European Journal of Biomedical and Pharmaceutical Sciences

INVESTIGATION OF THE EFFECT OF FORMULATION ADDITIVES ON TELMISARTAN DISSOLUTION RATE: DEVELOPMENT OF ORAL DISINTEGRATING TABLETS

Maysa A. Hussien*, Ebtessam A. Essa and Sanaa A. El Gizawy

ABSTRACT

The aim of this work was to enhance solubility of telmisartan by the preparation of amorphous solid dispersion in presence and absence of pH modifying agent. This was achieved by preparing solid dispersion (SD) of telmisaratin with a hydrophilic polymer (polyethylene glycol 4000), in presence and absence of meglumine. The latter was used as alkanizer. Binary solid dispersion was prepared by solvent evaporation technique at different drug:polymer weight ratios. To selected formulation, meglumine was included as third component at different molar ratios to obtain ternary mixtures. The obtained microparticles were evaluated using differential scanning calorimetry (DSC), Foriur Transform Infrared (FTIR), X-ray powder diffraction and in vitro drug release studies. Binary solid dispersion slightly improved drug dissolution over unprocessed drug. The optimum SD combination was formulated into oral disintegrating tablets using different ODT bases namely Pearlitol® Flash, Pharmaburst ® 500 and Ludiflash®. Incorporation of meglumine markedly increased telmisartan dissolution with about 80% of the loaded dose librated after 5 minutes. Physical characterization indicated compatibility between ingredients and reduced drug crystallinity. The optimum formulation was sucessfully used to prepare orodispersible tablets, with those prepared using Pharmaburst ® 500 as filler showed optimum tablets quality and drug release pattern, compared to other fillers.

Keywords: Telmisartan, meglumine, solid dispersion, pH modifier, fast disintegrating tablets.