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目的:研究注射用兰索拉唑在健康人体内的药动学特征。方法:30名健康受试者随机分为3组,男女各半,分别静脉滴注兰索拉唑15,30,60mg,进行低、中、高单剂量药动学研究。30mg剂量组并进行多剂量药动学研究。采用LC-MS/MS测定血浆中兰索拉唑的浓度。应用DAS2.1.1软件计算药动学参数。结果:30名健康受试者分别单次静脉滴注注射用兰索拉唑15,30,60mg的主要药动学参数如下tmax为(0.67±0.00),(0.67±0.00),(0.73±0.09)h;Cmax为(857.1±251.2),1 738.5±263.8),(3 609.4±421.6)μg.L-1;AUC0-12为(2 873.9±2 065.4),(3 366.2±1 138.9),(12 321.1±5 632.5)μg.h.L-1;t1/2为(2.5±1.8),(1.4±0.4),(3.0±1.8)h。多次给药的主要药动学参数如下tmax为(0.70±0.07)h;Cmax为(1 530.2±305.1)μg.L-1;AUC0-12为(3 048.1±1 181.0)μg.h.L-1;AUCSS为(3 048.1±1 181.0)μg.h.L-1;t1/2z为(1.3±0.3)h;CLz为(11.0±4.1)L.h-1;Cav为(254.0±98.4)μg.L-1。结论:注射用兰索拉唑单剂量静脉滴注后在15~60mg剂量范围内呈线性动力学特征;性别对注射用兰索拉唑的体内药动学无差异;连续给药后在体内无蓄积。
Objective: To study the pharmacokinetics of lansoprazole for injection in healthy volunteers. Methods: Thirty healthy subjects were randomly divided into 3 groups, male and female in half, respectively, intravenous lansoprazole 15,30,60 mg, low, medium and high single dose pharmacokinetic studies. 30mg dose group and multi-dose pharmacokinetic study. Plasma concentrations of lansoprazole were determined by LC-MS / MS. Pharmacokinetic parameters were calculated using DAS2.1.1 software. Results: The main pharmacokinetic parameters of 30, 60 and 60 mg single-dose intravenous injection of lansoprazole in 30 healthy volunteers were as follows: tmax was (0.67 ± 0.00), (0.67 ± 0.00), (0.73 ± 0.09 ) h; Cmax was (857.1 ± 251.2), 1 738.5 ± 263.8), (3 609.4 ± 421.6) μg.L-1; AUC0-12 was (2 873.9 ± 2 065.4), (3 366.2 ± 1 138.9) 12 321.1 ± 5 632.5) μg.hL-1; t1 / 2 was (2.5 ± 1.8), (1.4 ± 0.4), (3.0 ± 1.8) h. The main pharmacokinetic parameters of multiple administrations were as follows: tmax was (0.70 ± 0.07) h; Cmax was (1 530.2 ± 305.1) μg.L-1; AUC0-12 was (3 048.1 ± 1 181.0) μg.hL- ; AUCSS was (3 048.1 ± 1 181.0) μg.hL-1; t1 / 2z was (1.3 ± 0.3) h; CLz was (11.0 ± 4.1) Lh-1; Cav was 254.0 ± 98.4 μg.L-1 . CONCLUSION: Lansoprazole injection has a linear kinetic characteristic within 15-60mg dose range after single-dose intravenous drip infusion. There is no difference in the pharmacokinetics of lansoprazole for injection after inoculation in vivo Accumulation.