Formulation Development and Optimization of Taste-Masked Azithromycin Oral Suspension with Ion Exchange Resins, Including Bioanalytical Method Development and Validation, In Vivo Bioequivalence Study, and In-Silico PBPK Modeling for the Pediatric Population
DOI:
https://doi.org/10.64149/J.Carcinog.24.7s.700-708Keywords:
Azithromycin, taste masking, ion exchange resins, bioequivalence, PBPK modeling, pediatric formulationAbstract
Background: Azithromycin, a macrolide antibiotic, exhibits significant bitter taste that limits pediatric compliance. This study aimed to develop a taste-masked azithromycin oral suspension using ion exchange resins and evaluate its bioequivalence with reference formulation.
Methods: Ion exchange resins (Amberlite IRP64 and Kyron T-114) were employed for taste masking. Formulation optimization was conducted using Design of Expert software. A validated HPLC method was developed for bioanalysis. Bioequivalence studies were performed in healthy volunteers, and PBPK modeling predicted pediatric pharmacokinetics.
Results: Optimized formulation containing 15% w/w Amberlite IRP64 demonstrated effective taste masking with 92.3% drug loading efficiency. The bioanalytical method showed linearity (R² = 0.999) over 50-5000 ng/mL range. Bioequivalence study confirmed 90% confidence intervals within 80-125% acceptance criteria. PBPK modeling predicted appropriate dosing for pediatric patients aged 6 months to 12 years.
Conclusion: Successfully developed taste-masked azithromycin suspension demonstrated bioequivalence with improved palatability for pediatric use
