Preparation, characterization, in vitro and in vivo studies of olmesartan medoxomil in a ternary solid dispersion with N-methyl-D-glucamine and hydroxypropyl-β-cyclodextrin

Olmesartan medoxomil (OM) has been used in treatment of hypertension disease, as a prodrug of olmesartan. However, its clinical application is limited by the low oral bioavailability (~28%). Ternary solid dispersion of OM was prepared with hydroxypropyl- β -cyclodextrin and N -methyl- d -glucamine to improve its oral bioavailability using roll mill ML 007. Its physicochemical characterization was measured by scanning electron microscope, differential scanning calorimetry , powder X-ray diffraction and transform infrared spectroscopy . The solutions properties of OM in ternary solid dispersion were investigated involving the solubility, dissolution profiles, 1 H NMR analysis, phase solubility study and PAMPA study. Instrument analysis results revealed an amorphous solid dispersion had been synthesized without any side-products. It also showed enhanced solubility and dissolution rate in vitro . Pharmacokinetic study demonstrated an improved oral bioavailability in vivo . The rapid storage assay showed that the chemical stability of inclusion complexes had no change. The synthesized OM ternary solid dispersion is promising to be a better alternative to its pure formation in the market with improved oral bioavailability.