替普瑞酮在大鼠体内的药动学研究

Study on the pharmacokinetics of Teprenone in rats

目的采用RP-HPLC法测定大鼠血浆中替普瑞酮浓度并用于大鼠药物动力学的研究。方法血浆样品用叔丁醚萃取,采用HPLC法测定。将大鼠分为高、中、低剂量组,ig给药后测定血药浓度,绘制药-时曲线,计算药动学参数。结果替普瑞酮在大鼠体内代谢符合一室模型,3种剂量的消除半衰期无统计学差异;随着剂量的增加Cmax和AUC存在剂量依耐性,且Cmax和AUC与剂量间呈线性相关。结论所用方法简便、灵敏、准确,适用于替普瑞酮的药动学研究。

OBJECTIVE To establish an HPLC method for quantitative determination of Teprenone and to apply it to the study on pharmacokinetics in rats.METHODS The sample was extracted with tert-butylmethylether and was determined by HPLC.Three dose groups were adopted to the pharmacokinetic experiment.Concentration-time curves were obtained and the pharmacokinetic parameters were calculated.RESULTS One-compartment model was best fit to the plasma concentration-time curves of three groups and there was no significant differences in t1/2,β among the 3 groups.AUC and Cmax increased proportionally with the dose.CONCLUSION This method is simple,sensitive,accurate and reproducible.It is applicable to the pharmacokinetic study of Teprenone.