Purpose <p>This study aimed to develop and evaluate a gastroretentive floating esomeprazole magnesium in situ gel to prolong gastric residence time and provide sustained drug release for improved management of GERD-associated erosive esophagitis. The research question was whether a sodium alginate–HPMC–based in situ gel could achieve rapid gelation, prolonged buoyancy, controlled release up to 12&#xa0;h, and acceptable stability.</p> Methods <p>Floating in situ gels (F1–F9) were prepared using sodium alginate (gelling polymer), HPMC K100M (viscosity enhancer/release retardant), calcium carbonate (gas-forming agent), and trisodium citrate. Formulations were evaluated for appearance, pH, drug content, viscosity, gelling capacity, floating lag time, floating duration, gel density, water uptake, in vitro drug release (USP II, 0.1&#xa0;N HCl, 37 ± 0.5&#xa0;°C), and 90-day stability.</p> Results <p>All formulations showed acceptable pH (7.65–7.90), drug content (89.40–97.20%), gel density &lt; 1&#xa0;g/cm³, and floating duration &gt; 12&#xa0;h. F5 was optimized, showing rapid gelation, short floating lag time, and sustained release with ~ 96.8% drug release over 12&#xa0;h, and remained stable for 90 days.</p> Conclusion <p>The developed floating in situ gel, particularly optimized formulation F5, demonstrated prolonged gastric retention with controlled esomeprazole release up to 12&#xa0;h and good stability, indicating its potential as a once-daily gastroretentive delivery system.</p>

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Esogel Embrace: Unveiling the Potential of Esomeprazole in Situ Gel for Gastric Retention

  • Raghwendra R. Waghmode,
  • Sandeep P. Barde,
  • Dipak P. Mali

摘要

Purpose

This study aimed to develop and evaluate a gastroretentive floating esomeprazole magnesium in situ gel to prolong gastric residence time and provide sustained drug release for improved management of GERD-associated erosive esophagitis. The research question was whether a sodium alginate–HPMC–based in situ gel could achieve rapid gelation, prolonged buoyancy, controlled release up to 12 h, and acceptable stability.

Methods

Floating in situ gels (F1–F9) were prepared using sodium alginate (gelling polymer), HPMC K100M (viscosity enhancer/release retardant), calcium carbonate (gas-forming agent), and trisodium citrate. Formulations were evaluated for appearance, pH, drug content, viscosity, gelling capacity, floating lag time, floating duration, gel density, water uptake, in vitro drug release (USP II, 0.1 N HCl, 37 ± 0.5 °C), and 90-day stability.

Results

All formulations showed acceptable pH (7.65–7.90), drug content (89.40–97.20%), gel density < 1 g/cm³, and floating duration > 12 h. F5 was optimized, showing rapid gelation, short floating lag time, and sustained release with ~ 96.8% drug release over 12 h, and remained stable for 90 days.

Conclusion

The developed floating in situ gel, particularly optimized formulation F5, demonstrated prolonged gastric retention with controlled esomeprazole release up to 12 h and good stability, indicating its potential as a once-daily gastroretentive delivery system.