2种盐酸美金刚片的人体生物等效性研究

目的:评价2种不同厂家盐酸美金刚片的生物等效性。方法:采用标准二阶段交叉设计自身对照试验方案,将20名健康男性受试者随机分为2组,分别单剂量口服盐酸美金刚片受试制剂(国产)或参比制剂(进口)10mg后,用液-质联用(LC-MS)法测定血浆中美金刚浓度,以DAS2.0软件计算药动学参数。结果:20名健康受试者单剂量口服受试制剂或参比制剂后,药动学参数分别为:t1/2(69.77±14.61)、(76.06±17.92)h,tmax(5.15±1.18)、(5.05±1.36)h,cmax(13.64±3.28)、(13.34±4.18)μg·mL-1,AUC0～240h(857.73±164.45)、(888.16±316.00)μg·h·mL-1,AUC0～∞(940.00±180.70)、(999.00±346.40)μg·h·mL-1。与参比制剂比较,受试制剂的生物利用度为104.2%。结论:2种盐酸美金刚片生物等效。

Study on Bioequivalence of 2 Kinds of Memantine Tablets in Healthy Volunteers

OBJECTIVE:To evaluate the relative bioavailability and bioequivalence of 2 kinds of Memantine tablets from different manufacturers.METHODS:In standard two step cross-design self-controlled trials,20 healthy male volunteers were randomly divided into 2 groups.2 groups orally took a single dose of 10 mg tablets of the test preparation (domestic tablet) and reference preparation (imported tablet).The plasma concentration of memantine was determined by LC-MS,and pharmacokinetic parameters were calculated by using DAS 2.0 software.RESULTS:The pharmacokinetic parameters of reference and test preparations were as follows:t1/2 were (69.77±14.61)h vs.(76.06±17.92)h;tmax(5.15±1.18)h vs.(5.05±1.36)h;cmax(13.64±3.28)μg·mL-1 vs.(13.34±4.18)μg·mL-1;AUC0～240 h(857.73±164.45)μg·h·mL-1 vs.(888.16±316) μg·h·mL-1;AUC0～∞(940.00±180.70)μg·h·mL-1 vs.(999.00±346.40)μg·h·mL-1,respectively.The relative bioavailability of test preparation was 104.2%,compared with reference preparation.CONCLUSION:2 kinds of Memantine tablets are bioequivalent.