Preparation, characterization, and in vivo anti-ulcer evaluation of pantoprazole-loaded microparticles

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Renata P RaffinSílvia S Guterres

Abstract

Pantoprazole is an important drug in the treatment of acid-related disorders. This work concerns the preparation and characterization of gastro-resistant pantoprazole-loaded microparticles prepared using an O/O emulsification/solvent evaporation technique. The in vivo activity of the pantoprazole-loaded Eudragit S100 microparticles was carried out in rats. Furthermore, tablets containing the microparticles were also investigated. Microparticles presented spherical and smooth morphologies (SEM) and they remained intact in the inner surface of tablets. DSC and IR analyses showed that pantoprazole was physically and molecularly dispersed in the polymer. In vivo anti-ulcer evaluation showed that the microparticles were able to protect rat stomachs against ulcer formation, while the drug aqueous solution did not present activity. Drug dissolution profiles from tablets demonstrated slower release than untabletted microparticles. Weibull equation was the best model for describing the drug release profiles from microparticles and tablets. As regards the acid protection, tablets showed a satisfactory drug protection in acid medium (61.05 +/- 8.09% after 30 min).

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Citations

Mar 26, 2009·AAPS PharmSciTech·Renata P RaffinSilvia S Guterres
Mar 25, 2014·Materials Science & Engineering. C, Materials for Biological Applications·Aline de Arce VelasquezLetícia Cruz
May 2, 2013·Journal of Microencapsulation·Acarilia Eduardo SilvaEryvaldo Sócrates Tabosa do Egito
Oct 27, 2007·Pharmaceutical Development and Technology·Renata Platcheck RaffinAdriana Raffin Pohlmann
Mar 4, 2010·Drug Delivery·Letícia CruzAdriana Raffin Pohlmann
Apr 20, 2012·Drug Development and Industrial Pharmacy·Suryakanta SwainM E B Rao
May 18, 2010·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Letícia CruzAdriana R Pohlmann
Apr 1, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·R P RaffinS S Guterres
Sep 1, 2020·International Journal of Pharmaceutics·Helissara Silveira DiefenthaelerIrene Clemes Külkamp-Guerreiro
Mar 18, 2021·Journal of Drug Targeting·Larissa SpósitoMarlus Chorilli

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