口腔内速崩壊錠の開発(II)

抄録

We have established a novel direct compression method for the oral rapidly disintegrating tablet (RDT) of hydrophilic model drug ascorbic acid (VC). In this research, RDT containing the hydrophobic model drug ethenzamide (ETZ) was prepared with ordinary equipment. The formulation and preparation conditions were optimized for the preparation of RDT that has satisfactory physical strength and can be disintegrated rapidly in the oral cavity. Furthermore, we investigated the disintegration mechanism of RDT containing ETZ.

As result, to prevent the strong cohesion of ETZ, 0.5% of light anhydrous silicic acid was used as a surface modifying material for the successful coating of ETZ particles. Then, 3% of Kollidon-CL and 0.3% of magnesium stearate were added to the coated ETZ particles as disintegrant and lubricant, respectively. The tablets were prepared by the direct compression method at a pressure of 0.4 t. Similar to RDT containing VC, the prepared ETZ tablets had a mean strength greater than 30 N and a friability less than 0.5% and could disintegrate within 30 seconds. This result suggested that our method may find wide application for RDT of both hydrophilic and hydrophobic drugs. Scanning electron microscopy observation found that the structure of a tablet cross-section was different in the process methods, with the direct compression method having a smaller contact angle and shorter wetting time as compared to the wet compression method. Furthermore, the tablets prepared by the direct compression method showed 30% higher pore volume than those of the wet compression method. The disintegration mechanism of RDT containing ETZ was supposed to be both the wetting and swelling.