Fast disintegrating pellets: Formulation and evaluation.

BACKGROUND

Extrusion-spheronization is the most commonly used technology to produce pellets using microcrystalline cellulose as a pelletizing agent. However, it has the major drawbacks of lack of disintegration and prolonged drug release. This study aimed to develop rapidly disintegrating microcrystalline cellulose-based pellets.

METHODS

Several pellet formulations were prepared via extrusion spheronization using a combination of microcrystalline cellulose, mannitol, polyethylene glycol 400(PEG 400), polyplasdone (PPXL), and croscarmellose sodium (CCS). Subsequently, they were evaluated for their physical characteristics.

RESULTS

Process optimization indicated that 500 RPM is the ideal extrusion speed. Furthermore, the best spheronization speed was to start with a speed of 3000 RPM speed to cut off the extrudate at a shorter length and then lower the speed to 1000 RPM to reduce fine production and allow for spherical pellet formation. Increasing the polyethylene glycol content to 20% and maintaining the percentages of croscarmellose sodium (15%), 15%), and polyplasdone xl (5%), respectively, demonstrated a significant improvement in disintegration time (DT).

CONCLUSIONS

MCC-based pellets with fast-disintegrating characteristics were obtained by extrusion and spheronization. Incorporating the soluble filler mannitol, hydrophilic polymer PEG 400 with super-disintegrant CCS, and PPXL 400 resulted in a more porous matrix that facilitated water entry and rapid swelling of the pellets to explode and disintegrate quickly (2 min).