酒石酸美托洛尔片在中国健康人体的药代动力学

Pharmacokinetics of metoprolol tartrate tablet in Chinese healthy volunteers

目的 研究单剂量和多剂量酒石酸美托洛尔片在中国健康人体的药代动力学。方法 22名健康受试者口服酒石酸美托洛尔片50mg,用HPLC-荧光检测法测定血浆中美托洛尔的浓度。结果 所得药代动力学参数如下。单剂量:AUC0-t为(395. 6±298. 95)ng·h·mL-1,AUC0-∞为(433. 83±342. 94)ng·h·mL-1,Cmax为(63. 06±34. 61)ng·mL-1,tmax为(1. 573±0. 52)h,MRT为(7. 40±2. 31 )h;多剂量:AUCss0-t为( 504. 67±322. 35 )ng·h·mL-1,Cmax为(77. 72±45. 69)ng·mL-1,tmax为(1. 7±0. 6)h,Cmin为(4. 12±1. 57)ng·mL-1,平均稳态血药浓度Cav是( 21. 03±13. 43 )ng·mL-1,血药浓度波动度DF为(367. 29±112. 56)%。结论 酒石酸美托洛尔片单剂量和多剂量给药后,安全性良好。

Objective To study the safety and pharmacokinetics of metoprolol tablet in Chinese healthy volunteers. Methods Twenty two Chinese healthy volunteers were given a single and multiple oral dose 50 mg of metoprolol tartrate tablets. The concentration of metoprolol in blood plasma was measured by an validated HPLC fluorescence method and were assessed with non-compartment model. Results The pharmacokinetic parameters of metoprolol tartrate tablet for orally administered were as follow: AUC 0-t was (395.6±298.95)μg·h·mL -1 , AUC 0-∞ was (433.83±342.94)ng·h·mL -1 ,C max was(63.06±34.61)ng·mL -1 ,t max was(1.573±0.52)h,MRT was(7.40±2.31)h after single dose.AUC ss 0-t was(504.67± 322.35 )ng·h·mL -1 ,C max was(77.72±45.69)ng·mL -1 ,t max was(1.7±0.6)h,C min was(4.12±1.57)ng·mL -1 ,C av was(21.03±13.43)ng·mL -1 ,DF was(367.29±112.56)% after multiple doses. No any adverse events occurred during the whole study.Conclusion There are good safety after administrating single and multiple oral dose of metoprolol tartrate.