MULTIPLE UNIT PELLET SYSTEM (MUPS) BASED FAST DISINTEGRATING DELAYED-RELEASE TABLETS FOR PANTOPRAZOLE DELIVERY
Keywords:Multiple Unit Pellet System (MUPS), Ceolus, Celphere, Delayed Release Pellets, Pellet Compression, Extrusion-Spheronization, Drug Layering
Objective: The rationale for the study was to develop multiple unit pellet system (MUPS) of delayed release pantoprazole with desired physical properties and unaltered drug release profile from pellets even after compression into a fast disintegrating tablet.
Methods: In the presented study, delayed release pellets of pantoprazole were developed by two methods, i.e. extrusion-spheronization and drug layering techniques, coated using enteric polymer and subsequently compressed in to tablet. In drug layering technique, pantoprazole was loaded on CelphereÂ®102 (microcrystalline cellulose spheres) as well as on SugletÂ® (sugar spheres) in fluid bed processor. Acid resistant polymer Eudragit ND 30D was subsequently coated on each type of drug loaded pellets. Suitable tableting excipients were prepared such as soft pellets, CeolusÂ® (fibrous grade of microcrystalline cellulose) granules, LudipressÂ® (compressible lactose composition), AvicelÂ® PH 200 and different combination of them. Various factors like property of pellets to be compressed, coating level, the composition of tableting excipient and ratio of drug-loaded pellets to tableting excipients were identified and optimized.
Results: MUPS with delayed releasing pellets of pantoprazole proved to provide sufficient hardness, rapid disintegration property, and unaltered release profile after compression. Delayed release pantoprazole pellets prepared by drug layering on celphereÂ® 102 followed by coating with EudragitÂ® NE 30D showed better compressibility to withstand the drug release properties. The combination of CeolusÂ® granules and Ludipress (in 1:1 ratio) was found to be suitable tableting excipient that helped compression of pellets without rupturing polymeric coat. Pellets to excipients ratio at 1:3 was found optimum.
Conclusion: Compaction behaviour of pantoprazole delayed-release pellets without loss of original delayed release profile was achieved by formulating as MUPS based tablet of pantoprazole delayed release pellets using celephereÂ® 102 was developed which was found suitable for desired release profile and physical properties.
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