美金刚胶囊剂与片剂的人体生物等效性

目的评价美金刚胶囊剂与片剂的人体生物等效性。方法20名健康男性受试者采用随机交叉实验设计,用高效液相色谱-质谱联用法,测定单剂量口服美金刚胶囊剂与片剂各10 mg后美金刚的血浆浓度,所得数据经DAS 2.0软件处理获得各自的药动学参数。结果美金刚胶囊和片剂的主要药动学参数:t_(max)分别为(6.1±s 2.4)和(6.6±2.6)h,c_(max)分别为(13±3)和(12±4)μg·L~(-1),t_(1/2)分别为(63±14)和(64±12)h;用梯形法计算,AUC_(0～1)分别为(902±292)和(845±256)μg·h·L~(-1);以AUC_(0～1)计算,美金刚胶囊剂的平均相对生物利用度为(110±28)%。统计学分析结果表明胶囊剂与片剂的主要药动学参数c_(max)、AUC_(0～1)和t_(max)均无显著差异。结论2种制剂在人体内具有生物等效性。

Bioequivalence of memantine capsules and tablets in human volunteers

AIM To evaluate the bioequivalenee of memantine tablets and capsules.METHODS A randomized,cross over designed trial was conducted in 20 healthy volunteers.The plasma concentrations of memantine were determined by HPLC-MS after a single oral dose of 10 mg tablets of the test and reference preparation,and the pharmacokinetics parameters of memantine were obtained using DAS 2.0 software. RESULTS The pharmacokinetic parameters of the capsule vs tablet drug were as follows:t_(max)(6.1±s 2.4)h and(6.6±2.6)h,c_(max)(13±3)μg·L~(-1)and(12±4)μg·L~(-1),t_(1/2)(63±14)h and(64±12)h,AUC_(0-1) (902±292)μg·h·L~(-1) and (845±256)μg·h·L~(-1).The relative bioavailability of memantine capsules was(110±28)%.The result of statistical analysis showed that there was no significant difference between c_(max),AUC_(0-1) and t_(max) of the two preparations.CONCLUSION The memantine capsules and tablets were bioequivalent.