DESIGN AND DEVELOPMENT OF MODIFIED RELEASE DOSAGE FORM OF BCS CLASS-III DRUG BY NOVEL PASTILLATION TECHNIQUE

The primary goal of this study was to evaluate solid lipids as an alternative to polymers in the formulation of oral modified-release pastilles. Lipids have been used in pharmaceuticals since ancient times for a variety of purposes. They are used as polymer substitutes in the development of dosage forms. The solvent-free technique of pastillation uses lipids to formulate a modified-release oral dosage form explored in this research study. The melt solidification apparatus was developed at the laboratory scale to formulate hemispherical-shaped pastilles using solid lipid stearic acid; the apparatus was optimized by applying a 2³-factorial design in Minitab. Three factors (X1 needle gage, X2 dropping height, and X3 base plate temperature) were considered and studied at 2-level.Optimized conditions were found to be ideal dropping height of 1 cm, a needle gauge of 20 G, and a cooling plate temperature of 4°C. Pastilles were characterized for drug content uniformity, 94 ± 1.64% to 98.8 ±1.03%; drug release of the F8 batch showed 99.98% ± 1.09 drug release at 12 hr; an angle of contact greater than 95° ±0.45 was considered optimal for hemispherical-shaped pastilles with good flow and uniform size weight, which sustained drug release for 12 hr. These pastilles were then filled into “0” sized capsules and sachets. Compared to melt extrusion and freeze pillarization, the pastillation method is more convenient for formulating lipid-based dosage forms. Large-scale manufacturing is possible as the equipment for pastillation, the “Rotoformer,” has already been established in the chemical and agrochemical industries.