Entry of the New Quinolone Antibacterial Agents of Ofloxacin and NY-198 into the Central Nervous System in Rats
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概要
- 論文の詳細を見る
The present study describes quantitatively the pharmacokinetics of the antibacterial agents, of loxacin and NY-198 (quinolonecarboxylic acid derivatives), in the central nervous system in rats by physiological modeling of the penetration, distribution and sequestration processes. The simulation curves corresponded well with the observed concentrations in the cerebrospinal fluid (CSF) and various brain regions after intravenous bolus administration. The estimated cerebrovascular diffusion clearances were considerably small compared with reported serum flow rates and similar among the brain parenchymal tissues examined. The distribution volume of each drug in each brain region was almost the same as the brain extracellular space (15 to 25% of the wet weight). It was also found that the K_p values of these drugs were similar among the various brain regions. These lines of evidence suggest that the antibacterial agents, ofloxacin and NY-198,localized only in the brain extracellular space and exhibited little region-specificity in distribution into the brain. Moreover, it was suggested from unexpectedly low CSF : serum concentration ratios after intravenous administration that these quinolones, which once diffused into CSF, could be sequestrated from CSF to blood via some transport system.
- 公益社団法人日本薬学会の論文
著者
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Tsuji Akira
Faculty Of Pharmaceutical Sciences Kanazawa University
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Tsuji Akira
金沢大学 薬
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Sato Hitoshi
Faculty of Pharmaceutical Sciences, Showa University
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Tsuji A
Kanazawa Univ. Ishikawa Jpn
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Nagata O
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Nagata Osamu
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kato H
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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KATO Hideo
Faculty of Engineering Chiba University
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Okezaki Eiichi
Faculty Of Pharmaceutical Sciences Kanazawa University:central Research Laboratory Hokuriku Seiyaku
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YAMAMOTO Setsuko
Faculty of Pharmaceutical Sciences, Kanazawa University
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NAGATA Osamu
Faculty of Pharmaceutical Sciences, Kanazawa University
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Kato Hideo
Nihon Bioresearch Inc.
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Sato H
Department Of Pharmacy University Of Tokyo Hospital Faculty Of Medicine University Of Tokyo
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Nagata O
Narch
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Yamamoto Setsuko
Faculty Of Pharmaceutical Sciences Kanazawa University:central Research Laboratory Hokuriku Seiyaku
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Kato Hideo
Yamaguchi Univ. Yamaguchi Jpn
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Sato Hitoshi
Faculty Of Pharmaceutical Sciences Showa University
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