Absorption, distribution and excretion of [<SUP>14</SUP>C] gatifloxacin after repeated oral administration in rats

  • Idesawa Akira
    Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.
  • Machida Masaaki
    Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.
  • Yuasa Ryuzo
    Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.
  • Komuro Masakatsu
    Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.
  • Ishida Ryozo
    Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.
  • Uchida Hiroshi
    Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.

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  • [<SUP>14</SUP>C] Gatifloxacinのラットにおける反復経口投与時の吸収, 分布, 排泄

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Abstract

We investigated the absorption, distribution, and excretion of [14C] gatifloxacin (GFLX) during and after repeated oral administration at a once-daily dose of 10 mg/kg for 14 days in rats.<BR>1) Radioactivity in the blood 1 hour after each oral administration ranged from 0.63 to 0.88μg ea./mL.and radioactivity at 24 hours reached a steady state, 0.04μg eq./mL, after the 6th dose.There was no significant change in pharmacokinetic parameters between the first and last days.<BR>2) One hour after the 14th administration, radioactivity in the kidney, spleen, and liver were higher than in other tissues: 7.55, 4.17, and 3.77μg eq./g, respectively.On the other hand, radioactivity in the brain, eyeball, and fat tissues were less than half of that in the blood. Radioactivity in almost all tissues except the bone decreased to the limit of detection (below 0.01μg eq./g) by 192 hours after the final dosing.<BR>3) The daily excretion of radioactivity into urine and feces during repeated dosing ranged from 22.2 to 34.7% and from 68.2 to 84.3% of the daily dose, respectively.Nearly all of the excretion of the total dose in urine and feces was 28.4% and 78.6%, respectively, within 192 hours after the last dosing.

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