Formulation and Evaluation of Sublingual Tablet of Solid Dispersion of Raloxifene Hydrochloride

Abstract

Raloxifene Hydrochloride is an oral selective estrogen receptor
modulator (SERM) which is used to treat and prevent osteoporosis and
breast cancer in postmenopausal women. It has very low oral
bioavailability of approximately 2% due to extensive first pass
metabolism and poor aqueous solubility. The present investigation was
aimed to develop the sublingual tablet containing solid dispersion of
Raloxifene Hydrochloride to improve its oral bioavailability. Solid
dispersions of drug were prepared by using different hydrophilic polymer
such as HPMC, Eudragit S100, PEG 6000 by solvent evaporation and
physical mixing method. Solid dispersions prepared with HPMC (SD7)
by solvent evaporation method found best based on improvement in
aqueous solubility, % drug content and % yield. Sublingual tablet
containing solid dispersion was prepared by direct compression method
by using cross povidone as super disintegrating agent. Powder blend of
all the formulation before compression was evaluated for bulk density,
tapped density, Carr’s index, Hausners ratio, angle of repose and was
found to be free flowing.
Prepared tablets were evaluated for thickness, hardness, weight uniformity, friability, wetting time, water
absorption ratio, % drug content, dispersion time, in-vitro drug release study and stability studies. Results
of in-vitro drug release studies revealed improved i.e 97.12±59% drug release and dissolution up to 30
min.