Preparation, characterization and evaluation of solid dispersions of rilpivirine

Abstract

Rilpivirine (RPV) is a pharmaceutical drug used for the treatment of HIV infection. The drug

is characterized with poor aqueous solubility and dissolution rate leading to low bioavailability of the drug. Hence, there is a need for the improvement of the solubility and dissolution of such drugs. In this exertion, enhancement of the solubility and dissolution of the practically water insoluble drug Rilpivirine was achieved by solid dispersion (SD) preparation using HPC and Poloxamer by kneading method and solvent evaporation method in 1:3 and 3:1 ratios which eventually leads to bioavailability enhancement. The SD's were characterized by Fourier transform infrared spectroscopy and X-ray powder diffraction studies and also evaluated by Powder dissolution studies. It was found that the SD's formed showed the absence of crystalline nature of the drug and its conversion to amorphous state. Overall, the rank order of improvement in dissolution properties of Rilpivirine with different polymers is Poloxamer > HPC, with ratios 1:3 > 3:1 and methods SE > KNE > PM > Pure drug.