Liu Lihua, Li Xin, Liu Yujie, Li Yuan, Deng Yang, Zhang Ping, Tu Shengqing, Wang Keli, Xu Bing
Department of Pharmacy, The Third Hospital of Changsha, Changsha, Hunan, China.
Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd, Jiangsu, China.
Clin Pharmacol Drug Dev. 2022 Sep;11(9):1110-1115. doi: 10.1002/cpdd.1096. Epub 2022 Apr 5.
This study aimed to evaluate the bioequivalence of two pazopanib tablet formulations in healthy Chinese subjects. A randomized, open-label, single-dose, two-period, two-sequence, crossover study was conducted under fasting conditions. A total of 32 eligible subjects were randomly administered a single dose of a 200-mg generic or branded pazopanib tablet with a 16-day washout period. Blood samples were collected before and up to 72 hours after dosing. Pharmacokinetic parameters were analyzed with noncompartmental analysis. Safety assessments included physical examinations, laboratory tests, and adverse events reporting. Maximum plasma concentration (C ), area under the plasma concentration-time curve (AUC) from zero to the last quantifiable concentration (AUC ), and AUC from zero to infinity (AUC ) were similar between the generic and branded products (all P > .05). The 90% confidence intervals of the geometric mean ratio of the test/reference products for C , AUC , and AUC were 89.1%-117.1%, 81.9%-108.5%, and 82.4%-109.6%, respectively. There were no serious adverse events during the study. The newly developed generic pazopanib tablet was bioequivalent to the reference product under fasting conditions. Both formulations were well tolerated in healthy Chinese volunteers.
本研究旨在评估两种帕唑帕尼片剂在中国健康受试者中的生物等效性。在禁食条件下进行了一项随机、开放标签、单剂量、两周期、两序列的交叉研究。共有32名符合条件的受试者随机接受单剂量200毫克的仿制或原研帕唑帕尼片剂，洗脱期为16天。在给药前及给药后长达72小时采集血样。采用非房室分析法分析药代动力学参数。安全性评估包括体格检查、实验室检查和不良事件报告。仿制产品和原研产品之间的最大血浆浓度（Cmax）、从零至最后可定量浓度的血浆浓度-时间曲线下面积（AUC0-t）以及从零至无穷大的血浆浓度-时间曲线下面积（AUC0-∞）相似（所有P>0.05）。试验/参比产品Cmax、AUC0-t和AUC0-∞几何平均比值的90%置信区间分别为89.1%-117.1%、81.9%-108.5%和82.4%-109.6%。研究期间无严重不良事件发生。新研发的仿制帕唑帕尼片剂在禁食条件下与参比产品生物等效。两种制剂在中国健康志愿者中耐受性良好。
