Pharmacokinetics study of lansoprazole for injection in Chinese healthy volunteers

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;AUC0-12(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±305.1)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;CLz(11.0±4.1)L·h-1;Cav(254.0±98.4)μg·L-1.CONCLUSION Lansoprazole for injection displays linear pharmacokinetics 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.