Development of taste masked fexofenadine hydrochloride orodispersible tablets using hot melt extrusion

Abstract

Orodispersible tablet desired the oral solid formulations with a pleasant taste, and a rapid disintegration in the mouth with no need of water. In this study, orodispersible tablet formulations of fexofenadine HCl, a second generation anti-histamine drug were developed for pediatric and geriatric patients. To improve patient compliance, bitter taste masking using hot melt extrusion (HME) technology was studied. Fexofenadine HCl and Eudragit® EPO extruded powder at three different drug loadings (20%, 40% and 60%) was prepared by HME at various temperature (120°C, 150°C and 180°C). Physicochemical characterization using FT-IR spectroscopy, powder X ray diffraction and differential scanning calorimetry revealed that the amorphous state or molecularly dispersed state of fexofenadine HCl in HME powder was obtained at lower drug/polymer ratio and higher temperature. The HME powder extruded at 180°C was selected to prepare orodispersible tablet formulations. The orodispersible tablets with drug containing HME powder had physical properties conforming to pharmacopoeial standards, including weight variation, hardness, friability, disintegration time and drug dissolution in 0.1 N HCl. The taste masking performance using drug release test in simulated salivary fluid indicated that the orodispersible tablets had lower drug release, thus enabling taste masking effect in oral cavity. In conclusion, fexofenadine HCl orodispersible tablets with desired taste masked effect were successfully prepared by using hot melt extrusion technology.