盐酸美金刚胶囊人体药代动力学研究

Pharmacokinetics of memantine hydrochloride capsule in Chinese healthy volunteers

目的:进行健康志愿者盐酸美金刚胶囊单次和多次口服的药代动力学研究。方法:采用高效液相色谱串联质谱法测定美金刚血浓度,以DAS2.0计算其药代动力学参数。结果:盐酸美金刚胶囊5、10和15 mg单次口服,美金刚药代动力学参数tmax为(5.6±1.2)、(5.2±2.0)和(4.9±1.1)h;Cmax为(4.4±0.9)、(8.9±1.6)和(16.5±2.8)ng/mL;t1/2为(47±10)、(47±9)和(51±9)h。10 mg多次口服,美金刚药代动力学参数tmax为(6.0±1.4)h,Cmax为(31.8±6.0)ng/mL,t1/2为(46±8)h。结论:美金刚单次给药,Cmax和AUC有良好剂量相关性;多次给药可发生蓄积。

AIM：To study the pharmacokinetics of memantine in healthy Chinese volunteers after single and multiple doses of memantine hydrochloride capsule.METHODS：The concentration of memantine in human plasma was determined by HPLC-MS/MS method and its pharmacokinetic parameters were calculated by DAS 2.0.RESULTS：The main pharmacokinetic parameters of memantine after single oral dose of 5,10,15 mg memantine hydrochloride capsule were as follows： tmax were（5.6±1.2）,（5.2±2.0） and（4.9±1.1） h.Cmax were（4.4±0.9）,（8.9±1.6） and（16.5±2.8） ng/mL,t1/2 were（47±10）,（47±9）and（51± 9） h,and after multiple oral dose of 10 mg memantine hydrochloride capsule were as follows： tmax was（6.0±1.4） h,Cmax was（32±6） ng/mL,t1/2（46±8）h.CONCLUSION：A dose relationship of Cmax and AUC existed after single oral doses of 5,10 and 15 mg memantine hydrochloride capsule.There is accumulation after a multiple dose of 10 mg once daily administration.