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Pharmacokinetics of huperzine A following oral administration to human volunteers

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Summary

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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References

  1. 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.

    Article  CAS  Google Scholar 

  2. 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.

    CAS  Google Scholar 

  3. 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.

    Article  CAS  Google Scholar 

  4. Tang X.C., (1996): Huperzine A (Shuangyi**): a promising drug for Alzhemimer’s disease. Zhongguo Yaoli Xuebao 17, 481–484.

    CAS  PubMed  Google Scholar 

  5. 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.

    Article  CAS  PubMed  Google Scholar 

  6. Qian B.C., Wang M., Zhou Z.F., (1995): Pharmacokinetics of tablet huperzine A in six volunteers. Acta Pharmacol. Sin. 16, 396–398.

    CAS  Google Scholar 

  7. Wang Y.E., Feng J., Lu W.H., (1988): Pharmaceutics of huperaine A in rat and mice. Acta Pharmacol. Sin. 9, 193–197.

    CAS  Google Scholar 

  8. 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.

    Article  Google Scholar 

  9. 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.

    CAS  Google Scholar 

  10. 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.

    Article  CAS  PubMed  Google Scholar 

  11. 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.

    Article  PubMed  Google Scholar 

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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

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