新規フルオロキノロン系抗菌剤Q―35の生体内動態 (第1報) ラットにおける`14´C―Q―35単回投与後の吸収および排せつ

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タイトル別名
  • Disposition of Q-35. (1). Absorption and Excretion after Single Administration of 14C-Q-35 in Rats.

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The absorption and excretion of 14C labeled Q-35[(±)-1-Cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-7-(3-methylaminopiperidin-1-yl)-4-oxoquinoline-3-carboxylic acid], a new fluoroquinolone antimicrobial agent, were studied in rats.<BR>1. When 14C-Q-35 was administered orally at the dose of 20 mg/kg to fasted rats, the radioactivity was absorbed rapidly and reached a maximum plasma concentration (Cmax) at 0.38 h, thereafter was eliminated at a half-life of 2.84 h.<BR>The AUC of the plasma radioactivity after an oral administration of 14C-Q-35 to nonfasted rats decreased to about half of AUC in fasted rats. It was suggested that there was a significant decrease in the extent of absorption by food.<BR>2. It was suggested that 14C-Q-35 was absorbed from the upper and middle segments of small intestine but scarcely from the stomach as revealed by the loop method of the digestive tracts.<BR>3. The urinary and fecal excretion rate of the radioactivity during 72 h after an oral administration of 14C-Q-35 to fasted rats were 42.2% and 56.5 % (total: 98.6%) of dose, respectively. It was suggested that the administered radioactivity was excreted in about 100% into the urine and feces.<BR>4. The biliary excretion rate during 24h after an oral administration of 14C-Q-35 to nonfasted rats was 32.3% of the dose, and the quarter of the radioactivity excreted to bile was reabsorbed.

収録刊行物

  • 薬物動態

    薬物動態 10 (5), 595-603, 1995

    日本薬物動態学会

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