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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 study the pharmacokinetics of two formulations of clevidipine butyrate in rats. Methods Twenty-four rats were randomly divided into four groups. The low, medium and high dose of clevidipine butyrate test preparation and reference preparation were respectively administered intravenously. The determination of clevidipine butyrate The pharmacokinetic parameters were calculated and their pharmacokinetic characteristics in rats were evaluated. Results The main pharmacokinetic parameters of low, medium and high doses of test and reference preparations in rat plasma were Cmax 46.16 ± 10.65,82.99 ± 9.34,177.80 ± 38.32,80.31 ± 3.04 ng · m L-1; AUC0-t were 2.309 ± 0.628,4.221 ± 0.988,9.339 ± 1.759,3.968 ± 0.411 min · μg · m L-1 respectively; t1 / 2 was 12.20 ± 4.65,16.74 ± 6.93,15.13 ± 4.81, 18.34 ± 4.43 min. Conclusion There was no significant difference in the pharmacokinetic parameters of clevidipine butyrate and reference preparations in rats. The test formulation showed non-linear kinetic characteristics in the range of 0.36-3.24 mg · kg-1.