Abstract
Novel
orally disintegrating system based on multiparticulate form was
developed, offering an alternative to encounter major issues in the
design of dosage form for pediatric patients, i.e. the difficulty in
swallowing large solid dosage form (tablet or capsule), and the
requirement to cover a broad range of doses for different age groups.
Microcrystalline cellulose-based pellets containing acetaminophen were
prepared via extrusion/spheronization followed by freeze-drying. The in
vitro disintegration behavior of these pellets was quantitatively
measured with a texture analyzer. Mercury intrusion and gas adsorption
techniques, scanning electron microscopy of pellet surface and
cross-section were performed in order to characterize their internal
porous structure. Pellets characteristics such as size distribution,
sphericity, friability and drug release were also determined. The
developing process was able to produce pellets containing high drug
loading (25, 50 and up to 75%, w/w) with good sphericity (aspect ratio
∼1) and low friability. The pellets exhibited an instantaneous
disintegration upon contact with water, which was indicated by two
parameters: the disintegration onset was approximating to 0, and the
disintegration time less than 5 seconds. The fast disintegration
behavior is correlated with the pellet internal structure characterized
by a capillary network with pore diameter varying from 0.1 to 10 μm.
Such a structure not only ensured a rapid disintegration but it also
offers to freeze-dried pellets adequate mechanical properties in
comparison with conventional freeze-dried forms. Due to pellet
disintegration, fast dissolution of acetaminophen was achieved, i.e.
more than 90% of drug released within 15 minutes. This novel
multiparticulate system offers novel age-appropriate dosage form for
pediatric population owing to their facility of administration (fast
disintegration) and dosing flexibility (divided and reduced-size solid
form).
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Formulation