兰索拉唑肠溶胶囊在健康人体的生物等效性  

Bioequivalence of lansoprazole enteric caspsules in healthy volunteers

作　　者：魏敏吉[1] 赵彩芸[1] 齐慧敏[1] 张朴[1] 刘燕[1] 张曼[1] 张薇[1] 吕媛[1] 

机构地区：[1]北京大学第一医院临床药理研究所,北京100034

出　　处：《中国临床药理学杂志》2011年第1期24-28,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价2种国产兰索拉唑肠溶胶囊制剂(抗溃疡药)的生物等效性。方法 24例健康成年男性受试者随机分组,按照自身对照的方法单次口服兰索拉唑肠溶胶囊30 mg,用LC-MS/MS测定兰索拉唑和其代谢物5-羟基兰索拉唑、兰索拉唑砜的浓度,用非房室模型方法计算主要药代动力学参数。结果参比制剂和试验制剂的主要药代动力学参数如下。兰索拉唑:t1/2分别为(2.10±1.58),(2.18±1.85)h;tmax分别为(2.20±1.10),(2.00±1.01)h;Cmax分别为(1160.8±550.3),(1232.3±628.1)ng.mL-1;AUC0-t分别为(4963.7±4233.4),(4947.0±4669.3)ng.mL-1.h;AUC0-∞分别为(5027.4±4256.9),(5036.0±4751.2)ng.mL-1.h。5-羟基兰索拉唑:t1/2分别为(1.95±1.20),(1.75±1.00)h,tmax分别为(2.10±1.20),(1.80±1.00)h,Cmax分别为(106.2±61.2),(114.5±61.0)ng.mL-1,AUC0-t分别为(279.1±124.2),(277.2±127.2)ng.mL-1.h,AUC0-∞分别为(292.3±122.7),(286.7±124.6)ng.mL-1.h。兰索拉唑的生物利用度为(111.5±54.7)%。结论试验制剂和参比制剂为生物等效性制剂,2种制剂服用安全,耐受性良好。Objective To study the bioequivalence of lansoprazole enteric easpsules in healthy volunteers. Methods A single oral dose of 30 mg lansoprazole was given to 24 healthy volunteers in an open randomized crossover design. The concentrations of lansoprazole and its metabolites, 5 -hydroxy lansoprazole and lansoprazole sulfone in plasma, were simultaneously determined by a validated LC - MS/MS method. The pharmacokinetic parameters were calculated based on non - compartment model. Results The main pharmacokinetic parameters of lansoprazole for reference and test preparations were as following： t1/2 were （2. 10 ± 1.58） , （2. 18 ± 1.85） h;tmax were （2.20 ± 1.10 ）, （2.00 ±1.01） h;Cmax were （1160. 8 ±550. 3） , （1232. 3 ±628.1 ） ng · mL^-1 ;AUC0-1 were （4963.7 ±4233.4） , （4947.0 ±4669.3） ng · mL^-1· h;AUC0-1 were （5027.4 ± 4256.9）, （5036.0 ± 4751.2） ng · mL^-1· h, respectively. Main pharmaeokinetic parameters of 5 - hydroxy lansoprazole for refer- ence and test preparation were as follow： t1/2 were （1.95 ± 1.20 ）, （1.75±1.00） h,tmax were （2. 10±1.20）, （1.80±1.00） h,Cmax were （106.2±61.2）, （114.5±61.0） ng · mL^-1,AUC0-1 were （279.1 ± 124.2） , （277.2 ± 127.2 ） ng · mL^-1· h,AUC0-1 were （292.3 ±122.7）, （286.7 ± 124.6） ng· mL^-1· h, respectively. The relative bioavalability of lansoprazole was （111.5 ± 54.7） %. Conclusion The results demonstrated that the two preparations of lansoprazole were bioequivalent.

关 键 词：兰索拉唑 5-羟基兰索拉唑 兰索拉唑砜 生物等效性 药代动力学 液相色谱-串联质谱 

分 类 号：R969.1[医药卫生—药理学] R975.6[医药卫生—药学]