Estimation of the Rates of Available Fraction for Some 4-Substituted Acetophenone Derivatives in the Rat Reversible Drug-Metabolite Pharmacokinetics

4-Acetamidoacetophenone (Ia), 4-acetylbenzenesulfonamide (IIa) and acetohexamide (IIIa) and the respective reduced compounds, 4-substituted α-hydroxyethylphenyl derivatives, are in a reversible drug-metabolite relationship in rats. The pharmacokinetic profiles of these agents were studied after intr...

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Published inChemical & pharmaceutical bulletin Vol. 36; no. 11; pp. 4612 - 4618
Main Authors NAGAMINE, SACHIKO, OTAWA, TOMOKO, NAKAE, HIROKO, ASADA, SHOZO
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 01.11.1988
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Summary:4-Acetamidoacetophenone (Ia), 4-acetylbenzenesulfonamide (IIa) and acetohexamide (IIIa) and the respective reduced compounds, 4-substituted α-hydroxyethylphenyl derivatives, are in a reversible drug-metabolite relationship in rats. The pharmacokinetic profiles of these agents were studied after intraportal (pv) administration in comparison with those after intravenous (iv) administration using an interconversion model. Fundamental clearances, CL10, CL12, CL20 and CL21, were calculated using four AUC (area under the plasma concentration-time curve) values obtained after iv administration of the drug and preformed metabolite. The hepatic available fraction of parent drug, FH1 and sequential hepatic available fraction of its metabolite, FH2 were estimated by the following equations.
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content type line 23
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.36.4612