丁酸氯维地平静脉注射乳剂在大鼠体内的药动学研究  

Study on the pharmacokinetics of Clevidipine butyrate injectable emulsion in rats

作　　者：郭军[1] 贺明 王凌[1] 赵萍[1] 蒋学华[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]成都蓉药集团四川长威制药有限公司,四川乐山614000

出　　处：《华西药学杂志》2015年第2期216-218,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的研究两种丁酸氯维地平制剂在大鼠体内的药动学特点。方法将24只大鼠随机均分为4组,分别静脉滴注低、中、高剂量的丁酸氯维地平受试制剂及参比制剂,采用HPLC法测定全血中的丁酸氯维地平,计算药动学参数,评价其在大鼠体内的药动学特点。结果丁酸氯维地平低、中、高剂量受试制剂和参比制剂在大鼠血浆中的主要药动学参数为：Cmax分别为46.16±10.65、82.99±9.34、177.80±38.32、80.31±3.04 ng·m L^-1;AUC0-t分别为2.309±0.628、4.221±0.988、9.339±1.759、3.968±0.411 min·μg·m L^-1;t1/2分别为12.20±4.65、16.74±6.93、15.13±4.81、18.34±4.43 min。结论丁酸氯维地平受试制剂和参比制剂在大鼠体内药动学参数差异无统计学意义,受试制剂在0.36-3.24 mg·kg-1剂量范围内呈非线性动力学特征。OBJECTIVE To investigate the pharmacokinetics of two kind of different Clevidipine butyrate injectable emulsions in rats. METHODS 24 rats were randomly divided into four groups and were respectively given test（ high, medium and low dose） and reference formulations. The blood concentration of Clevidipine butyrate was determined by HPLC method, and the pharmacokinetic parameters were calculated and the pharmacokinetic characteristics in rats was evaluated. RESULTS The main pharmacokinetic parameters of low, medium and high - dose test and reference formulation were as follows ： Cmax were 46.16±10.65、82.99±9.34、177.80±38.32、80.31±3.04 ng·m L^-1;AUC0-t, respectively. The A UCo were2.309±0.628、4.221±0.988、9.339±1.759、3.968±0.411 min·μg·m L^-1;respectively.The t1/2 ,respectively. The t1 /2 were 12.20±4.65、16.74±6.93、15.13±4.81、18.34±4.43 min min. CONCLUSION There is no significant difference between clevidipine butyrate test and reference formulation in rats. The pharmacokinetics characteristics of Clevidipine butyrate test formulation belong to nonlinear kinetics in the dose range of 0.36 - 3.24 rag. kg^- 1 in rats.

关 键 词：丁酸氯维地平 药动学 非线性动力学 高效液相色谱法 静脉注射乳剂 

分 类 号：R917[医药卫生—药物分析学]