Qihong Zhang, R. Wei, A. Dushkin
Apr 1, 2020
Citations
0
Influential Citations
16
Citations
Quality indicators
Journal
Journal of Drug Delivery Science and Technology
Abstract
Abstract 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, 1H 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.