Evaluation of a Pharmaceutical Preparation of 2-[4-(p-Fluorobenzoyl)-piperidin-1-yl]-2'-acetonaphthone Hydrochloride with Enhanced Dissolution Rate

概要

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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 C_<max>, area under the concentration-time curve (AUC_<0-6h>), or T_<max> 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 AUC_<0-6h> values after oral administration of the two preparations with NaHCO_3. These findings suggest that the bioavailability of E2001 from the oral administration preparation A will be higher than that of preparation B.
社団法人日本薬学会の論文
1994-08-15