Stability-enhanced solid dispersion formulation of amorphous raloxifene hydrochloride

Abstract

To develop a stabilized formulation of amorphous raloxifene hydrochloride (RXF), solid dispersion granules (SDG) of amorphous RXF were prepared by fluidized bed granulation with non-pareil beads, compressed and film-coated to produce solid dispersion tablets (SDT). Polymorphic changes in RXF were inhibited by SDG formulation. Drug content, impurity, and dissolution profile of SDT revealed that the SDT meets the acceptance criteria, and the content of RXF was maintained over 95% for 5 months at accelerated conditions of 40 degrees C and 75% R.H. In comparative dissolution study of reference tablet (Evista (R)) and SDT, the similarity factor (f(2)) provided evidence for similar dissolution profiles between two formulations. Therefore, we suggest the usefulness of SDT for the development of generic pharmaceuticals containing amorphous RXF.