AUTHOR=Ding Ying , Chu Nannan , Que Linling , Huang Kai , Chen Yuanxing , Qin Wei , Qian Zhenzhong , Shi Yunfei , Xu Zhen , He Qing 

TITLE=Pharmacokinetics and bioequivalence study of esomeprazole magnesium enteric-coated tablets 20 mg in healthy Chinese subjects under fasting and fed conditions

JOURNAL=Frontiers in Pharmacology

VOLUME=Volume 14 - 2023

YEAR=2023

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2023.1169103

DOI=10.3389/fphar.2023.1169103

ISSN=1663-9812

ABSTRACT=Objective: The main purpose of this study was to evaluate the pharmacokinetics, bioequivalence and safety properties between a new generic and a branded reference formulation of esomeprazole enteric-coated tablets 20 mg in healthy Chinese subjects under fasting and fed conditions. 
Methods: The fasting study was an open-label, randomized, two-period crossover study conducted in 32 healthy Chinese volunteers; another fed study was a four-period crossover study conducted in 40 healthy Chinese volunteers. Blood samples were collected at the specified time points and determined to obtain the plasma concentrations of esomeprazole. The main pharmacokinetic parameters were calculated by non-compartment method. Bioequivalence was analyzed by the geometric mean ratios (GMR) of the two formulations and the corresponding 90% confidence intervals (CIs). The safety of the two formulation s were assessed.
Results: The fasting and fed study showed that the pharmacokinetics of the two formulations were similar. Under the fasting condition, the 90% CIs of GMRs of the test to reference formulation were 87.92%-104.36% for Cmax, 87.82%-101.45% for AUC0-t, and 87.99%-101.54% for AUC0-∞, respectively; under the fed condition, the 90% CIs of GMRs of the test to reference formulation were 80.53%-94.95% for Cmax, 87.46%-97.26% for AUC0-t, and 87.46%-97.16% for AUC0-∞, respectively. The 90% CIs of GMRs all fall within the bioequivalence range of 80.00% to 125.00%. The two formulations had good safety and well tolerance, and no serious adverse events occurred.
Conclusion: According to relevant regulatory standards, esomeprazole enteric-coated generic and the reference products had bioequivalence and good safety in healthy Chinese subjects.
Key words: esomeprazole magnesium enteric-coated tablet, bioequivalence, pharmacokinetics, safety, Chinese healthy subjects
Clinical trials registration number: http://www.chinadrugtrials.org.cn/index.html
# CTR20171347 and CTR20171484