FORMULATION OF SELF EMULSIFYING TABLET OF RALOXIFENE HYDROCHLORIDE AND METHOD OF THEREOF

摘要

Raloxifene Hydrochloride (RLX) is a SERM used for treatment of osteoporosis and prevention of breast and endometrial cancer. RLX has poor bioavailability with extensive first pass metabolism. The present study was aimed to tailor RLX-loaded self emulsifying tablet to increase bioavailability and promoting absorption through lymphatic system to avoid first pass metabolism.The optimized batch of liquid SEDDS was formulated with RLX (40 mg/ml), Capmul MCM (20%), Tween 20 (53.4%) and PEG 200 (26.6%). Liquid SEDDS was converted into Solid SEDDS using three different methods, adsorbents, Lyophilization and spray drying. After screening, it was concluded that S-SEDDS prepared by spray drying was most efficient as compared to others. Colloidal silica was used as a hydrophobic carrier to convert L-SEDDS to S-SEDDS. A 32 factorial design was used to optimize the formulation parameters. Powder XRD studies of S-SEDDS demonstrate decrease in crystallinity of RLX, while SEM indicated complete incorporation of Liquid SEDDS into solid SEDDS and non-spherical shape of the particles. Self emulsifying tablet was prepared by using optimized batch of S-SEDDS and dissolution profile of tablet was compared with marketed formulation, Stability study results were found to be stable.