中国药房Issue(28)：3915-3917,3.DOI:10.6039/j.issn.1001-0408.2015.28.09
尼索地平控释贴剂在自发性高血压大鼠体内的药动学-药效学结合模型的建立Δ
Study on the Pharmacokinetic-pharmacodynamic Model of Nisoldipine Controlled-release Patches in Spon-taneously Hypertensive Rats
摘要
Abstract
OBJECTIVE:To establish the pharmacokinetic-pharmacodynamic(PK-PD) model of Nisoldipine controlled-release patches(NCRP)in spontaneously hypertensive rats(SHR). METHODS:SHR were randomized into a patch(NCRP)group and a tablet(Nisoldipine tablets)group,with 6 rats in each group. The microdialysis probes were implanted in SHR. Each rat was given 5 mg nisoldipine. Plasma microdialysate was collected within 36 h after administration. HPLC was adopted to determine the plasma concentration of nisoldipine,and WinNonlin 5.3 was employed to calculate Pharmacokinetic parameters. With heart rate and blood pressure as pharmacodynamic indexes,PK-PD model study was conducted. RESULTS:Vs. nisoldipine tablets,NCRP has con-trolled release effect. The relationship between NCRP drug effect and effect-site concentration met the Sigmoid-Emax model. The main parameters of the PK-PD model for heart rate and systolic blood pressure were as follows as Emax of (2.65 ± 0.06) and (10.71 ± 0.87),EC50 of (83.65 ± 35.25) and (1.29 ± 0.26) ng/ml,γ of (0.83 ± 0.91) and (1.2 ± 0.35),Keo of (0.37 ± 0.53) and (0.91±0.24)h-1. CONCLUSIONS:PK-PD model of NCRP in SHR has been established successfully.关键词
尼索地平/控释贴剂/微透析/自发性高血压大鼠/药动学-药效学结合模型Key words
Nisoldipine/Controlled-release patch/Microdialysis/Spontaneously hypertensive rat/Pharmacokinetic-pharmaco-dynamic model分类
医药卫生引用本文复制引用
聂阳,许良葵,李博,朱俊访,陈新颖..尼索地平控释贴剂在自发性高血压大鼠体内的药动学-药效学结合模型的建立Δ[J].中国药房,2015,(28):3915-3917,3.基金项目
广东省医学科研基金 （）
