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Received July 7, 2010
Accepted August 26, 2010
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Stability-enhanced solid dispersion formulation of amorphous raloxifene hydrochloride
College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156-756, Korea 1Chong Kun Dang Pharmaceutical Corporation, 864-1, Iui-dong, Yeongtong-gu, Suwon-si, Gyeonggido 443-270, Korea
Korean Journal of Chemical Engineering, November 2010, 27(6), 1906-1909(4), 10.1007/s11814-010-0409-y
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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 filmcoated 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 ℃ and 75% R.H. In comparative dissolution study of reference tablet (Evista®) and SDT, the similarity factor (f2) 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.
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