摘要
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），1738．5±263．8），（3609．4±421．6）μg·L^-1；AUC0-12为（2873．9±2065．4），（3366．2±1138．9），（12321．1±5632．5）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（1530．2±305．1）μg·L^-1；AUG0-12为（3048．1±1181．0）μg·h·L^-1；AUC。；为（3048．1±1181．0）μg·h·L^-1；t1／2：为（1．3±0．3）h；CL。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 Chinese healthy volunteers. METHODS 30 healthy volunteers were randomly into 3 groups, with 5 males and 5 females in each group. The volunteers in three groups were administrated with single dose of lansoprazole 15, 30, and 60 mg, respectively. Those who got the dose of 30 mg were administrated twice daily till 5th day. The concentrations of lansoprazole in plasma were determined by LC-MS/MS while the pharmacokinetics parameters were calculated by DAS software. RESULTS The main pharmacokinetic parameters of lansoprazole after single-dose IV administration were as follows： tmax （0. 67 ± 0. 00）, （0. 67 ± 0. 00）, （0. 73 ± 0. 09）h; Cmax （857. 1 ± 251.2）, （ 1 738. 5 ± 263. 8）, （3 609. 4± 421.6）μg·L^-1 ; AUG0-12 （2 873. 9 ± 2 065.4）, （3 366. 2 ± 1 138. 9）, （ 12 321.1 ± 5 632. 5）μg·h·L^-1 ; t1/2 （2. 5 ± 1.8）, （1.4 ± 0. 4）, （3. 0 ± 1.8）h. The main pharmacokinetic parameters of lansoprazole after multiple-dose administration were as follows： tmax （0. 70 ± 0. 07）h; Cmax （1 530. 2 ± 305. ] μg·L^-1 ; AUC0-12 （3 048. 1 ± 1 181.0）μg·h·L^-1 ; AUCSS（3 048. 1 ± 1 181.0）μg·h·L^-1;t1/2z（1.3±0. 3）h;CL,（11.0±4. 1）μg·h·L^-1; CL2（254. 0±98. 4）μg·L^-1. CONCLUSION Lansoprazole for injection displays linear pharmaeokineties in the dose range of 15 to 60 mg after single intravenous doses. No significant differences between genders are observed. There is no significant accumulation of lansoprazole in healthy volunteers with repeated dosing.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第4期280-283,共4页
Chinese Journal of Hospital Pharmacy
