Pharmacokinetics and Bioequivalence Evaluation of Erlotinib Hydrochloride Tablets: Randomized, Open‐Label, 2‐Period Crossover Study in Healthy Chinese Subjects

Abstract

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.

Analytical Method Validation and Bioequivalence Study of Erlotinib 150 Mg Tablets in Iranian Healthy Volunteers Under Fasting Condition

“…Further, the mean Tmax values were 2.1±0.4 h and 2.1±0.5 h in reference and test formulations, respectively (table 5). The reported values of Cmax and AUC varied greatly between investigations due to the substantial intra-subject variability [9,[18][19][20][21][22].…”

Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

“…In vivo bioequivalence (BE) studies are pivotal to show similarity between a generic product and reference product, and are routinely applied during the development of various generic products 9–11 . However, these studies often require costly clinical investigations.…”

“…8 In vivo bioequivalence (BE) studies are pivotal to show similarity between a generic product and reference product, and are routinely applied during the development of various generic products. [9][10][11] However, these studies often require costly clinical investigations. Early assessment of potential BE risk is critical for an effective and streamlined clinical pharmacology strategy.…”