Tolerability of fosaprepitant and bioequivalency to aprepitant in healthy subjects
Tolerability of fosaprepitant and bioequivalency to aprepitant in healthy subjects
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DOI：
10.1177/0091270007301800
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发表时间：
2007-07-01
影响因子：
2.9
通讯作者：
Murphy, M. Gail
中科院分区：
文献类型：
--
作者：
Lasseter, Kenneth C.;Gambale, Jay;Murphy, M. Gail
福沙匹坦是阿瑞匹坦的静脉注射制剂，阿瑞匹坦是一种口服NK 1拮抗剂，用于预防化疗引起的恶心和呕吐。本随机化研究旨在评价聚山梨酯80溶剂中福沙匹坦与阿瑞匹坦的耐受性和生物等效性。通过体格检查、实验室检查和不良事件评估耐受性。分析72小时收集的血浆中的阿瑞匹坦和福沙匹坦。将方差分析模型应用于自然对数转换的阿瑞吡坦曲线下面积（AUC）数据。高达150 mg（1 mg/mL）的福沙匹坦通常耐受良好。福沙匹坦115 mg与阿瑞匹坦125 mg的AUC具有生物等效性;福沙匹坦115 mg/阿瑞匹坦125 mg的阿瑞匹坦AUC几何均值比的90%置信区间在预先规定的等效性界限0.80 - 1.25内。
Fosaprepitant is an intravenous formulation of aprepitant, an oral NK1 antagonist used to prevent chemotherapy-induced nausea and vomiting. This randomized study was designed to evaluate fosaprepitant in polysorbate 80 vehicle for tolerability and bioequivalency to aprepitant. Tolerability was assessed by physical and laboratory examinations and adverse events. Plasma collected for 72 hours was assayed for aprepitant and fosaprepitant. Analysis of variance models were applied to natural log-transformed aprepitant area under the curve (AUC) data. Fosaprepitant up to 150 mg (1 mg/mL) was generally well tolerated. Fosaprepitant 115 mg was AUC bioequivalent to aprepitant 125 mg; the 90% confidence interval for the geometric mean ratio of aprepitant AUC for fosaprepitant 115 mg/aprepitant 125 mg fell within prespecified equivalence bounds of 0.80 to 1.25.