Modification of Dissolution Profile of Rivaroxaban by spray Drying

Abstract

The objective of the present study was to enhance the solubility and modification of dissolution profile of poorly water soluble drug Rivaroxaban by formulating its biodegradable microspheres. A major challenge in the drug development and delivery process is improving aqueous solubility and rate of dissolution of drugs, which ultimately improves absorption of the drug. One of the major problems with BCS class II drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. Rivaroxaban is an oral factor Xa inhibitor. By binding reversibly to the active site of factor Xa, Rivaroxaban attenuates thrombins generate on and reduce fibrin formation. One of the possible way to overcome this outcome is to use formulate biodegradable microspheres by using spray drying technique. Spray drying is the transformation of feed from a fluid state into a dried particulate form by spraying the feed into a hot drying medium. The purpose of this research was to improve the solubility and modification of dissolution profile of Rivaroxaban by spray drying technique using Methanol and polymer like Eudragit RS100. Prepared biodegradable microspheres were evaluated for drug release profile. The compatibility and surface morphology was studied by Fourier Transforms Infrared spectroscopy (FTIR), Motic microscopy, X-Ray Diffraction (XRD) and Scanning Electron Microscopy (SEM) respectively. Prepared biodegradable microspheres were subjected to various physicochemical evaluations and in-vitro dissolution profile. The effects of different polymer concentrations on solubility enhancement and modification of dissolution profilewere studied. Stability study was carried out, result obtained after study complied with the limits. The batch with highest combination of polymer concentration with drug showed greaterenhancement in solubility.