注射用兰索拉唑在健康人体内的药动学研究  

Pharmacokinetics of lansoprazole injection in healthy volunteers

作　　者：张杰[1] 何世英[1] 阳国平[2] 周彦彬[1] 田娟[1] 丁劲松[1] 

机构地区：[1]中南大学药学院,长沙410013 [2]中南大学湘雅三医院,长沙410013

出　　处：《中南药学》2011年第3期169-172,共4页Central South Pharmacy

摘　　要：目的研究兰索拉唑在健康受试者体内的药动学过程。方法采用三交叉拉丁方设计,12名健康受试者分别静脉滴注兰索拉唑15、30、60 mg（45 min滴完）,洗脱期为1周。血浆中兰索拉唑的浓度以HPLC-UV法测定,以DAS Ver 2.1计算药动学参数。结果受试者静脉滴注兰索拉唑后体内过程符合二室模型,单次给药15、30、60 mg后主要药动学参数：t1/2分别为（1.76±1.43）、（1.21±0.4）、（1.86±1.29）h,Cmax分别为（0.92±0.33）、（2.05±0.59）、（4.04±0.55）μg.mL-1,AUC0-10h分别为（3.41±2.14）、（6.25±3.55）、（11.65±5.96）μg.h.mL-1,AUC0-∞分别为（7.67±6.37）、（9.21±7.13）、（14.68±10.01）μg.h.mL-1,V分别为（5.95±5.18）、（6.32±3.74）、（5.26±6.03）L,CL分别为（3.98±4.38）、（4.81±2.18）、（5.43±2.43）L.h-1。结论中国健康受试者单剂量静脉滴注兰索拉唑后,在15~60 mg内的体内过程呈线性药动学特征。兰索拉唑在人体的代谢存在较大的个体差异,变异来源可能与CYP2C19的基因多态性有关,临床宜个体化用药。Objective To determine the pharmacokinetics in healthy volunteers following intravenous administration of lansoprazole.Methods A three-way crossover Latin square design was applied.Twelve healthy volunteers were randomized to administer a single dose of lansoprazole at 15,30 and 60 mg,respectively.Wash-out period lasted a week.The concentration of lansoprazole in human plasma was determined by HPLC-UV.The main pharmacokinetic parameters were calculated with DAS Ver 2.1.Results The pharmacokinetics of lansoprazole fit a two-compartment open model.The main parameters of a single dose were as follows（low,medium,and high）：t1/2（1.76±1.43）,（1.21±0.4）and（1.86±1.29）h;Cmax（0.92±0.33）,（2.05±0.59）and（4.04±0.55）μg·mL-1;AUC0-10h（3.41±2.14）,（6.25±3.55）and（11.65±5.96）h·μg·mL-1;AUC0-∞（7.67±6.37）,（9.21±7.13）and（14.68±10.01）μg·h·mL-1;V（5.95±5.18）,（6.32±3.74）and（5.26±6.03）L;CL（3.98±4.38）,（4.81±2.18）and（5.43±2.43）L·h-1 respectively.Conclusion The process of lansoprazole in the dosage range of 15-60 mg fits the linear dynamic feature.There are great inter-individual variations in the metabolism of lansoprazole in humans due to the close relation with the gene polymorphism of CYP2C19,which should be personalized when taking medicine.

关 键 词：兰索拉唑 药动学 高效液相色谱-紫外法 CYP2C19 

分 类 号：R969.1[医药卫生—药理学] R927.2[医药卫生—药学]