Abstract
A granule of 2-[4-(p-fluorobenzoyl)-piperidin-1-yl]-2'-acetonaphthone hydrochloride (E2001) with an enhanced dissolution rate (preparation A) prepared by a method previously reported (T. Tokumura, T. Tanaka, Yakuzaigaku, accepted) was evaluated by the dissolution test and its bioavailability in beagle dogs was determined. The dissolution rate of E2001 from preparation A at pH 6.0-6.8 was increased significantly in comparison with that from preparation B (a physical mixture of the same formula). There was no significant difference in Cmax, area under the concentration-time curve (AUC0-6h), or Tmax between preparations A and B when a dose equivalent to 20 mg of E2001 was administered to the beagle dogs. However, a significant difference was observed between the AUC0-6h values after oral administration of the two preparations with NaHCO3. These findings suggest that the bioavailability of E2001 from the oral administration preparation A will be higher than that of preparation B.
