注射用雷贝拉唑钠的人体药动学特征

目的研究注射用雷贝拉唑钠的人体药动学特征。方法 30名健康志愿者分成低（10 mg）、中（20 mg）、高（40 mg）3个剂量组,单次给药后采取8 h动态血样;中剂量组完成单次给药试验后即进入多次给药试验,采集动态血样。采用LC-MS/MS法测定血浆中雷贝拉唑的浓度,并采用DAS软件计算药动学参数。结果 30名受试者分别单次给低、中、高3个剂量后雷贝拉唑的主要药动学参数ρ_max分别为（699.89±198.89）、（1 274.82±272.99）和（2 572.00±640.57）μg·L^-1,t_max分别为（0.53±0.09）、（0.43±0.09）和（0.52±0.09）h,t_1/2分别为（1.34±0.47）、（0.97±0.29）和（1.43±0.39）h,AUC_0→8分别为（864.23±369.13）、（1 477.88±311.65）和（3 444.86±1 175.38）μg·h·L^-1,AUC_0→∞分别为（877.16±379.48）、（1 484.05±313.24）和（3 501.05±1 236.70）μg·h·L（¹）;中剂量组给药20 mg,连续7 d达稳态后的主要药动学参数ρ_max^ss为（1 299.50±290.20）μg·L^-1,t_max为（0.53±0.10）h,t_1/2为（0.89±0.29）h,AUC_0→8^ss为（1 447.08±421.03）μg·h·L^-1,AUC_0→∞^ss为（1 454.19±420.65）μg·h·L^-1,波动度DF为（22.58±5.50）%。结论在给药剂量10～40 mg内,注射用雷贝拉唑钠在健康志愿者体内呈现线性药动学特征。

Pharmacokinetic characteristics of sodium rabeprazole in humans

AIM To study the pharmacokinetics of sodium mbeprazole injection in humans. METHODS Thirty healthy volunteers were randomly divided into 3 groups who received the sodium mbepmzole injection, and the doses were 10 nag, 20 rng and 30 rag, respectively. Each volunteer＇s blood samples were collected in 8 h after the injection.The 20 nag group＇ s volunteers were given multiply dose subsequently when the first dose tests were finished and the blood samples were collected. LC-MS/MS was used to detemaine plasma concentrations of mbepmzole and pharrnacokinetic parameters were calculated by DAS software. RESULTS The main pharmacokinetic parameters of mbeprazole in the 10 mg, 20 mg and 40 mg groups were as follows： Pmax were （699.89 ±198 ： 89）, （ 1 274.82±272.99） and （2 572.00 ±640.57） ug.L-1;tmax were （0.53±0.09）,（0.43 ±0.09） and （0.52±0.09） h; t1/2 were （1.34±0.47）, （0.97 ±0.29） and （1.43± 0.39） h;AUC0→∞ were （864.23 ±369.13）, （1 477.88 ±311.65） and （3444±1175.38） ug.h.L-1; AUC0→∞ were （877.16 ±379.48）, （ 1 484.05 ±313.24） and （ 3 501.05±1 236.70）ug.h.L-1, respectively. The main pharmacokinetic parameters of 20 mg group were as follows： pmax^88 was （1 299.50±290.20） ug.L-1; tmx was （0.53±0.10） h; t1/2 was （0.89±0.29） h; AUCs was （1 447.08±421.03） ug.h.L-1; AUC0→∞ was （1 454.19＋420.65） ug.h.L^-1; DF was （22.58±5.50）%. CONCLUSION Sodium mbeprazole injection showes well linear pharmacokinetie characteristics in human body when the doses range from 10 mg to 40 mg.