Rifampin の体内動態

概要

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Rifampicin in single oral dose of 450mg was administered to eight healthy subjects and eleven tuberculous patients. Rifampicin in blood and urine samples was measured by high-performance liquid chromatography. Blood and urine samples were collected frequently up to 24 hrs after each dose. Data of rifampicin level in serum (Ct) were fitted by a computer. Biexponential equation, Ct=A (e-ke·t-e-ka·t), and the pharmacokinetic parameters were obtained by non linear least squares regression analysis. The data of rifampicin and 25-desacetylrifampicin in urine was fitted by a computer to sigma-minus plot. The first-pass effect was calculated by method of Gibaldi and coworkers. Vd/F and total body clearance values were higher in the tuberculous patients than in the healthy subjects. Recovery of rifampicin and 25-desacetylrifampicin in urine was lower in the tuberculous patients than in the healthy subjects. First-pass effect (%) washigher in the tuberculous patients than in the healthy subjects. On these results, it seems reasonable that the increased biliary excretion is due to a process of self-induced enzyme activity, which results in facilitation of the transfer of the antibiotic from blood to bile.
一般社団法人日本臨床薬理学会の論文