Frohna Paul, Lu Jianfeng, Eppler Steve, Hamilton Marta, Wolf Julie, Rakhit Ashok, Ling Jie, Kenkare-Mitra Saraswati R, Lum Bert L
CV Therapeutics, Inc, Palo Alto, California, USA.
J Clin Pharmacol. 2006 Mar;46(3):282-90. doi: 10.1177/0091270005284193.
A randomized, open-label, 2-period crossover study was conducted to evaluate the bioequivalence of 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg (arm A, n = 42) and the oral bioavailability of the 150-mg tablet versus a 25-mg intravenous infusion (arm B, n = 20) in healthy subjects. The washout period was 2 weeks between treatments. Plasma concentrations of erlotinib and its active metabolite, OSI-420, were measured after each dose. The ratios of geometric means for AUC(0-infinity) and Cmax of erlotinib following 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg were (1 and 0.95) within the predefined bioequivalence range of 0.80 to 1.25. The mean absolute oral bioavailability, using compartmental analysis, was estimated as 59% (95% confidence interval, 55%-63%). Overall, 6 tablets of erlotinib 25 mg are bioequivalent to a single 150-mg tablet. Both intravenous and oral erlotinib were generally well tolerated with an estimated bioavailability of 59% following oral administration.
开展了一项随机、开放标签、两期交叉研究，以评估6片25毫克厄洛替尼与1片150毫克厄洛替尼（A组，n = 42）的生物等效性，以及在健康受试者中150毫克片剂相对于25毫克静脉输注（B组，n = 20）的口服生物利用度。治疗之间的洗脱期为2周。每次给药后测量厄洛替尼及其活性代谢物OSI-420的血浆浓度。6片25毫克厄洛替尼和1片150毫克厄洛替尼后厄洛替尼的AUC(0-无穷大)和Cmax的几何均值比在预先定义的0.80至1.25生物等效性范围内（分别为1和0.95）。使用房室分析估计的平均绝对口服生物利用度为59%（95%置信区间，55%-63%）。总体而言，6片25毫克厄洛替尼与1片150毫克片剂生物等效。静脉注射和口服厄洛替尼一般耐受性良好，口服给药后的估计生物利用度为59%。
