METABOLIC FATE OF TE-031 (A-56268)(VI):ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF TE-031 IN MONKEYS
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The metabolic fate of <SUP>14</SUP>C-TE-031 was studied in monkeys, and compared with that of erythromycin by microbiological assay.<BR>After oral administration of <SUP>14</SUP>C-TE-031 (5 mg/kg), radioactivity in blood reached a peak of 1.5μg eq./ml at 2 h, and the AUC0-24h value was 12.0μg·h/ml. Two hours after oral administration, the highest radioactivity was observed in liver, and almost all other tissues-including lung, bone marrow and kidney-contained higher radioactivity than plasma. After intravenous administration, on the other hand, the highest concentration was observed in lung, suggesting high affinity of TE-031 to lung tissue. Furthermore, high radioactivity was observed in gallbladder bile. The amount of unchanged TE-031 in the lung was remarkably high, while other tissues contained appreciable amounts of N-demethyl TE-031 (M-1) and the active metabolite, (14 R)-14-hydroxy TE-031 (M-5), as well as unchanged TE-031.<BR>The excretion route was mainly via feces, and fecal and urinary recovery within 7 days after oral administration was 69.2% and 24.1%, respectively. M-1 and M-5 were the main metabolites in urine and feces. Compared by microbiological assay, the peak plasma concentration of TE-031 was four times that of EM. The half-life and AUC value were also rather higher in the case of TE-031. Systemic availability (assessed by comparing the AUC value after oral and intravenous administration) was about 70% in TE-031, but only about 20% in EM. After oral administration of TE-031, concentration in each tissue including the lung was considerably higher than in plasma. Urinary and fecal recovery of TE-031 after oral administration was 11.8% and 4.0% of the dose, but was very low in the case of EM.
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公益社団法人 日本化学療法学会 | 論文
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