天然冰片对大鼠口服尼莫地平药代动力学的影响

Effect of Natural Borneol on Pharmacokinetics of Nimodipine in Rats after Oral Administration

目的:研究天然冰片对雄性SD大鼠口服尼莫地平药代动力学的影响。方法:大鼠随机分为3组:对照组、天然冰片临床等效剂量组(90 mg·kg-1)及高剂量组(270 mg·kg-1),在灌胃给予空白溶媒或天然冰片后各组均口服尼莫地平20 mg·kg-1,于给药前和给药后不同时间点取血,样品处理后用液相色谱-串联质谱(LC-MS-MS)法测定尼莫地平含量,采用WinNonlin 5.0.1计算药代动力学参数。结果:临床等效剂量的天然冰片对尼莫地平口服吸收无显著影响,高剂量天然冰片使血浆中尼莫地平的浓度-时间曲线下面积(AUC)增大,但与对照组间的差异无统计学意义。结论:高剂量天然冰片可轻微促进尼莫地平的口服吸收,但影响较小。

Objective： To study the effects of natural borneol （NB） on the pharmacokinetics of nimodipine in rats after oral administration. Method： The rats were randomly divided into three groups, control group, clinically-equivalent-dose group and higher-dose group, and were gavaged with NB at doses of 0, 90, 270 mg ·kg-1, respectively. After l0 min, all rats were gavaged with nimodipine at a dose of 20 mg·kg-1. The blood was obtained at different time points before and after the administration. Concentrations of nimodipine in plasma were determined by LC-MS-MS and the main pharmacokinetic parameters were calculated by WinNonlin 5.0. 1. Result： Clinically equivalent dose of NB showed little influence on the pharmaeokinetics of nimodipine. The mean value of AUC in higher-dose group was slightly higher than that in control group, but no significant differences were found between two groups. Conclusion： The results suggested that higher dose of NB may enhance the absorption of nimodipine in rats, but the enhancing effect is not very obvious.