Lasseter Kenneth C, Gambale Jay, Jin Bo, Bergman Art, Constanzer Marvin, Dru James, Han Tae H, Majumdar Anup, Evans Judith K, Murphy M Gail
Clinical Pharmacology Research Unit, Clinical Pharmacology of Miami, Inc, 550 West 84th Street, Hialeah, FL 33014, USA.
J Clin Pharmacol. 2007 Jul;47(7):834-40. doi: 10.1177/0091270007301800. Epub 2007 May 24.
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.
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NK1拮抗剂，用于预防化疗引起的恶心和呕吐。这项随机研究旨在评估聚山梨酯80溶媒中的福沙匹坦的耐受性以及与阿瑞匹坦的生物等效性。通过体格检查、实验室检查和不良事件评估耐受性。收集72小时的血浆样本，检测其中阿瑞匹坦和福沙匹坦的含量。将方差分析模型应用于经自然对数转换的阿瑞匹坦曲线下面积（AUC）数据。高达150mg（1mg/mL）的福沙匹坦通常耐受性良好。115mg的福沙匹坦与125mg的阿瑞匹坦AUC生物等效；115mg福沙匹坦/125mg阿瑞匹坦的阿瑞匹坦AUC几何平均比值的90%置信区间落在预先设定的0.80至1.25等效范围内。
