics of huperaine A in rat and mice. Acta Pharmacol. Sin. 9, 193–197.
Wang Y.W., Chu D.F., Gu J.K., (2004): Liquid chromatographic tandem mass spectrometric method for the quantitation of huperzine A in dog plasma. J. Chromatogr. B. 4, 375–378.
Yue P., Zhao Y., Tao T., (2005): Determination of hupezine A in cerebrospinal fluid of rats by HPLC-Fluorescence. Zhongguo Yaoxue Zazhi. 40, 1503–1507.
Li C, Du F.F., Yu C, (2004): A sensitive method for the determination of the novelcholinesterase inhibitor ZT-1 and its active metabolite huperzine A in rat blood using liquid chromatography /tandem mass spectrometry, Rapid Commun. Mass Spectrom. 18, 651–656.
Li Y.X., Jiang X.H., Lan K., Wang L., (2007): Simple determination of huperzine A in human plasma by liquid chromatographic tandem mass spectrometric method, Biomed. Chromatogr. 21, 15–20.
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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). https://doi.org/10.1007/BF03191002