2007 年 67 巻 5 号 p. 347-355
We investigated the development of oral rapidly disintegrating tablets (ORDTs) for medications that are used to prevent or treat stomatitis related to cancer chemotherapy. One of the challenges is taste masking, especially in medications with a bitter taste. We developed Chocolets, a new chocolate-flavored ORDT formulation which could be useful because the chocolate flavor can mask the bitterness. On the other hand, optimal amounts of cocoa powder and aspartame must be decided in order to preserve the physical properties of the medication and formulation itself. We use rebamipide, a gastric mucosal protectant with a strong bitter taste, as a model to investigate the optimal conditions in preparing extemporaneous Chocolets formulation.
Gas chromatography analysis suggested that the aspartame could potentiate the cocoa smell from the cocoa powder. As a result, rebamipide Chocolets using 10% cocoa powder and 1% aspartame could be the most appropriate conditions to prepare this extemporaneous formulation. This was further confirmed by Euclidean analysis by an electronic nose sensor in vitro. A clinical trial in healthy volunteers also provided similar in vivo results.
