朱珍真 1郎丽巍 1王红艳 1王丽珍 1段锋 1张丽 1王敏 1宋占东 1魏振满1
作者信息
- 1. 中国人民解放军第三〇二医院 药物试验中心,北京 100039
- 折叠
摘要
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 .关键词
石杉碱甲/缓释制剂/单次给药/药代动力学/血药浓度Key words
Huperzine A/extended release dosage system/single dose/pharmacokinetics/plasma concentration分类
医药卫生
