title: Layered lipid microcapsules for mesalazine delayed-release in children.
abstract: The goal was to make available a delayed-release dosage form of mesalazine to be dispersed in water to facilitate swallowing in adults and children. Mesalazine microparticles containing carnauba wax were prepared by spray-congealing technique. A second step of spray-congealing of carnauba microparticles dispersed in liquefied stearic acid gave rise to mesalazine lipid microcapsules in which several carnauba microparticles remained embedded as cores in a reservoir structure. In order to favor their water dispersion, the lipid microcapsules were dry coated by tumbling them with different ratios of mannitol/lecithin microparticles prepared by spray-drying. Release rate measurements showed a delayed-release behavior, in particular a pH-dependence with less than 10% of drug released in acidic medium and complete release in phosphate buffer pH 7.4 in 4-5h. The layering with hydrophilic excipient microparticles allowed manufacturing of a pH-dependent dosage form suitable for extemporaneous oral use in adults and children.
authors: Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, 43124 Parma, Italy.
authors: Anna Giulia
authors: AG
authors: Balducci
authors: Gaia
authors: G
authors: Colombo
authors: Giuseppe
authors: G
authors: Corace
authors: Cristina
authors: C
authors: Cavallari
authors: Lorenzo
authors: L
authors: Rodriguez
authors: Francesca
authors: F
authors: Buttini
authors: Paolo
authors: P
authors: Colombo
authors: Alessandra
authors: A
authors: Rossi
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002214:Capsules; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D054709:Lecithins / Q000737:chemistry; D008353:Mannitol / Q000737:chemistry; D019804:Mesalamine / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D011109:Polymethacrylic Acids / Q000737:chemistry; D033362:Powder Diffraction; D013229:Stearic Acids / Q000737:chemistry*; D014885:Waxes / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D003692:Delayed-Action Preparations; D054709:Lecithins; D011109:Polymethacrylic Acids; D013229:Stearic Acids; D014885:Waxes; C038300:methylmethacrylate-methacrylic acid copolymer; D008353:Mannitol; C031183:stearic acid; D019804:Mesalamine; C026344:carnauba wax