Development and evaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granules prepared by hot melt extrusion

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2011-09, Vol.86 (2), p.275-284
• Main Authors: Gryczke, Andreas, Schminke, Silke, Maniruzzaman, Mohammed, Beck, Julien, Douroumis, Dennis
• Format: Article
• Language: English
• Subjects: Administration, Oral; Adolescent; Adult; Carboxymethylcellulose Sodium - chemistry; Chemistry, Pharmaceutical - methods; Chromatography, High Pressure Liquid; colloids; composite polymers; crosslinking; Disintegration; dispersions; Drug Compounding - methods; Extrusion; Female; Granular materials; Granules; Hardness; Hot Temperature; Hot-melt extrusion; Humans; Ibuprofen; Ibuprofen - chemistry; Male; Masking; melting; Orally disintegrating tablets Eudragit EPO; palatability; Polymethacrylic Acids - chemistry; polyvinylpyrrolidone; porosity; Povidone - chemistry; Pressure; sensory evaluation; Sodium; Solubility; Tablets; Tablets - chemistry; taste; Taste - physiology; Taste masking; volunteers; X-Ray Diffraction
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2011.04.007

Hot melt extrusion (HME) was used to increase the Ibuprofen (IBU) dissolution profiles and mask the bitterness of the produced dosage forms. IBU was embedded in a polymethacrylate polymer and the produced granules were incorporate in oral disintegrating tablets (ODTs). The developed dosage forms presented excellent taste masking and increased dissolution rates. [Display omitted] ► Ibuprofen and Eudragit EPO processed by hot melt extrusion at high drug loadings. ► The produced solid dispersions showed the existence of amorphous Ibuprofen. ► Hot melt extruded products were compressed to manufacture ODTs. ► Robust ODTs presented excellent mechanical strength, friability and disintegration times. ► Ibuprofen solid dispersions showed effective taste masking and increased dissolution rates. In the current study Ibuprofen was embedded in a methacrylate copolymer (Eudragit ® EPO) matrix to produce solid dispersions by hot-melt extrusion (HME) processing. The obtained granules were incorporated in orally disintegrating tablets (ODTs). The tablets were developed by varying the ratio of superdisintegrants such as sodium croscarmellose and crosslinked polyvinylpyrrolidone grades while a direct compression process was used to compress the ODTs under various compaction forces to optimize tablet robustness. The properties of the compressed tablets which included porosity, hardness, friability and dissolution profiles were further evaluated and compared with Nurofen ® Meltlet ODTs. The taste and sensory evaluation in human volunteers demonstrated excellence in masking the bitter active and improved tablet palatability.