论文部分内容阅读
目的:研究10名健康志愿者按单剂量和多剂量静脉滴注异甘草酸镁100mg后的药动学特性。方法:多剂量给药方案为每日1次,连续9d。采用高效液相色谱法测定异甘草酸镁的血药浓度。色谱条件包括:HypersilODS2色谱柱(5μm,300mm×4.6mm),流动相为0.23mol·L-1磷酸盐 缓冲液(pH=7.4)∶乙腈=79∶21,柱温40°C,流速 为1.0mL·min-1,紫外检测波长为250nm。数据 用3P87软件处理,按二室模型拟合并求算药动学参 数。结果:单剂量给药后的药动学参数分别为:cmax=(29±3)mg·L-1;t12α=(1.72±0.27)h; t12β=(23±3)h;AUC0～72(以梯形法计算)=(448±75)mg·L-1·h-1。多剂量给药达稳态后的药动 参数分别为:cssmin=(13±3)mg·L-1;cssmax=(43± 6)mg·L-1;cav=(21±4)mg·L-1;t12α=(1.6± 0.4)h;t12β(24±4)h;AUCss0～τ=(513± 108)mg·L-1·h-1。结论:该药在人体内的分布和 消除速度不随连续给药而变化。
Objective: To investigate the pharmacokinetic characteristics of 10 healthy volunteers by single-dose and multiple-dose intravenous infusion of magnesium isoglycyrrhizinate 100mg. Methods: The multi-dose regimen was once daily for 9 days. Determination of plasma concentration of magnesium isoglycyrrhizinate by high performance liquid chromatography. Chromatographic conditions include: Hypersil ODS2 column (5 μm, 300 mm × 4.6 mm) with a mobile phase of 0.23 mol·L -1 phosphate buffer (pH = 7.4): acetonitrile = 79:21, column temperature 40 ° C and flow rate 1.0 mL · min-1, UV detection wavelength of 250nm. Data were processed using 3P87 software and fitted to two compartment models to calculate pharmacokinetic parameters. RESULTS: The pharmacokinetic parameters after single-dose administration were cmax = (29 ± 3) mg · L-1; t12α = (1.72 ± 0.27) h; t12β = (23 ± 3) h; AUC0-72 Calculated by trapezoidal method) = (448 ± 75) mg · L-1 · h-1. The pharmacokinetic parameters after multi-dose administration reached steady state were as follows: cssmin = (13 ± 3) mg · L-1; cssmax = (43 ± 6) mg · L-1; L-1; t12α = (1.6 ± 0.4) h; t12β (24 ± 4) h; AUCss0 ~ τ = (513 ± 108) mg · L-1 · h-1. Conclusion: The drug distribution in the human body and the elimination rate does not change with continuous administration.