拉科萨米德延长释放囊与拉科萨米德即时释放片具有生物等价性:药理学观察和模拟
James Wheless1, Barry Gidal2, Lixin Gong3
1Department of Pediatrics, Division of Pediatric Neurology, University of Tennessee Health Science Center, 49 N Dunlap Ave., 3rd Floor FOB, Memphis, TN 38105, United States; Neuroscience Institute and Le Bonheur Comprehensive Epilepsy Program, Le Bonheur Children's Hospital, 49 N Dunlap Ave, 3rd Floor FOB, Memphis, TN 38105, United States.
每天一次的拉科萨米德延长释放 (XR) 囊与每天两次的即时释放 (IR) 片具有生物等价性. 药物动力学模拟显示了部分粘附的类似效应,支持XR作为一种方便的替代方案.
科学领域:
- 药理动力学和药物开发
- 临床药理学 临床药理学
- 生物等价性研究 生物等价性研究
背景情况:
- 拉科萨米德是一种抗药物,可提供即释放 (IR) 和延长释放 (XR) 配方.
- 了解不同类型的lacosamide配方的生物等价性和临床效用对于优化患者治疗至关重要.
研究的目的:
- 评估每天服用一次的lacosamide XR囊和每天服用两次的lacosamide IR片之间的生物等价性.
- 通过药理动力学模拟来解决关于lacosamide XR在现实世界中使用的临床问题.
主要方法:
- 一项随机的,开放的,比较的生物利用性研究,涉及35名健康男性.
- 参与者接受了拉科萨米德XR (400毫克每天一次) 或IR (200毫克每天两次) 治疗7天.
- 主要终点包括度-时间曲线下的面积 (AUC0-τ,ss) 和稳定状态的最大度 (Cmax,ss);生物等价性由几何最小方位平均比率 (GLSMs) 的90%置信区间 (CI) 确定,在80%至125%之间.
主要成果:
- 拉科萨米德XR囊和IR片证明了生物等价性,GLSMs的所有90%CI都处于80%-125%的范围内.
- 副作用是轻微的,没有发现严重的安全问题.
- 药物动力学模拟表明,在两种配方中,部分粘附的影响相似,推的切换策略包括早上IR和晚上XR剂量以达到一致的度.
结论:
- 每天服用一次的lacosamide XR囊与每天服用两次的lacosamide IR片剂具有生物等价性.
- 由于每天服用一次和易于切换配方,Lacosamide XR提供了潜在的临床优势.
- 这些发现支持lacosamide XR作为可行的每日一次替代lacosamide IR治疗的可行替代品.
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