EFFECTS OF EXCIPIENTS ON THE TECHNOLOGICAL PROPERTIES OF GRANULAR MATERIALS BASED ON SUBSTANCES FROM A GROUP OF PROTON PUMP INHIBITORS

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DOI: https://doi.org/None
Issue: 
5
Year: 
2016

N.V. Mironcheva, A.L. Marchenko, PhD Saint Petersburg State Chemopharmaceutical Academy; 14, Lit. A, Prof. Popov St., Saint Petersburg 197376, Russian Federation

Introduction. The drugs from a group of proton pump inhibitors (PPIs) are most effective in treating acid-dependent diseases of the gastrointestinal tract. PPIs act directly in the duodenum and other parts of the small intestine so they are manufactured as modified release formulations. Objective. To elaborate a comprehensive approach to designing technologically stable granular materials containing substances from a group of PPIs. Material and methods. The investigation used 3 PPIs: omeprazole, rabeprazole, and esomeprazole. The prepared model mixtures varied in the types of an excipient (lactose, microcrystalline cellulose, corn starch, mannitol, and calcium hydrophosphate), which was 60-70 mass%. Granular materials were obtained by humid granulation using punches and dried at a temperature of 45-50 C. Results. The main technological characteristics of substances from the PPI group were analyzed. Their granular materials were prepared using different excipients. The technological properties of the granular materials moistened with organic and inorganic solvents were investigated. The optimal wetting agent was chosen for granulation when manufacturing the drug. Conclusion. The granular materials of omeprazole, rabeprazole, and esomeprazole with different excipients were examined. The best excipient (mannitol) and the best wetting agent (polyvinylpyrrolidone) were established. Analysis of the hygroscopicity of the granular materials obtained revealed their instability during high ambient humidity.
Keywords: 
proton pump inhibitors
fractional composition
hygroscopicity
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