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Pharmacokinetics and Bioequivalence Evaluation of Erlotinib Hydrochloride Tablets: Randomized, Open‐Label, 2‐Period Crossover Study in Healthy Chinese Subjects
Author(s) -
Wang Lu,
Ruan Zourong,
Yang Dandan,
Hu Yin,
Liang Jian,
Chen Jinliang,
Shao Rong,
Xu Yichao,
Guan Yanlu,
Jiang Bo
Publication year - 2021
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.811
Subject(s) - bioequivalence , pharmacokinetics , medicine , crossover study , confidence interval , pharmacology , area under the curve , geometric mean , mathematics , statistics , alternative medicine , pathology , placebo
A randomized, open‐label, 2‐period crossover study was performed to evaluate the pharmacokinetic properties and bioequivalence of 2 erlotinib hydrochloride tablets (a test formulation and a reference formulation) in healthy Chinese subjects. Subjects were randomized to receive a single oral dose of the erlotinib hydrochloride test or reference formulation (150 mg) under fasting conditions. The washout period was 12 days. Blood samples were collected at scheduled time points, and plasma concentrations were determined using a high‐performance liquid chromatography–tandem mass spectrometry method. A noncompartmental method was used to calculate pharmacokinetic parameters and to evaluate the bioequivalence of the 2 formulations. Safety assessments were performed during the whole study period. The results suggest that the pharmacokinetic parameter values of the test formulation were similar to those of the reference formulation. The 90% confidence intervals of the geometric least‐squares mean ratios of the test to reference formulation were 94.06% to 105.43% for maximum concentration, 88.21% to 97.57% for area under the concentration‐time curve to last measurement, and 87.37% to 97.14% for area under the curve extrapolated to infinity, which are all within the accepted bioequivalence range of 80% to 125%. No serious adverse events occurred during the study. These findings suggest that the 2 erlotinib hydrochloride tablets were bioequivalent in accordance with predetermined regulatory criteria.