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薬理と治療
Abstract
Objectives To determine the bioequivalence between the tablet and dry syrup of lacosamide (LCM), an open-label, randomized, single-oral dose, 2-way cross-over clinical trial (EP0059;ClinicalTrials. gov identifier: NCT02972125, EudraCT Number: 2016-002462-31)was conducted. Methods Healthy male Japanese volunteers aged from 20 to 55 years were eligible for the study. Participants were randomly assigned in a 1:1 ratio to the tablet-dry syrup or dry syrup-tablet treatment sequence. Each participant received the tablet and dry syrup of LCM 100 mg. The co-primary pharmacokinetic(PK)parameters were the maximum observed plasma concentration(Cmax)and the area under the concentration-time curve until the time of last quantifiable concentration(AUC(0-t)). Results Between October 2016 and March 2017, 24 participants(12 in each treatment sequence)received the study drugs and completed the study. All participants were included in the analysis. The geometric means of Cmax and AUC(0-t) were similar between the tablet and dry syrup(Cmax, 4.242 and 4.456μg╱mL; and AUC(0-t), 55.96 and 56.20 μg・h╱mL, respectively). Analysis of the primary PK parameters demonstrated bioequivalence between 2 formulations with the 90% confidence intervals for the dry syrup╱tablet ratio of Cmax(0.9294 to 1.1871)and AUC(0-t)(0.9869 to 1.0217)being within the accepted bioequivalence range(0.80 to 1.25). Eight participants(33.3%)experienced at least one treatment-emergent adverse event(TEAE) during the study. The common TEAEs were bradycardia (12.5%)and rhinorrhea(8.3%). All TEAEs were mild in intensity. Conclusions The tablet and dry syrup of LCM 100 mg were bioequivalent in healthy male Japanese volunteers. Both formulations were well tolerated.
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