Solubilized formulation and evaluation of Reloxifene for prevention and treatment of osteoporosis in postmenopausal women

 

By M.D.Dhanaraju, Yarra. Roopa Rani, G.Thirumurugan

Abstract

An increasing number of new chemical entities emerging from drug discovery and reaching drug development are poorly or very poorly water soluble. Our study aimed at developing solubilized formulation and evaluation of insoluble drug raloxifene (RLX) with improved bioavailability for the treatment of osteoporosis in postmenopausal women. Preformulation studies were conducted to determine the physical characteristic of drug like bulk density, particle size and solubility. Solid dispersions were prepared by hot melt method by employing 6 different carriers and mixing ratios (1:1, 1:2, and 1:3). And selection of suitable complexing agent/ carriers and ratio was done on the basis of solubility. DSC studies were made to define the physical state of drug in the carrier and possible interaction of RLX- carrier complex. Compatibility of excipients with RLX- carrier complex was tested with regard to their taste, in order to increase the palatability of the RLX formulation. Totally 10 trial bathes of RLX formulation were conducted to select prototype formula, batch S0010 was selected as optimized formulation. The best formulation obtained was investigated by preliminary stability studies at fresh (stored at RT) and stressed (stored at 40ºC & 75% RH for 1 month) conditions and initial RLX formulation were compared with aged (1 month) one. No substantial changes in its stability were observed.

 

Key Words : Insoluble drug, Raloxifene (RLX), Solubilization, Osteoporosis, DSC

 

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