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
10.1007/s11596-017-1807-8
- Author:
WU SAN-LAN
1
;
GAN JUN
;
RAO JING
;
HE SI-JIE
;
ZHU WEN-WEN
;
ZHAO YING
;
LV YONG-NING
;
HUANG JIAN-GENG
;
LIU YA-NI
Author Information
1. Department of Pharmacy
- Keywords:
huperzine A;
pharmacokinetics;
bioequivalence;
tolerability;
liquid chromatography tandem mass spectrometry
- From:
Journal of Huazhong University of Science and Technology (Medical Sciences)
2017;37(5):795-802
- CountryChina
- Language:Chinese
-
Abstract:
Huperzine A is a potent,reversible,and blood-brain barrier permeable acetylcholinesterase irhibitor.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.
