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Clinical Trials

A001: Comparison of the Pharmacokinetics/Pharmacodynamics of a Fixed-Dose Combination of Rabeprazole/Magnesium Oxide 20/350 mg to the Enteric-Coated Rabeprazole 20 mg

Monday, September 9, 2024
5:00 PM – 7:00 PM ET

    Presenting Author(s)

  • Heejae Won, PharmD

    Ph.D. candidate
    Seoul National University College of Medicine and Hospital, Seoul-t'ukpyolsi, Republic of Korea

    • 1st/Primary Author(s)

  • Heejae Won, PharmD

    Ph.D. candidate
    Seoul National University College of Medicine and Hospital, Seoul-t'ukpyolsi, Republic of Korea

    • Co-Author(s)

  • SL

    SeungHwan Lee, MD, PhD

    Professor
    Seoul National University College of Medicine and Hospital
    Seoul, Seoul-t'ukpyolsi, Republic of Korea

Statement of Purpose, Innovation or Hypothesis: Proton pump inhibitors (PPIs), including rabeprazole is commonly used for acid-related disorders. However, the use of enteric-coated (EC) formulation of PPIs, due to their rapid degradation in acid environments, presents limitations such as delayed absorption and slow onset of action. The fixed-dose combination (FDC) of rabeprazole/magnesium oxide (MgO) 20/350 mg was newly developed to overcome these limitations. This study evaluated pharmacokinetics (PKs) and pharmacodynamics (PDs) of FDC of rabeprazole/MgO 20/350 mg in comparison to the conventional EC formulation of rabeprazole 20 mg (Pariet® 20 mg).

Description of Methods & Materials: A randomized, open-label, multiple-dose, 2-sequence, 2-period crossover study was conducted in healthy subjects. Eligible subjects randomly received either the FDC or the conventional formulation for 7 days in the first period and the alternative in the second period with a 14-day washout period. Blood samples were collected for PK analysis after the single-dose (Day 1) and multiple-dose (Day 7). Concurrently, continuous 24-hour intragastric pH monitoring was conducted for PD analysis, including baseline intragastric pH monitoring before dosing (Day -1). Geometric mean ratios (GMRs) and 90% confidence intervals (Cls) of the FDC to the conventional formulation were estimated for the PK and PD parameters.

Data & Results: Thirty-seven healthy subjects completed the study and included in PK and PD analyses. The systemic exposures of rabeprazole were similar between the treatments after the single- and multiple-dose. The GMR (90% CI) of the FDC to the conventional formulation for the area under the curve within a dosing interval (τ) at steady state (AUCτ,ss) was 0.9852 (0.8916 – 1.0887). The time to reach the maximum rabeprazole concentration of the FDC (1.5 h) was faster than the conventional formulation (3.5-4.0 h). The extents of gastric acid suppression after the single- and multiple-dose were comparable between the treatments. The GMR (90% CI) of the FDC to the conventional formulation for percent decrease from baseline in the integrated gastric acidity over a 24-hour interval was 0.9650 (0.8932 – 1.0425) at steady state. All adverse events were mild and well-tolerated in both treatments.

Interpretation, Conclusion or Significance: The FDC of rabeprazole/MgO 20/350 mg showed rapid absorption compared to the conventional formulation of rabeprazole 20 mg, without altering the overall systemic exposure and the intragastric acid suppression effect.

Disclosures: This study was sponsored by DaehanNupharm Co., Ltd, Republic of Korea. Authors do not have any conflicts of interest for this study.

Citations/References:

Additional Information/Authors: N/A