单剂量及多剂量口服奥扎格雷钠口服液的人体药动学研究

 目的考察奥扎格雷钠在国人中的药动学过程。方法采用双周期试验设计,选用12名健康志愿者单剂量及多剂量po200 mg奥扎格雷钠口服液,建立HPLC测定奥扎格雷钠的血药浓度并计算药动学参数,进而对主要药动学参数进行统计分析。结果单剂量与多剂量的药-时曲线均符合一级吸收的二房室开放模型,其主要药动学参数AUC_0-t分别为(3.50±0.90)与(5.87±1.18)mg·h·L^-1,AUC_0-∞分别为(3.73±0.91)与(6.32±1.29)mg·h·L^-1,ρ_max分别为(3.10±1.06)与(5.12±1.37)mg·L^-1,t_max分别为(0.42±0.12)与(0.50±0.26)h,t_1/2β分别为(0.72±0.26)与(0.75±0.99)h。结论单剂量与多剂量给药的主要药动学参数比较ρ_max,AUC_0-t,AUC_0-∞采用Excel进行成对t检验具有极显著性差异(P<0.01)。

Pharmacokinetic Study on Ozagrel in Twelve Healthy Volunteers

OBJECTIVE To study the pharmacokinetic profiles of ozagrel in healthy Chinese volunteers.METHODS In a two period study,12 healthy male volunteers received a single dose and multiple-dose regimen of 200 mg ozagrel.The plasma concentrations of ozagrel were determined by HPLC.The pharmacokinetic parameters of ozagrel were calculated and analyzed with statistical method.RESULTS The concentration-time curves of a single dose and multiple-dose regimen were fit to a two-compartment open model with first-order absorption.The main pharmacokinetic parameters of a single-dose and multiple-dose regimen were as follows:AUC_0-t(3.50±0.90)and(5.87±1.18)mg·h·L^-1,AUC_0-∞(3.73±0.91) and(6.32±1.29) mg·h·L^-1,ρ_max(3.10±1.06)and(5.12±1.37)mg·L^-1,t_max(0.42±0.12)and((0.50±0.26)h),t_1/2β(0.72±0.26) and(0.75±0.99)h,respectively.CONCLUSION The statistical analysis shows that there are significant difference after the treatment of a single dose and multiple-dose regimen.