Pharmacokinetics of single dose sustained release microspheres of Huperzine A for injection in Chinese healthy volunteers
10.13699/j.cnki.1001-6821.2018.20.014
- VernacularTitle:注射用石杉碱甲缓释微球单次给药在中国健康人体药代动力学研究
- Author:
Zhen-Zhen ZHU
1
;
Li-Wei LANG
;
Hong-Yan WANG
;
Li-Zhen WANG
;
Feng DUAN
;
Li ZHANG
;
Min WANG
;
Zhan-Dong SONG
;
Zhen-Man WEI
Author Information
1. 中国人民解放军第三〇二医院 药物试验中心
- Keywords:
Huperzine A;
extended release dosage system;
single dose;
pharmacokinetics;
plasma concentration
- From:
The Chinese Journal of Clinical Pharmacology
2018;34(20):2441-2444
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the sustained release microspheres of Huperzine A for injection single dose pharmacokinetic changes in healthy volunteers.Methods This study taken randomized , double -blind, placebo-controlled, dose escalation experiment design , 48 healthy vol-unteers were randomly divided into 5 groups, then they respectively taken orally single dose (0.75,1.5,3.0,4.5,6.0 mg) sustained release mi-crospheres of Huperzine A for injection by intramuscular injection .Before and after administration , we taken biological samples for detection of blood drug concentration , furthermore, calculation of blood drug pharma-cokinetic parameters.Results After single dose injected 0.75 mg,1.5 mg,3.0 mg,4.5 mg,6.0 mg sustained release microspheres of Huperzine A, the main pharmacokinetic parameters of plasma Huperzine A , tmax were (120.00 ±41.57 ), (150.00 ±37.95 ), (120.00 ±12.83), (105.00 ±12.42 ), (108.00 ±18.14 ) h; t1/2were (61.66 ±20.78 ), ( 44.84 ± 16.05 ), ( 73.73 ± 30.25 ), (41.47 ±21.65), (55.89 ±18.17)h; Cmaxwere (0.21 ±0.04),(0.62 ±0.41), (1.18±0.24),(2.74 ±0.47),(2.86 ±0.67)μg· L-1; AUC0-twere (41.32 ±7.02),(106.68±66.79), (227.97 ±42.09),(505.01 ±79.38),(541.93 ±124.47)ng· mL-1· h.Conclusion After single injection of dif-ferent doses of Huperzine A sustained release microspheres , the Cmaxand AUC0-twere increased with the dose escala-tion, presented dose-proportional relationship.and the absorption rate and elimination rate were not affected by the dosage.The drug has a long half-life, that supports long intervals of administration during treatment .
