Design and development of co-processed excipients for fast dissolving tablets of Irbesartan by melt agglomeration technique

Abstract

The co-processing is most widely explored method for development of directly compressible excipients. The present research was focused on development of co-processed excipients for fast dissolving tablets of Irbesartan by melt agglomeration technique. From the preliminary trials Lactose monohydrate and mannitol was selected as a diluent and Poly ethylene glycol 4000 as binder. To improve functionality of co-processed excipients 8 % crospovidone was incorporated. Diluent blend ratio and concentration of binder (%) were selected as independent variables in central composite design. The agglomerates were evaluated in terms of % fines, angle of repose, Carr’s index, Hausner ratio. The tablets were manufactured on a rotary press and their friability, tensile strength and disintegration time were evaluated. This optimized batch was characterized by means of the granular friability index, Heckel analysis, Kawakita, Kuno’s analysis, lubricant sensitivity ratio and a dilution potential study. Result of dilution potential showed that up to 40 % drug can be incorporated. In addition to these, bitter taste of drug was masked by forming drug—β-cyclodextrin inclusion complex and by adding aspartame as a Sweetener. Compared to conventional tablet it showed faster dissolution. Instrumental studies like Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray diffraction showed that the compatibility of various excipients with drug. The present study underlines the fact that melt granulation technique may be adopted for the development of directly compressible adjuvant for use in pharmaceuticals.