Preparation and In Vivo Efficacy Study of Pancreatin Microparticles as an Enzyme Replacement Therapy for Pancreatitis
Autor: | Rupali Namdeo Meshram, Amrita Bajaj, Sonali R. Naikwade |
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Rok vydání: | 2009 |
Předmět: |
Male
Pancreatitis Alcoholic Polymers Chemistry Pharmaceutical Drug Compounding Pharmaceutical Science Capsules Dispersant Dosage form Diffusion chemistry.chemical_compound Drug Delivery Systems Differential scanning calorimetry Cellulose acetate phthalate In vivo Drug Discovery Animals Denaturation (biochemistry) Particle Size Rats Wistar Microparticle Pancreas Pharmacology Chromatography Organic Chemistry Microspheres Rats Disease Models Animal Biochemistry chemistry Delayed-Action Preparations Methyl cellulose Pancreatin Female |
Zdroj: | Drug Development and Industrial Pharmacy. 35:417-432 |
ISSN: | 1520-5762 0363-9045 |
Popis: | Deficiency manifestations because of pancreatic insufficiency are treated by oral administration of pancreatic enzymes. As pancreatic enzymes get denatured in hostile acidic conditions of stomach, this investigation was aimed at formulating multiparticulates of pancreatic enzymes coated with enteric polymers such as eudragit L100, cellulose acetate phthalate, and hydroxyl propyl methyl cellulose phthalate, which will circumvent gastric inactivation in addition to providing optimal mixing with chyme. Pancreatin microspheres were prepared by emulsification phase separation by nonsolvent addition and solvent evaporation techniques. This process was optimized for core : coat ratio (1:0.5), stirrer speed (350-400 rpm), dispersant concentration, and amount of nonsolvent added to precipitate microspheres. Optimized formulations were assessed for % enzyme content, acid resistance, flow properties, particle size, particle morphology (by standard electron microscopy), compatibility of drug and polymer in formulation (by differential scanning calorimetry), in vitro release kinetics, and in vivo efficacy study in pancreatitis-induced animal model. Capsules containing enteric-coated pancreatin microspheres offered adequate protection to enzymes and prevented their denaturation in acidic environment. Developed multiparticulate dosage forms promoted effective mixing, instant and complete in vitro release compared with marketed tablets. |
Databáze: | OpenAIRE |
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