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.

Optimisation and scale-up of a highly-loaded 5-ASA multi-particulate dosage form using a factorial approach / G. Di Pretoro, L. Zema, L. Palugan, D. Wilson, S. Rough, A. Gazzaniga. - In: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0928-0987. - 45:1-2(2012), pp. 158-168. [10.1016/j.ejps.2011.11.005]

Optimisation and scale-up of a highly-loaded 5-ASA multi-particulate dosage form using a factorial approach

G. Di Pretoro
Primo
;
L. Zema
Secondo
;
L. Palugan;A. Gazzaniga
Ultimo
2012

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.
5-Aminosalicylic acid; Design of experiment; Extrusion-spheronisation; Multi-particulate dosage form; Statistical optimisation
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
2012
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/175924
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