异甘草酸镁单剂量与多剂量静脉滴注的药动学(英文)  

Pharmacokinetics of magnesium isoglycyrrhizinate after a single and multiple intravenous dose in healthy volunteers

作　　者：沈金芳[1] 孙黎[1] 李端[2] 

机构地区：[1]上海第二医科大学附属仁济医院临床药学研究室,上海200001 [2]复旦大学药学院药理教研室,上海200032

出　　处：《中国新药与临床杂志》2005年第2期85-89,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：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。AIM: To study the pharmacokinetics of magnesium isoglycyrrhizinate (MgIG), which was diluted by 5 % glucose injection in a total volume of 250 mL, after a single and multiple intravenous dose in 10 healthy volunteers. METHODS: MgIG 100 mg once daily for 9 d in the multiple-dose regiment. Plasma MgIG concentrations are measured using high performance liquid chromatography (HPLC). Waters HPLC instrument was used with the Hypersil ODS2 C18 (5 μm, 300 mm×4.6 mm) column. The mobile phase was composed of 0.23 mol·L -1 phosphate buffer (pH=7.4)∶acetonitrile (79∶21). Flow rate was 1.0 mL·min -1 and column temperature was maintained at 40 °C. The UV detector was set at 250 nm. The concentration-time curves of MgIG were fitted to a two-compartment open model. RESULTS: The pharmacokinetic parameters obtained from the single-dose study were as follows: c max=(29±s 4) mg·L -1;t 12α= (1.72±0.27) h;t 12α=(23±3) h and AUC 0-72= (448±75) mg·h·L -1. The steady-state pharmacokinetic parameters were: c ss min=(13±3) mg·L -1; c ss max= (42±6) mg·L -1;c av=(21±4) mg·L -1; t 12α=(1.6±0.4) h;t 12β=(24±4) h and AUC ss 0-24= (513±108) mg·h·L -1. CONCLUSION:The distribution and elimination rate of MgIG were not changed after multiple intravenous administration.

关 键 词：药动学 色谱法 高压液湘 人类实验 异甘草酸镁 

分 类 号：R969.1[医药卫生—药理学] R975.5[医药卫生—药学]