摘要
目的用基于分布平衡的药代动力学理论,建立单纯消除相的血药浓度-时间曲线,测定奥美拉唑的主要药代动力学参数。方法大鼠缓慢恒速静脉滴注奥美拉唑,滴注期间不同时间动脉采血,高效液相色谱法测定血浆药物浓度,GraphPrism6.0软件计算参数。结果奥美拉唑恒速静脉滴注的血药浓度-时间呈一阶指数关系,血药浓度在静脉滴注初期上升速度快,随着时间延长,上升速度逐渐减慢,在5个消除半衰期达到稳态。奥美拉唑在大鼠的消除速率常数K为(2.95±0.67)/h,半衰期为(15±4)min,表观分布容积为(0.30±0.17)L,清除率为(0.83±0.33)L/h。结论恒速静滴给药过程中药物在体内分布基本平衡,无分布干扰,测得的药动学参数更接近实际。
Objective To determine the pharmacokinetic parameters based on distribution equilibrium theory by establishing the blood drug concentration-time curve of single elimination phase.Methods Rats were intravenously infused with omeprazole at andante constant rate.Blood was collected at different time points during infusion,and drug concentration in plasma was detected by HPLC.Pharmacokinetic parameters were calculated with GraphPrism 6.0 software.Results The concentration-time curve of omeprazole during intravenous infusion showed a first-order exponential relationship.The increase of plasma omeprazole concentration was rapid at the initial stage of the infusion and then became gradually slow as time went on.After 5 half lives a steady state was reached.The elimination rate constant(K)of omeprazole in rats was(2.95±0.67)h-1.The half-life was(15±4)min.The apparent volume of distribution was(0.30±0.17)L,and the drug clearance was(0.83±0.33)L/h.Conclusion The distribution of the drug in the body is basically balanced during the process of andante constant-rate intravenous infusion,and there is no interference of distribution.The measured pharmacokinetic parameters are closer to the reality.
作者
叶丹
朱青青
徐显亮
于瑞红
曹永孝
YE Dan;ZHU Qing-qing;XU Xian-liang;YU Rui-hong;CAO Yong-xiao(Department of Pharmacology,Xi'an Jiaotong University Health Science Center,Xi'an 710061,China)
出处
《西安交通大学学报（医学版）》
CAS
CSCD
北大核心
2020年第1期120-123,共4页
Journal of Xi’an Jiaotong University（Medical Sciences）
基金
国家大学生创新实验项目~~
关键词
奥美拉唑
静脉滴注
药动学参数
分布平衡
omeprazole
intravenous infusion
pharmacokinetic parameter
distribution equilibrium
作者简介
通信作者:曹永孝,教授.E-mail:yxy@xjtu.edu.cn。
