AAPS PharmSciTech

, Volume 10, Issue 2, pp 335–345 | Cite as

Agglomerates Containing Pantoprazole Microparticles: Modulating the Drug Release

  • Renata P. Raffin
  • Paolo Colombo
  • Fabio Sonvico
  • Alessandra Rossi
  • Denise S. Jornada
  • Adriana R. Pohlmann
  • Silvia S. Guterres
Research Article


Pantoprazole-loaded microparticles were prepared using a blend of Eudragit® S100 and Methocel® F4M. The accelerated stability was carried out during 6 months at 40°C and 75% relative humidity. In order to improve technological characteristics of the pantoprazole-loaded microparticles, soft agglomerates were prepared viewing an oral delayed release and gastro-resistant solid dosage form. The agglomeration was performed by mixing the pantoprazole microparticles with spray-dried mannitol/lecithin powders. The effects of factors such as the amount of lecithin in the spray-dried mannitol/lecithin powders and the ratio between pantoprazole microparticles and spray-dried mannitol/lecithin powders were evaluated. The pantoprazole-loaded microparticles present no significant degradation in 6 months. The agglomerates presented spherical shape, with smooth surface and very small quantity of non-agglomerated particles. The agglomerates presented different yields (35.5–79.0%), drug loading (58–101%), and mechanical properties (tensile strength varied from 44 to 69 mN mm−2), when the spray-dried mannitol/lecithin powders with different lecithin amounts were used. The biopharmaceutical characteristics of pantoprazole microparticles, i.e., their delayed-release properties, were not affected by the agglomeration process. The gastro-resistance of the agglomerates was affected by the amount of spray-dried mannitol/lecithin powders. The ratio of lecithin in the spray-dried mannitol/lecithin powders was the key factor in the agglomerate formation and in the drug release profiles. The agglomerates presenting better mechanical and biopharmaceutical characteristics were prepared with 1:2 (w/w) ratio of pantoprazole-loaded microparticles and mannitol/lecithin (80:20) powder.

Key words

agglomerates delayed release gastro-resistance microparticles 



The authors are grateful for the financial support of CNPq/MCT, Universal 2007 CNPq and for the CAPES fellowship. The financial support of the Italian Ministry for University and Research is also gratefully acknowledged. We thank Prof. Edilson Benvenutti for the BET analysis.


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Copyright information

© American Association of Pharmaceutical Scientists 2009

Authors and Affiliations

  • Renata P. Raffin
    • 1
  • Paolo Colombo
    • 2
  • Fabio Sonvico
    • 2
  • Alessandra Rossi
    • 2
  • Denise S. Jornada
    • 1
  • Adriana R. Pohlmann
    • 1
    • 3
  • Silvia S. Guterres
    • 1
  1. 1.Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de FarmáciaUniversidade Federal do Rio Grande do SulPorto AlegreBrazil
  2. 2.Dipartimento FarmaceuticoUniversità degli Studi di ParmaParmaItaly
  3. 3.Departamento de Química Orgânica, Instituto de QuímicaUniversidade Federal do Rio Grande do SulPorto AlegreBrazil

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