尼群地平共研粉末的制备及大鼠体内药动学  

Preparation of nitrendipine co-grinding powder and its pharmacokinetics in rats

作　　者：游本刚[1] 张娅梅[1] 李颖[1] 李新章[1] 唐丽华[1] 

机构地区：[1]苏州大学医学部药学院,江苏苏州215123

出　　处：《中国医院药学杂志》2011年第12期984-987,共4页Chinese Journal of Hospital Pharmacy

基　　金：苏州大学大学生课外学术科研基金(编号:KY2010357B)

摘　　要：目的:研究难溶性药物尼群地平共研粉末在大鼠体内的药动学。方法:采用HPLC-UV法,测定大鼠灌胃尼群地平共研粉末(T)和物理混合粉末(R)后不同时间点的血药浓度,绘制药-时曲线,计算药动学参数及相对生物利用度。结果:大鼠灌胃相当于尼群地平20mg的T和R后,血浆中尼群地平的tmax分别为(1.6±0.5)和(2.0±0.7)h;Cmax分别为(496.2±215.1)和(260.6±56.9)μg.L-1;用梯形法计算,AUC0-t分别(4 077.0±1 487.3)μg.h.L-1和(2 438.1±1 039.8)μg.h.L-1。与物理混合粉末R相比,尼群地平共研粉末T的相对生物利用度为209.27%。结论:尼群地平共研粉末与尼群地平物理混合粉末相比,在大鼠体内吸收迅速、生物利用度高。OBJECTIVE To study the pharmacokinetics of nitrendipine co grinding powder in rats. METHODS HPLC method was developed to quantify the drug plasma concentration in rats after adminstered a single dose of nitrendipine co-grinding powder （T） and physical mixture （R）, and then the plasma concerntration of drug-time profiles were drawn, the pharmacokinetic parameters and relative oral bioavailability were also calculated. RESULTS After administration of T and R （equal 20mg nitrendipine）, the pharmacokinetic parameters were obtained as follows： tmax were（1.6 ± 1）. 5）h and （2.0 ±0. 7）h, respec tively; Cmax were （496. 2±215.1） ）μg·L^-1, and （260. 6±56. 9） ）μg·L^-1 , respectively; AUC0-t were （4077. 0±1487. 3）μg·h·L^-1 and （2438. 1 ±1039.8）μg·h·L^-1 , respectively. Compared with R, the relative bioavailabilities of T was 209. 27%. CONCLUSION Nitrendipine co-grinding powder can be absorbed rapidly and has an enhanced relative oral bioavailability, compared with its physical mixture.

关 键 词：尼群地平 共研粉末 大鼠 药动学 

分 类 号：R222[医药卫生—中医基础理论]