6毫克卡巴拉汀胶囊（单剂量）在健康志愿者中的生物等效性研究。
Bioequivalence Study of Rivastigmine 6 mg Capsules (Single Dose) in Healthy Volunteers.
作者信息
Abhyankar Dhiraj, Shedage Ashish, Gole Milind, Raut Preeti
机构信息
1 Cipla Ltd, R&D Centre, Mumbai, Maharashtra, India.
出版信息
Am J Alzheimers Dis Other Demen. 2017 Sep;32(6):360-366. doi: 10.1177/1533317517712890. Epub 2017 Jul 3.
OBJECTIVE
To assess the bioequivalence of generic formulation of rivastigmine (test) and Exelon (reference).
METHODS
This randomized, open-label, 2-period, single-dose, 2-treatment, 2-sequence, crossover study was conducted in 40 healthy men under fed condition. Participants were randomized to receive a single dose of Exelon or rivastigmine capsule.
RESULTS
A total of 31 participants completed the study. Area under the concentration-time curve from time zero to time t (AUC) and area under the concentration-time curve from time zero to infinity (AUC) for Exelon (mean [standard deviation], h·ng/mL) were 126.40 (56.95) and 129.46 (59.94), respectively, while they were 122.73 (43.46) and 125.08 (45.39) for rivastigmine. Geometric mean ratios of rivastigmine/Exelon were 99.17% for AUC, 98.81% for AUC, and 105% for maximum observed plasma concentration ( C). The 90% confidence intervals (CIs) were 94.14% to 104.46%, 93.77% to 104.12%, and 93.08% to 118.44%, respectively. Both formulations were well tolerated.
CONCLUSION
The generic and reference formulations were bioequivalent, as the 90% CIs for C, AUC, and AUC were within the range of 80% to 125%.
目的
评估卡巴拉汀仿制制剂（试验品）与艾斯能（参比制剂）的生物等效性。
方法
本随机、开放标签、两周期、单剂量、双治疗、双序列交叉研究在40名处于进食状态的健康男性中进行。参与者被随机分配接受单剂量的艾斯能或卡巴拉汀胶囊。
结果
共有31名参与者完成了研究。艾斯能从零时间到t时间的浓度-时间曲线下面积（AUC）以及从零时间到无穷大的浓度-时间曲线下面积（AUC）（均值[标准差]，h·ng/mL）分别为126.40（56.95）和129.46（59.94），而卡巴拉汀的相应值为122.73（43.46）和125.08（45.39）。卡巴拉汀/艾斯能的几何平均比值对于AUC为99.17%，对于AUC为98.81%，对于最大观察血浆浓度（C）为105%。90%置信区间（CI）分别为94.14%至104.46%、93.77%至104.12%以及93.08%至118.44%。两种制剂耐受性均良好。
结论
仿制制剂与参比制剂具有生物等效性，因为C、AUC和AUC的90%CI在80%至125%范围内。
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