Efficient Loading of Rabeprazole Sodium via Porous Anion Exchange Resin for Enteric Delivery

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Conventional oral rabeprazole sodium (RAB) formulations present swallowing challenges for pediatric and dysphagic patients.
• Proton pump inhibitors (PPIs) like RAB are crucial for managing gastroesophageal reflux disease (GERD).

Purpose of the Study:

• To develop a novel, pediatric-friendly oral rabeprazole sodium formulation addressing administration difficulties.
• To enhance drug loading and create enteric-coated microcapsules for improved delivery.

Main Methods:

• Synthesized a novel anion exchange resin (AER) with favorable morphology and porosity.
• Developed RAB-loaded AER complexes (RAB@AER) via ion exchange, followed by Eudragit L100 coating for microcapsule formation (RAB@AER@L100).
• Evaluated in vitro drug release, enteric protection, and in vivo pharmacokinetics in rats.

Main Results:

• The synthesized AER demonstrated efficient RAB loading, achieving 1.63-fold higher capacity than conventional resins.
• In vitro studies confirmed enteric protection, with minimal release at pH 1.2 and sustained release at pH 6.8.
• In vivo pharmacokinetic studies in rats showed accelerated absorption (Tmax = 2h vs. 3h) and higher Cmax (3.19 vs. 2.82 μg/mL) for the suspension compared to commercial capsules.

Conclusions:

• The developed RAB@AER@L100 enteric suspension offers a promising alternative for pediatric and dysphagic patients.
• This formulation enhances swallowing safety and dosing convenience.
• The study highlights the potential of AER-based microcapsules for improved oral drug delivery.