摘要
对１０名男性受试者单剂量ｐｏ２４０ｍｇＶｅｒ缓释片药代动力学及心电图变化进行研究。血药浓度—时间数据用零级吸收过程的一室模型拟合，其药代动力学参数：Ｔｍａｘ５．９±１．６ｈ；Ｃｍａｘ１１８．９±３７．２μｇ·Ｌ－１；Ｔ１５．４±１．５ｈ；ｋ０３０．５±１７．５μｇ·Ｌ－１·ｈ－１；Ｔ１／２１０．８±４．９ｈ。ＰＲ间期延长有显著意义，血药浓度与ＰＲ间期变化满足Ｓ型模型，其药效学参数：ＥＣ５０６４．６±１６．９μｇ·Ｌ－１；Ｅｍａｘ５４±１１ｍｓ；ｓ１．６８±０．
Both verapamil pharmacokinetics and electrocardio graphic changes in 10 Chinese volunteers were studied after po 240 mg of verapamil sustained release tablet. A one compartment model with zero order absorption gave a better fitting to concentration-time data with values of r 2>0.96. The main pharmacokinetic parameters obtained were: T max , 5.9±1.6 h; C max , 118.9±37.2 μg\5L -1 ; T 1, 5.4±1.5 h; k 0, 30.5±17.5 μg\5L -1 \5h -1 ; T 1/2 , 10.8 ±4.9 h; MRT, 15.4±3.2 h and AUC. 1.96±0.82 mg\5h\5L -1 . There were significant prolongations of PR intervals after dose. Relationships between PR interval changes and plasma concentrations of verapamil were better fitted to sigmoidal model, with r 2>0.98. The corresponding pharmacodynamic parameters were estimated. EC 50 , 64.6±16.9 μg\5L -1 , E max , 54±11 ms and s, 1.68±0.66.
出处
《药学学报》
CAS
CSCD
北大核心
1996年第7期487-491,共5页
Acta Pharmaceutica Sinica
关键词
维拉帕米
药代动力学
心电图
Verapamil
Pharmacokinetics
Electrocardiography
Zero order absorption
