Background:
The Microcrystalline Cellulose is called as a gold standard for the manufacture of
pellets. The poor disintegration leads to incomplete drug release restricts the use of MCC in the
immediate-release formulation.
Objective:
The present work aims to explore non-MCC extruder aid for pellet formulation and
solubility modulation potential of Aeroperl®
300 Pharma.
Methods:
Bicalutamide (BCL) was selected as a model BCS class-II drug. The solubility of BCL
was assessed in different vehicles like polyethylene glycol, propylene glycol, and Tween by
carrying out phase solubility study. The suitable vehicle was selected based on the higher solubility
of BCL. The vehicle was further adsorbed on newer adsorbent Aeroperl®
300 Pharma to formulate
liquisolid granules. The liquisolid granules were further incorporated into the pellet using mannitol
and microcrystalline cellulose as an extruder aid. Box-Behnken design was adopted for
optimization of formulation considering MCC: mannitol ratio, concentration of HPMC and
spheronizer speed as independent factors whereas drug release at 30 min, disintegration time and
aspect ratio were selected as dependent variables. The pellets were evaluated for different
evaluation parameters.
Results:
Propylene glycol was selected for the formulation of liquisolid technique based on the
results of the phase solubility study. Propylene glycol containing BCL was adsorbed on Aeroperl
300 Pharma. The optimized batch was selected exploring the Design-Expert software by
considering limits of different responses. Pellet had excellent flowability. Friability was found to
be within the range (<1%). Pellets were found to be spherical and had pores on the surfaces.
Conclusion:
Liquisolid granules containing newer solubilizer Aeroperl was found to be a
promising approach for the improvement in the solubility of the drug. The use of mannitol with
MCC has a profound effect on disintegration time, without altering flow property and other
parameters. No patents were reported on the combination of Bicalutamide, mannitol and Aeroperl.
The critical finding of the present work is to use mannitol as an extruder aid to fasten the
disintegration leads to complete drug release within a short period of time. Aeroperl and Mannitol,
MCC: mannitol ratio, concentration of HPMC and spheronizer speed was found to be significant
and had the potential effect in pellet formulation.
Solubility Determination of Tris(hydroxymethyl)aminomethane in Water + Methanol Mixtures at Various Temperatures Using a Laser Monitoring Technique
