A continuous-spray granulator (CTS-SGR) is a one-step granulation technology capable of using solutions or suspensions. The present Research Article objectives were, (1) to reduce the manufacturing operations for solid dosage formulations, (2) to make amorphous solid dispersion (ASD) granules without pre-preparation of amorphous solids of active pharmaceutical ingredients (API), and (3) to characterize the obtained SGR granules by comprehensive pharmaceutical analysis. Rebamipide (RBM), a biopharmaceutical classification system class IV drug, that has low solubility or permeability in the stomach, was selected as a model compound. Five kind of granules with different concentrations of polyvinylpyrrolidone/vinyl acetate copolymer (PVP-VA) were prepared using a one-step SGR process. All of the SGR granules could be produced in amorphous or ASD form and their thermodynamic stability was very high because of high glass transition temperatures (>178 degrees C). They were unstable in 20 degrees C/75%RH; however, their stability was improved according to the proportion of polymer. The carboxy group of RBM was ionized in the granules and interactions appeared between RBM and PVP-VA, with the formation of an ASD confirmed and the solubility was enhanced compared with bulk RBM crystals. The SGR methodology has the possibility of contributing to process development in the pharmaceutical industry.

• Musashino University
• University of Minnesota
• Powrex Corporation; Musashino University

• API
• Oral Dosis

1. amorphous
2. API
3. characterization
4. continuous processing
5. Granulation
6. interaction
7. molecular complex
8. Oral Dosis
9. Polymer
10. Process development
11. rebamipide
12. Research Article
13. Solid dispersion
14. stability