title: Optimisation and scale-up of a highly-loaded 5-ASA multi-particulate dosage form using a factorial approach.
abstract: Pellets with high loading of 5-aminosalicylic acid (5-ASA, mesalamine) are desired to reduce the number of tablets required to deliver the daily dosing regimen. Recently, we reported an extrusion-spheronisation route for the development of a 90 wt% 5-ASA/microcrystalline cellulose formulation based on milled 5-ASA which gave good yields of pellets at the lab scale. In the present work, such formulation was optimised further by preliminary studies using a lab-scale ram extruder, and then scaled up to the pilot plant scale on a Nica screen extruder using a mixed fractional factorial approach. The final formulation featured 95 wt% 5-ASA and 5 wt% Avicel RC591 (all dry basis) and yielded spherical pellets suitable for use as the drug core of a multi-particulate DDS.
authors: Dipartimento di Scienze Farmaceutiche P. Pratesi, Via G. Colombo 71, 20133 Milano, Italy. giustino.dipretoro@unimi.it
authors: G
authors: G
authors: Di Pretoro
authors: L
authors: L
authors: Zema
authors: L
authors: L
authors: Palugan
authors: D I
authors: DI
authors: Wilson
authors: S L
authors: SL
authors: Rough
authors: A
authors: A
authors: Gazzaniga
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D002482:Cellulose / Q000737:chemistry / Q000648:ultrastructure; D055598:Chemical Phenomena; D004339:Drug Compounding / Q000379:methods; D005079:Excipients / Q000737:chemistry; D005240:Feasibility Studies; D007700:Kinetics; D019804:Mesalamine / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D033362:Powder Diffraction; D012995:Solubility; D013223:Statistics as Topic; D013499:Surface Properties; D013607:Tablets; D014867:Water / Q000032:analysis
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D013607:Tablets; D014867:Water; D019804:Mesalamine; D002482:Cellulose