马来酸咪达唑仑片在汉族健康人体内的药动学研究

Pharmacokinetics of Midazolam Tablets in Han Healthy Volunteers

目的:研究马来酸咪达唑仑片在汉族健康人体内的药动学。方法:10名汉族健康受试者口服马来酸咪达唑仑片15mg后,用高效液相色谱法测定咪达唑仑血药浓度,用DAS2.0药动学软件拟合药动学参数。结果:受试者单剂量口服马来酸咪达唑仑片后的主要药动学参数分别为Cma(x103.11±26.37)ng·mL-1、tma(x1.52±0.75)h、t1/(22.96±0.77)h、Vz/F(170.08±50.97)L、CL/F(41.05±12.33)L·h-1、AUC0～1(2368.80±103.37)ng·h·mL-1、AUC0～∞(397.29±124.06)ng·h·mL-1。部分受试者的药-时曲线存在双峰现象。结论:咪达唑仑片的药动学参数个体差异较大,临床应用时应注意个体化给药。

OBJECTIVE： To study the pharmacokinetics of midazolam tablets in Hart healthy volunteers. METHODS： 10 healthy volunteers enrolled in the study received a single oral dose of 15 mg midazolam tablets. The plasma concentration was determined by HPLC and the pharmacokinetic parameters were calculated by DAS2.0 software. RESULTS： The main pharmacokinetic parameters were as follows： Cmax（103.11±26.37）ng·mL^-1、tmax（1.52±0.75）h、t1/2（2.96±0.77）h、V2/F（170.08±50.97）L、CL/F（41.05±12.33）L·h^-1、AUC0-12（368.80±103.37）ng·h·mL^-1、AUC0-∞（397.29±124.06）ng·h·mL^-1. There were double peaks in plasma concentration-time profile in part of volunteers. CONCLUSION： Midazolam should be used by means of individualized administration because of significant individual variability in pharmacokinetics.