兰索拉唑在健康受试者体内药动学和药效学  

Pharmacokinetics and pharmacodynamics of lansoprazole in the healthy volunteers

作　　者：杨远荣[1] 吴健鸿[2] 汤绍迁[1] 任贻军[1] 李华荣[1] 陈海燕[1] 高逢喜[1] 黄陵生[1] 曾繁典[2] 

机构地区：[1]华中科技大学同济医学院附属荆州医院国家药物临床试验机构,湖北荆州434020 [2]华中科技大学同济医学院临床药理研究所,湖北武汉430030

出　　处：《中国医院药学杂志》2010年第21期1813-1817,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究兰索拉唑在健康受试者体内的药动学和药效学。方法:选择健康受试者20名,男女各半,随机分为兰索拉唑组(30mg)和奥美拉唑组(40mg),给药后监测24h胃内pH,并用高效液相色谱法测定兰索拉唑和奥美拉唑血药浓度,数据分别用SPSS11.5和DAS2.0处理。结果:兰索拉唑药动学参数为AUC0-t:(7.2±3.9)mg.h.L-1;AUC0-∞(7.7±4.6)mg.h.L-1;AUMC0-t(24.0±21.2);AUMC0-∞(33.2±35.6);MRT0-t(2.8±1.1)h;MRT0-∞(3.4±1.8)h;t1/2(2.2±1.3)h;CL(5.3±3.1)L.h-1;Cmax(2.3±0.4)mg.L-1。奥美拉唑药动学参数为:AUC0-t(4.8±4.1)mg.h.L-1;AUC0-∞(4.6±4.2)mg.h.L-1;AUMC0-t(11.0±15.1);AUMC0-∞(12.2±17.1);MRT0-t:(1.8±0.8)h;MRT0-∞(1.9±0.9)h;t1/2(1.1±0.6)h;CL(13.6±7.4)L.h-1;Cmax(2.1±0.8)mg.L-1;给药后胃内pH明显升高,给药结束后12h胃内pH仍分别达(5.1±1.6)和(3.9±1.9)。结论:健康受试者体内血药浓度未能实时反映该药在人体胃组织中的浓度及抑酸效果,该药能蓄积在人体胃组织中并维持较长时间的抑酸作用。OBJECTIVE To study pharrnacokinetics and pharmacodynamics of lansoprazole in the healthy volunteers. METHODS Twenty healthy volunteers were randomly divided into two group （ lansoprazole 30 mg and omeprazole 40 mg）, with 5 males and 5 females in each group. The pH of gastric juice in healthy volunteers was monitored within 24 hours, the plasma drug concentration of lansoprazole and omeprazole was detected by HPLC. DAS2. 0 and SPSS11.5 was performed for calculat- ing pharmacokinetics parameter and comparing the data of pH. RESULTS The main pharmacokinetic parameters of lanso- prazole was as follows .AUG0-t（7.2±3.9）mg·h·L-1;AUC0-∞（7.7±4.6）mg·h·L-1;AUMG0（24.0±21.2）;AUMG0-∞（33.2±35.6）;MRT0-t（2.8±1.1）h;MRT0-∞（3.4±1.8）h;t1/2（2.2±1.3）h;CL（5.3±3.1）L·h-1;Cmax（2.3±0.4）mg·L-1.The main pharmacokinetic parameters of omeprazole was as follows：AuCp-t（4.8±4.1）mg·h·L-1;AUG0-∞（4.6±4.2）mg·h·L-1;AUMC0-t （11.0±15.1）;AUMG0-∞（12.2±17.1）;MRT0-t（1.8±0.8）h;MRT0-∞（1.9±0.9）h;t1,2（1.1±0.6）h;CL（13.6±7.4）L·h-1;Cmax（2.1±0.8）mg·L-1;. The pH value of gastric juice was rising significantly after single intravenous lansoprazole or omeprazole application,and maintained the pH at （5. 1 ± 1.6）and（3. 9± 1.9）twelve hours later. CONCLUSION The plasma drug concentration was different from the tissue drug concentration,and uncorrelated with the pH. The effect of lansoprazole was cumulative over extended periods.

关 键 词：兰索拉唑 药动学 药效学 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]