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注射用兰索拉唑在健康人体内的药动学研究 被引量:3

Pharmacokinetics of lansoprazole injection in healthy volunteers
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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.
出处 《中南药学》 CAS 2011年第3期169-172,共4页 Central South Pharmacy
关键词 兰索拉唑 药动学 高效液相色谱-紫外法 CYP2C19 lansoprazole pharmacokinetics HPLC-UV CYP2C19
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