書誌事項
- タイトル別名
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- Pharmacokinetics of garenoxacin in laboratory animal species
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抄録
The pharmacokinetics of a novel des-fluoro (6)-quinolone antibacterial agent, garenoxacin mesilate hydrate (GRNX), was investigated using several laboratory animal species. GRNX was rapidly absorbed and widely distributed into most tissues/organs except the cerebrum and spinal cord. Radioactivity was completely excreted from the body after the administration of [14C] GRNX in rats and monkeys, suggesting low persistence of GRNX. The linearity of systemic exposure on laboratory animal species was suggested among the dose range tested in this study (rats: 2 to 25mg/kg, dogs: 8 to 75mg/kg, and monkeys: 25 to 100mg/kg). The in vitro serum protein binding of GRNX was consistent in GRNX concentrations tested on mice, rats, dogs, monkeys, and humans (mice: 66.7 to 71.9%, rats: 86.5 to 89.0%, dogs: 64.5 to 67.6%, monkeys: 71.2 to 74.5%, and humans: 78.3 to 84.0%). The urinary recovery of GRNX in rats decreased with increasing dose. However, that in dogs was consistent at each dose; species difference was observed in the urinary excretion of GRNX. Systemic exposure of GRNX in female rats was lower than that in male rats (about 33% of AUC0-∞in male), the gender difference was observed. No gender difference was observed in biliary and urinary excretion of radioactivity. One of the reasons for the gender difference in systemic exposure of GRNX is GRNX metabolism.
収録刊行物
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- 日本化学療法学会雑誌
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日本化学療法学会雑誌 55 (Supplement1), 78-86, 2007
公益社団法人 日本化学療法学会
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詳細情報 詳細情報について
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- CRID
- 1390282681264734592
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- NII論文ID
- 10019948584
- 130004298351
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- NII書誌ID
- AN10472127
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- ISSN
- 18845886
- 13407007
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可