Reparation of controlled release spheronized beads by simple extrusion and modified spheronization process.

Beads loaded with the water-soluble drug, phenylpropanolamine HCl (PPA), were prepared using an extruder and double arm counter-rotating roller modified from a traditional pill machine. The mean diameter of the cylindrical rod-like extrudate from the ram extruder was 3 mm; that of the uncoated bead after cutting and spheronization by the modified double arm counter-rotating roller was 3.26-3.28 mm. Although the surface of the beads was moderately rough and irregular, some exhibited hump-shaped protrusions, the sphericity was acceptable (roundness 1.15) and adequate for the subsequent coating process. An increase in mean diameter of the coated beads and improvements in friability and sphericity were observed in proportion to the amount of coating material applied (ethylcellulose or Eudragit RS 100). It was also found that the release rate of PPA from the coated beads could be controlled by the amount and type of coating materials applied or with the incorporation of Eudragit RS 100 into the core matrix. Further modifications to the double arm counter-rotating roller, including adjustment of the rotation speed and distance between the rollers, would yield smaller uncoated beads with improved roundness and surface roughness. In conclusion, the present method could be potentially applied to prepare controlled release drug delivery beads or pellet dosage forms.