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

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-lo...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2006-06, Vol.63 (2), p.198-204
Main Authors: Raffin, R.P., Colomé, L.M., Pohlmann, A.R., Guterres, S.S.
Format: Article
Language:English
Subjects:
2-Pyridinylmethylsulfinylbenzimidazoles
Animals
Anti-Ulcer Agents - chemical synthesis
Anti-Ulcer Agents - pharmacology
Benzimidazoles - chemical synthesis
Benzimidazoles - pharmacology
Calorimetry, Differential Scanning
Chromatography, High Pressure Liquid
Emulsification/solvent evaporation
Gastric resistance
In vivo ulcer evaluation
Male
Microparticles
Microscopy, Electron, Scanning
Omeprazole - analogs & derivatives
Omeprazole - chemical synthesis
Omeprazole - pharmacology
Pantoprazole
Polymer
Rats
Rats, Wistar
Release profile
Reproducibility of Results
Sensitivity and Specificity
Solubility
Sulfoxides - chemical synthesis
Sulfoxides - pharmacology
Tablet
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Summary: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).
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2006.01.013