单剂量静脉滴注兰索拉唑在中国健康人体的药代动力学  

Pharmacokinetics of lansoprazole injection after a single dose in Chinese healthy volunteers

作　　者：高晨[1] 赵志刚[1] 司延斌[1] 孙浩[1] 刘腾[1] 张相林[2] 刘晓[2] 

机构地区：[1]首都医科大学附属北京天坛医院药剂科,北京100050 [2]卫生部中日友好医院,北京100029

出　　处：《中国临床药理学杂志》2010年第4期263-266,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究中国健康志愿者单次静脉滴注兰索拉唑(抑胃酸药)的药代动力学特点。方法 12名健康志愿者,先后单次静滴3个剂量(15,30,60mg)兰索拉唑;用高效液相色谱-紫外检测法测定给药后不同时间点的血药浓度,用3P97软件计算药代动力学参数。结果血药浓度-时间曲线符合二房室模型,健康受试者单次静滴3个剂量(15,30,60mg)兰索拉唑后主要的药代动力学参数:Cmax分别为(1105.65±506.24),(2171.33±799.02),(4070.53±643.04)μg·L-1;t1/2分别为(1.63±0.86),(2.30±2.01),(1.90±1.19)h;AUC0-12分别为(991.16±814.49),(3495.87±1770.92),(8351.14±2599.90)μg·h·L-1。结论兰索拉唑的体内过程在男女性别间无显著差异,剂量在15～60mg内较安全。Objective To study the pharmacokinetics of lansoprazole injection with a single intravenous injection administration using a constant speed in Chinese healthy volunteers. Methods Twelve healthy volunteers were enrolled and each of whom was administered with single dose of 15,30,and 65 mg lansoprazole injection in 3 cross periods. The plasma concentrations of lansoprazole were determined by HPLC - UV. The pharmacokinetic parameters of three dose （ 15, 30, 65 mg） lansoprazole were calculated by 3P97 software. Results The plasma concentration - time curve fits two compartment model. After single iv dose of 15,30 ,and 65 mg lansoprazole injection, 12 volunteers, the main pharmacokinetic parameters of three doses （15, 30, 60 mg）lansoprazole were as follows： Cmax were （1105.65 ±506.24）, （2171.33 ±799.02）, （4070.53 ± 643.04） ug . L-1; t1/2 were （1.63 ±0. 86）, （2.30 ±2.01）, （1.90 ± 1. 19） h; AUC0-12 were （991.16 ± 814. 49）, （3495.87 ± 1770. 92）, （8351.14 ± 2599.90） ug . h. L-1 respectively. Conclusion After administration of single -dose lansoprazole, it was safe within the dosage ranged from 15 to 60 mg, and there was no significant difference of physiological disposition between the male and female.

关 键 词：兰索拉唑 高效液相色谱-紫外法 药代动力学 

分 类 号：R975.2[医药卫生—药品] R969.1[医药卫生—药学]