Aim To investigate the pharmacokinetics of levosimendan administered as intravenous injection in Chinese healthy volunteers. Methods Twelve subjects were randomly divided into three groups. Each subject in the group 1...Aim To investigate the pharmacokinetics of levosimendan administered as intravenous injection in Chinese healthy volunteers. Methods Twelve subjects were randomly divided into three groups. Each subject in the group 1 was administered at a single dose of 6 μg·kg^-1 levosimendan by intravenous bolus injection within 10 min, and then followed by intravenous infusion for 4 h at a dose per minute of 0.05 μg·kg^-1·min^-1. Similarly, each subject in the group 2 （or group 3） was given by intravenous bolus injection at a dose of 12 μg·kg^-1 （or 18 μg·kg^-1） followed by an infusion at a dose of 0.10 μg·kg^-1·min^-1 （or 0.15 μg·kg^-1·min^-1） levosimendan. Blood samples were collected at 0 （prior to dosing）, 0.17, 0.5, 1, 2, 3, 4, 4.25, 4.5, 4.75, 5, 5.5, 6, 7, 8 and 10 h after administrations. Levosimendan concentrations in plasma were measured by LC-MS/MS method. The pharmacokinetic parameters were calculated using a software Drug and Statistic （version 2.0）. Results After administrations of levosimendan at various dose levels, the half-life （t1/2） values were 1.50 ± 0.35, 1.64 ± 0.25 and 1.54 ± 0.39 h; the maximal concentrations after injections （Co） were 9.54 ± 3.90, 15.95 ± 7.84 and 28.46 ± 10.74 ng·mL^-1; the areas under concentration-time （AUCo-t （t=7.8）） were 33.63± 9.34,54.39 ± 15.34 and 78.36 ± 23.74 ng ·mL^-1·h, respectively. Conclusion The C0 and A UC0-tvalues of levosimendan exhibited a dose-dependent manner, respectively. No differences in the pharmacokinetic parameters were observed between male and female Chinese subjects.展开更多
文摘Aim To investigate the pharmacokinetics of levosimendan administered as intravenous injection in Chinese healthy volunteers. Methods Twelve subjects were randomly divided into three groups. Each subject in the group 1 was administered at a single dose of 6 μg·kg^-1 levosimendan by intravenous bolus injection within 10 min, and then followed by intravenous infusion for 4 h at a dose per minute of 0.05 μg·kg^-1·min^-1. Similarly, each subject in the group 2 （or group 3） was given by intravenous bolus injection at a dose of 12 μg·kg^-1 （or 18 μg·kg^-1） followed by an infusion at a dose of 0.10 μg·kg^-1·min^-1 （or 0.15 μg·kg^-1·min^-1） levosimendan. Blood samples were collected at 0 （prior to dosing）, 0.17, 0.5, 1, 2, 3, 4, 4.25, 4.5, 4.75, 5, 5.5, 6, 7, 8 and 10 h after administrations. Levosimendan concentrations in plasma were measured by LC-MS/MS method. The pharmacokinetic parameters were calculated using a software Drug and Statistic （version 2.0）. Results After administrations of levosimendan at various dose levels, the half-life （t1/2） values were 1.50 ± 0.35, 1.64 ± 0.25 and 1.54 ± 0.39 h; the maximal concentrations after injections （Co） were 9.54 ± 3.90, 15.95 ± 7.84 and 28.46 ± 10.74 ng·mL^-1; the areas under concentration-time （AUCo-t （t=7.8）） were 33.63± 9.34,54.39 ± 15.34 and 78.36 ± 23.74 ng ·mL^-1·h, respectively. Conclusion The C0 and A UC0-tvalues of levosimendan exhibited a dose-dependent manner, respectively. No differences in the pharmacokinetic parameters were observed between male and female Chinese subjects.
