A continuous-spray granulator (CTS-SGR) is a one-step granulation technology capable of\nusing solutions or suspensions. The present research objectives were, (1) to reduce the manufacturing\noperations for solid dosage formulations, (2) to make amorphous solid dispersion (ASD) granules\nwithout pre-preparation of amorphous solids of active pharmaceutical ingredients (API), and (3) to\ncharacterize the obtained SGR granules by comprehensive pharmaceutical analysis. Rebamipide\n(RBM), a biopharmaceutical classification system class IV drug, that has low solubility or permeability\nin the stomach, was selected as a model compound. Five kind of granules with different concentrations\nof polyvinylpyrrolidone/vinyl acetate copolymer (PVP-VA) were prepared using a one-step SGR\nprocess. All of the SGR granules could be produced in amorphous or ASD form and their\nthermodynamic stability was very high because of high glass transition temperatures (>178 DegreeC).\nThey were unstable in 20 DegreeC/75%RH; however, their stability was improved according to the\nproportion of polymer. The carboxy group of RBM was ionized in the granules and interactions\nappeared between RBM and PVP-VA, with the formation of an ASD confirmed and the solubility\nwas enhanced compared with bulk RBM crystals. The SGR methodology has the possibility of\ncontributing to process development in the pharmaceutical industry.
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