Pharmacokinetics, Bioequivalence, and Safety of 2 Formulations of Hydroxychloroquine Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions

• Published in: Clinical pharmacology in drug development 2023-03, Vol.12 (3), p.273-278
• Main Authors: Luo, Hong‐Yu, Long, Hui‐Zhi, Zhou, Zi‐Wei, Xu, Shuo‐Guo, Li, Feng‐Jiao, Cheng, Yan, Wen, Dan‐Dan, Deng, Ping, Gao, Li‐Chen
• Format: Article
• Language: English
• Subjects: Area Under Curve; Bioequivalence; East Asian People; Fasting; fed; Healthy Volunteers; Humans; hydroxychloroquine; Hydroxychloroquine - pharmacokinetics; pharmacokinetic; Pharmacokinetics; safety; Tablets; Therapeutic Equivalency
• ISSN: 2160-763X; 2160-7648
• DOI: 10.1002/cpdd.1166

The purpose of this trial was to evaluate the pharmacokinetics (PK), bioequivalence (BE), and safety of 2 preparations of hydroxychloroquine (200‐mg tablet) under fasting and fed conditions. A total of 180 subjects (fasting condition: n = 80; fed condition: n = 100) were randomly enrolled in this randomized, open, single‐dose, single‐cycle parallel phase Ⅰ clinical study. Under the 2 conditions, the subjects were randomly administered the test (T) or reference (R) tablet, both at a dose of 200 mg (1 tablet). Liquid chromatography–tandem mass spectrometry was used to determine the concentration of hydroxychloroquine in healthy subjects after oral administration of the T or R preparation to evaluate the PK characteristics. In this trial, the T and R preparations of hydroxychloroquine were bioequivalent under both conditions within the range of 80%–125%. No serious adverse events (SAEs) were found in the safety assessments for either condition, and all adverse events (AEs) were mild, except for 2 moderate AEs in the fed condition, indicating good safety.