• Editors
  • Scope
  • Current Issue
  • Archive
  • Artical Processing Charge
  • Instruction for Author
  • Principles and Policies of transparency
  • Policies of corrections and retractions
  • EndNote style


2018 (v.26 no.1)

Translational and Clinical Pharmacology

Korean Society for Clinical Pharmacology and Therapeutics
Quarter
ISSN: 2289-0882

  • Pharmacokinetics of fixed-dose combination of rosuvastatin 20 mg and ezetimibe 10 mg compared to concurrent administration of individual tablets in healthy Korean subjects

    Inyoung Hwang, Sang-In Park, SeungHwan Lee, BackHwan Lee, Kyung-Sang Yu, Ji-Young Jeon, Min-Gul Kim

    TCP | v.26, no.1, pp.16-24, Mar, 2018

    Abstract

    This study aimed to compare the pharmacokinetics of fixed-dose combination (FDC) tablet of rosuvastatin 20 mg/ezetimibe 10 mg with that of concurrent administration of individual rosuvastatin 20 mg tablet and ezetimibe 10 mg tablet in healthy subjects. A randomized, open label, single-dose, two-way crossover study was conducted. Subjects randomly received test formulation (FDC tablet of rosuvastatin 20 mg/ezetimibe 10 mg) or reference formulation (co-administration of rosuvastatin 20 mg tablet and ezetimibe 10 mg tablet). After 2 weeks of washout, subjects received the other treatment. Blood samples were collected up to 72 hours post-dose in each period. Plasma concentrations of rosuvastatin, ezetimibe and total ezetimibe (ezetimibe + ezetimibe glucuronide) were analyzed by liquid chromatography-tandem mass spectrometry (LC/MS/MS). The geometric mean ratio (GMR) of Cmax and AUClast (90% confidence interval, CI) for rosuvastatin was 1.036 (0.979-1.096) and 1.024 (0.981-1.070), respectively. The corresponding values for ezetimibe were 0.963 (0.888-1.043) and 1.021 (0.969-1.074), respectively. The corresponding values for total ezetimibe were 0.886 (0.835-0.940) and 0.983 (0.946-1.022), respectively. FDC tablet containing rosuvastatin 20 mg and ezetimibe 10 mg is bioequivalent to the co-administration of commercially available individual tablets of rosuvastatin and ezetimibe as GMR with 90% CI of Cmax and AUClast of rosuvastatin, ezetimibe and total ezetimibe were contained within conventionally accepted bioequivalence criteria.

    Keyword

    Rosuvastatin, Ezetimibe, Fixed-dose combination, Pharmacokinetics, Bioequivalence