安搏律定非线性药物动力学研究

Non-linear Pharmacokinetic Study of Aprindine

对6例健康志愿者进行了安搏律定(AP)口服单剂量40mg、80mg、160mg 及多剂量40mgbid×7d 的药动学研究。结果:40mg、80mg、160mg 的t_(172)β分别为8.83±5.08、18.05±5.85、29.31±10.23h。以40mg 单剂量与多剂量比较部分动力学参数,后者t_(1/2)β延长(8.83±5.08至38.11±12.23h,P<0.01);CL 减慢(29.00±14.20至3.54±0.09L/h,P<0.01);AUC 增加(1.80±1.85至10.00±2.98,P<0.01)。表明AP 存在着非线性药动学。导致AP非线性动力学原因推测存在着药物代谢酶饱和的现象。

The non-linear kinetics of Aprindine(AP)was studied in 6 healthy volunteersby taking AP single doses 40mg,80mg,160mg and multiple doses 40mg×bid for 7dayt at two week intervals.By receiving AP 40mg,80mg and 160mg,t(?)β were8.83±5.08,18.07±5.85 and 29.31±10.03h,respectively.Between that of single doseAP 40mg and multiple doses AP 40mg×bid,the parial pharmacokinetic parameterswere compared.With the administration of AP,t(?)β was prolonged(8.83±5.08 to38.11±12.23h,p<0.01),CL was decreased(29.0±14.2 to 3.54±0.99 L/h,p<0.01),and AUC was increased(1.80±1.85 to 10.00±2.98μg·h/ml,p>0.01).It is mostlikely that the non-linear kinetics of AP may de due to the saturatione of thedrug metabolizing enzymes.