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Pharmacokinetics and tolerability of oral dosage forms of huperzine a in healthy Chinese male volunteers: a randomized, single dose, three-period, six-sequence crossover study

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Summary

Huperzine A is a potent, reversible, and blood-brain barrier permeable acetylcholinesterase inhibitor. The aim of this study was to compare the pharmacokinetics, tolerability, and bioavailability of two formulations with the established reference formulation of huperzine A in a fasting, healthy Chinese male population. This was a randomized, single-dose, 3-period, 6-sequence crossover study. The plasma concentrations of huperzine A were determined by liquid chromatography tandem mass spectrometry. Tolerability was assessed based on subject interview, vital sign monitoring, physical examination, and routine blood and urine tests. The mean (SD) pharmacokinetic parameters of the reference drug were Cmax, 1.550 (0.528) ng/mL; t1/2, 12.092 (1.898) h; AUC0-72h, 17.550 (3.794) ng·h/mL. Those of the test formulation A and test formulation B were Cmax, 1.412 (0.467), 1.521 (0.608) ng/mL; t1/2, 12.073 (2.068), 12.271 (1.678) h; AUC0-72h, 15.286 (3.434) ng·h/mL, 15.673 (3.586) ng·h/mL. The 90% confidence intervals for the AUC0-72h and Cmax were between 0.80 and 1.25. No adverse events were reported by the subjects or found with results of clinical laboratory test. The test and reference products met the regulatory criteria for bioequivalence in these fasting, healthy Chinese male volunteers. All three formulations appeared to be well tolerated.

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  1. These authors contributed equally to this work.

Authors and Affiliations

  1. Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China

    San-lan Wu  (伍三兰), Ying Zhao  (赵 瑛), Yong-ning Lv  (吕永宁) & Ya-ni Liu  (刘亚妮)

  2. Clinical Research Organization for Pharmaceutical Products, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China

    San-lan Wu  (伍三兰), Ying Zhao  (赵 瑛), Yong-ning Lv  (吕永宁) & Ya-ni Liu  (刘亚妮)

  3. Department of Pharmaceutics, School of Pharmacy, Tongji Medical College, Huangzhong University of Science and Technology, Wuhan, 430030, China

    Jun Gan  (甘 珺), Jing Rao  (饶 静), Si-jie He  (贺思洁), Wen-wen Zhu  (朱雯雯) & Jian-geng Huang  (黄建耿)

Authors
  1. San-lan Wu  (伍三兰)
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  2. Jun Gan  (甘 珺)
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  3. Jing Rao  (饶 静)
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  4. Si-jie He  (贺思洁)
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  5. Wen-wen Zhu  (朱雯雯)
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  6. Ying Zhao  (赵 瑛)
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  7. Yong-ning Lv  (吕永宁)
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  8. Jian-geng Huang  (黄建耿)
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  9. Ya-ni Liu  (刘亚妮)
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Corresponding authors

Correspondence to Jian-geng Huang  (黄建耿) or Ya-ni Liu  (刘亚妮).

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Wu, Sl., Gan, J., Rao, J. et al. Pharmacokinetics and tolerability of oral dosage forms of huperzine a in healthy Chinese male volunteers: a randomized, single dose, three-period, six-sequence crossover study. CURR MED SCI 37, 795–802 (2017). https://doi.org/10.1007/s11596-017-1807-8

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  • DOI: https://doi.org/10.1007/s11596-017-1807-8

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