1,6-二磷酸果糖镁在大鼠体内的药动学研究

目的研究大鼠静脉注射不同剂量 1,6 二磷酸果糖镁 (FDP Mg)后的药动学。方法大鼠 2 0只随机分成 2组 ,分别静脉注射FDP Mg 10 0、2 0 0mg/kg ,在设定的时间点采血 ,测定血清中的FDP及Mg2 + 浓度 ,DAS程序计算药动学参数。结果大鼠静脉注射FDP Mg后 ,Mg2 + 血药浓度 时间曲线符合二室开放模型。其t1/2α为 0 .12～ 0 .14h ,t1/2 β为 1.78～ 1.89h ,分布容积 (V)为 3.2 6～ 4 .5 7L/kg ,显示非剂量依赖性特征。FDP在血清中代谢迅速 ,消除半衰期t1/2el为 0 .0 5 7～ 0 .0 86h ,平均滞留时间 (MRT)为 0 .0 90～ 0 .12 4h ,血浆清除率 (Cl)为 3.4 8～ 3.77L/ (kg·h)。结论FDP和Mg2 + 的药动学特征差异明显 ,表明FDP Mg在体内解离成FDP和Mg2 + 两部分后按照各自的代谢特征从体内消除。

Pharmacokinetics of fructose 1,6 diphosphate magnesium in rats

PurposeThe aim is to study the pharmacokinetics of iv fructose 1,6 diphosphate magnesium in Wistar rats.Methods20 Wistar rats was divided into 2 groups. A single dose of 100,200 mg/kg of fructose 1,6 diphosphage magnesium(FDP-Mg) was given by iv. Serial blood samples were collected at designed time points. The serum FDP concentration was measured by enzymology method and serum Mg 2+ concentration was detected by serum Mg 2+ determined kit. Pharmacokinetic parameters were computerized using DAS program.ResultsAfter intravenous injection of single dose FDP-Mg, the serum concentration versus time curves of Mg 2+ conformed to two-compartment model. t 1/2α was 0.12～0.14 h,t 1/2β was 1.78～1.89 h and Vd was 3.26～4.57 L/kg.The main pharmacokinetic parameters of FDP were different from those of Mg 2+.Non-compartment model was used to calculate the main pharmacokinetic parameters of FDP. t 1/2el was 0.057～0.086 h,MRT was 0.090～0.124 h and Cl was 3.48～3.77 L/(kg·h).ConclusionThe difference of the parameters between FDP and Mg 2+ suggested that FDP-Mg could be divided into two parts, and then, they could be eliminated from the organism taking their own routes.