Could the Change of Excipient Content Improve the Stability of Gastroresistant Omeprazole Pellets?

Abstract

Omeprazole (OM), a temperature, pH, and moisture-sensitive drug, poses formulation challenges. This study delves into the complex development of OM pellets, focusing on the impact of buffering excipients on stability and release. Addressing the challenges of OM pellet stability requires a comprehensive compatibility and stress study involving key excipients. Binary mixtures of OM with dibasic sodium phosphate dihydrate (DSPD), mannitol, hypromellose (Hyp), and polysorbate underwent scrutiny for possible incompatibilities, subjected to 40°C stress and 75% relative humidity. DSC, TGA, and ATR-FTIR analyses were conducted, with quantitative monitoring of OM by HPLC. Formulations with varied proportions of DSPD and Hyp were also stress-tested. While all excipients exhibited compatibility with OM, thermal analysis suggested a potential incompatibility between OM and mannitol, disproven by HPLC. Stress tests on diverse formulations confirmed their adequacy, maintaining OM content and impurities within acceptable limits. Increased Hyp reduced impurities, and its combination with DSPD further enhanced stability. The study concludes that augmenting DSPD with Hyp offers effective protection for OM pellets, ensuring their stability.

Keywords:
Compatibility and stress study; Dihydrate dibasic sodium phosphate; Hypromellose

HIGHLIGHTS

Development of stable omeprazole pellets (OMP).

Dibasic sodium phosphate dihydrate and hypromellose to protect OMP from degradation.

Analytical techniques for testing the compatibility and stability of unstable drugs.