Formulation and Characterization of Multiparticulate System for Proton Pump Inhibitor using Combination Therapy for...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Gastroenterology

Background:

• Peptic ulcer disease necessitates effective therapeutic strategies.
• Amla extract, rich in gallic acid, exhibits anti-ulcer properties by inhibiting gastric H+/K+ ATPase.
• Esomeprazole Magnesium is a proton pump inhibitor commonly used for acid-related disorders.

Purpose of the Study:

• To develop sustained-release enteric-coated granules of Amla extract and Esomeprazole Magnesium.
• To enhance synergistic anti-ulcer effects and mitigate potential side effects.
• To achieve prolonged drug release and improved therapeutic outcomes for peptic ulcer treatment.

Main Methods:

• Amla phenolic extract was prepared using Soxhlet extraction (ethanol:water, 7:3).
• Granules were formulated using wet granulation and enteric-coated with hydroxypropyl methylcellulose phthalate.
• In vitro drug release and entrapment efficiency were optimized; in vivo anti-ulcer activity was assessed in aspirin-induced Wistar albino rats.

Main Results:

• Enteric coating ensured negligible drug release at pH 1.2 (simulated gastric fluid) and efficient release at pH 6.8 (simulated intestinal fluid).
• The combination therapy exhibited significant therapeutic efficacy in the in vivo rat ulcer model.
• Optimized granules demonstrated sustained release characteristics and effective drug entrapment.

Conclusions:

• Sustained-release enteric-coated granules of Amla extract and Esomeprazole Magnesium were successfully developed.
• The combination therapy showed significant positive effects in treating peptic ulcers, supported by various efficacy parameters.
• The formulation offers a promising approach for enhanced peptic ulcer management through synergistic action and controlled drug delivery.