Comparative Pharmacokinetics of Sulpiride and N-[(1-Butyl-2-pyrrolidinyl)methyl]-2-methyl-5-sulfamoyl-2,3-dihydrobenzofuran-7-carboxamide Hydrochloride, a New Lipophilic Substituted Benzamide in Rats

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The pharmacokinetics of a new lipophilic substituted benzamide N-[(1-butyl-2-pyrrolidinyl)methyl]-2-methyl-5-sulfamoyl-2,3-dihydrobenzofuran-7-carboxamide hydrochloride (1) and sulpiride in both plasma and brain were investigated in rats.The octanol-water partition coefficients of the base of 1(2) and sulpiride were 6.3 and 0.2,respectively. The eliminations of 2 from plasma and brain were similar to those of sulpiride. The systemic bioavailabilities of 1 and sulpiride after oral administration of 200 mg/kg were 60.9±10.9 and 18.2±6.4%, respectively. The brain concentrations of 2 were about 2-3 times higher than those of sulpiride until 4 h after oral administration of 100 mg/kg. The brain/plasma ratios of 2 were about 2 times higher than those of sulpiride. These results indicate that the penetration of 2 through the gastrointestinal membrane and/or the blood-brain barrier are higher than those of sulpiride.
社団法人日本薬学会の論文
1990-09-25