Pharmacokinetics of huperzine A following oral administration to human volunteers

Abstract

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 (AUC(0-t)) and the area under plasma from zero to infinity (AUC(0-infinity) for huperzine A were found to be 1986.96 +/- 164.57 microg/l.min and 2450.34 +/- 233.32 microg/l.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 alpha and the beta half-life were 21.13 +/- 7.28 min and 716.25 +/- 130.18 min respectively, and showed a biphasic profile with rapid distribution followed by a slower elimination rate.

Clinic Pharmacokinetic Profiles of Huperzine A Following Transdermal Administration to Healthy Human Volunteers

“…Comparing with previous studies on pharmacokinetic behaviors of huperzine A in human plasma [15,17], the results from the present study suggested that transdermal administration resulted in much longer T max , lower C max , and produced a relatively constant plasma concentration, demonstrating more favorable clinic pharmacokinetic characteristics for AD treatment. Besides, no noticeable AEs were observed during the whole experiment, further manifesting the advantages of transdermal delivery.…”

Treatment with Huperzine A Improves Cognition in Vascular Dementia Patients

“…Compared with the same type of drugs approved by the United States Food and Drug Administration, the unique chemical structure of Huperzine A facilitates its penetration of the blood-brain barrier. Huperzine A tends to target the frontal and temporal lobes, as well as the hippocampus of the brain [8]. It selectively inhibits acetylcholinesterase activity and thus facilitates increase in acetylcholine levels in the brain thereby improving memory and learning abilities.…”

Population pharmacokinetic modeling and simulation of huperzine A in elderly Chinese subjects

“…Although some pharmacokinetic studies concerning huperzine A in young healthy subjects have been reported [8][9][10][11] , there are still no reports on the pharmacokinetic study of huperzine A in elderly subjects. Our preliminary experiments with huperzine A in elderly people showed that drug exposure AUC increased by 75% compared with that in young healthy individuals [8,9] .…”

“…Our preliminary experiments with huperzine A in elderly people showed that drug exposure AUC increased by 75% compared with that in young healthy individuals [8,9] . One factor may be the degraded physiological functions in elderly people compared with young people.…”

“…Li et al [8] and Qiang et al [9] reported that pharmacokinetic studies were conducted in young healthy volunteers after taking 0.4 mg [8] or 0.99 mg [9] of huperzine A, which are higher than the commonly used clinical dose in Chinese subjects. Li et al [10] conducted a pharmacokinetic study in healthy subjects who received a single 0.2-mg dose huperzine A.…”