Bioequivalence Analysis of 2 Dapoxetine Hydrochloride Formulations in Healthy Chinese Male Volunteers Under Fed and Fasting Conditions: A Randomized, Open‐Label, 2‐Sequence, 2‐Period, 2‐Way Crossover Study

• Published in: Clinical pharmacology in drug development Vol. 10; no. 4; pp. 384 - 392
• Main Authors: Yan, Keyu, Ju, Gehang, Tan, Qiong, Zeng, Lijiao, Qiu, Wen
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.04.2021
• Subjects: Adolescent; Adult; Area Under Curve; Asians; Benzylamines - administration & dosage; Benzylamines - pharmacokinetics; Bioequivalence; Chromatography, High Pressure Liquid; Cross-Over Studies; dapoxetine hydrochloride; Fasting; food effect; Food-Drug Interactions; HPLC‐MS/MS; Humans; Male; Naphthalenes - administration & dosage; Naphthalenes - pharmacokinetics; pharmacokinetics; Serotonin Uptake Inhibitors - administration & dosage; Serotonin Uptake Inhibitors - pharmacokinetics; Tandem Mass Spectrometry; Therapeutic Equivalency; Young Adult; pharmacokinetics; dapoxetine hydrochloride; HPLC-MS/MS; food effect; bioequivalence
• ISSN: 2160-763X; 2160-7648; 2160-7648
• DOI: 10.1002/cpdd.866

This study assessed whether the reference and test formulations of dapoxetine hydrochloride were bioequivalent under fed and fasting conditions postadministration of a single dose as well as evaluated the safety profile of these 2 formulations. This study was a randomized, single‐center, 2‐period, open‐label, 2‐way crossover design study with a washout period of 7 days between each period. The study included 80 subjects, 40 under fed and 40 under fasting conditions. During each study period, the subjects were administered a single oral dose of either the reference or the test formulation, followed by collection of plasma samples 70 hours postdose. High‐performance liquid chromatography‐tandem mass spectrometry (HPLC‐MS/MS) was performed to determine the concentrations of dapoxetine in plasma samples along with the calculation of Cmax, AUC0‐t, and AUC0‐inf. In addition, adverse events were monitored to determine the safety of these formulations. The geometric mean ratio (90%CI) for the reference and test formulations was 86% to 100%, 89% to 103%, and 89% to 103% under fasting conditions and 92% to 107%, 91% to 100%, and 92% to 101% under fed conditions for Cmax, AUC0‐t, and AUC0‐inf, respectively. The 90%CIs for the test/reference ratio for AUC and Cmax were within the acceptable limits of bioequivalence, thus demonstrating bioequivalence for these 2 dapoxetine hydrochloride formulations.