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Updated: Jun 24, 2026
07:32
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Agglomerates containing pantoprazole microparticles: modulating the drug release
Renata P Raffin1, Paolo Colombo, Fabio Sonvico
1Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752/405, 90610-000, Porto Alegre, Brazil. renata.raffin@ufrgs.br
AAPS Pharmscitech
|March 26, 2009
Summary
Pantoprazole microparticles were stabilized for six months. Agglomeration improved their properties for delayed-release and gastro-resistant dosage forms, with optimal results using a specific mannitol/lecithin ratio.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Pantoprazole is a proton pump inhibitor used to treat acid-related disorders.
- Developing stable, delayed-release, and gastro-resistant formulations is crucial for effective pantoprazole delivery.
- Microparticle technology offers potential for controlled drug release, but optimizing technological characteristics is essential.
Purpose of the Study:
- To prepare and characterize pantoprazole-loaded microparticles.
- To improve the technological and biopharmaceutical properties of pantoprazole microparticles through agglomeration for oral delayed release and gastro-resistance.
- To evaluate the impact of lecithin content and microparticle ratios on agglomerate formation and properties.
Main Methods:
- Pantoprazole microparticles were prepared using Eudragit S100 and Methocel F4M.
- Accelerated stability studies were conducted at 40°C and 75% RH for 6 months.
- Agglomeration was performed by mixing microparticles with spray-dried mannitol/lecithin powders, varying lecithin content and powder ratios.
Main Results:
- Pantoprazole microparticles showed no significant degradation over 6 months.
- Agglomerates exhibited spherical shapes, smooth surfaces, and high yields.
- Optimized agglomerates (1:2 ratio of microparticles to mannitol/lecithin (80:20)) demonstrated favorable mechanical and biopharmaceutical properties, including delayed release and gastro-resistance.
Conclusions:
- The agglomeration process effectively enhanced the technological characteristics of pantoprazole microparticles.
- Lecithin ratio in mannitol/lecithin powder is critical for agglomerate formation and drug release.
- The optimized formulation provides a promising gastro-resistant, delayed-release solid dosage form for pantoprazole.
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