盐酸美金刚片在中国健康人体的生物等效性

Study on the bioequivalence of memantine hydrochloride tablets in Chinese healthy volunteers

目的:评价国产与进口盐酸美金刚片在中国健康人体的生物等效性。方法:20名健康男性受试者随机交叉单剂量口服受试制剂或参比制剂盐酸美金刚片各10mg。用高效液相色谱-串联质谱法测定血浆中美金刚浓度;用DAS3.0软件计算药动学参数,并对两种药物进行生物等效性评价。结果:受试制剂和参比制剂的主要药动学参数:Cmax分别为(18.1±3.8)和(20.3±4.2)ng·mL-1;tmax分别为(12.7±15.1)和(8.8±3.0)h;t1/2分别为(60.8±15.5)和(61.4±19.2)h;AUC0-t分别为(1 748.6±338.9)和(1 720.2±317.3)ng·h·mL-1。AUC0-t、AUC0-∞、Cmax的90%置信区间分别为89.8%～105.6%、89.7%～106.1%、84.8%～93.9%。受试制剂相对生物利用度F0-t为(95.5±2.9)%。结论:受试制剂与参比制剂具有生物等效性。

OBJECTIVE To evaluate the bioequivalence of two preparations of memantine hydrochloride in healthy volunteers. METHODS A single oral dose of 10 mg test preparation or reference preparation memantine hydrochloride tablets were given to 20 male healthy volunteers in a randomized crossover study. The concentrations of mernantine were determined by HPLC-MS/MS meth od. The pharmacokinetic parameters and relative bioavailability were calculated by DAS 3. 0 software, and then the bioequivalence was judged. RESULTS The main pharmacokinetic parameters of test preparation and reference preparation were as follows： Cmax was （18. 1 ±3.8）, （20.3±4.2） ng·mL^-1 ; tmax was （12.7±15.1）, （8.8±3.0） h; t1/2 was （60.8± 15.5）, （61.4±19.2） h; AUGht was （ 1 748. 6 ±338. 9）, （1 720. 2 ± 317. 3） ng. h· mL^- 1 , respectively. The 900/o CIs for the ratios of AUGht ,AUG0-t ,Cmax were 89. 8% - 105.6 %,89. 7 % ~ 106. 1%0,84. 8 % ~ 93. 9%, respectively. The relative bioavailability of test preparation was （95. 5 ± 2. 9） %. CONCLUSION The results demonstrated that the two preparations were bioequivaient.