Physiologically-based Pharmacokinetic Analysis of Grepafloxacin
スポンサーリンク
概要
- 論文の詳細を見る
Grepafloxacin (GPFX) is a synthetic new quinolone antimicrobial agent that possesses an extensive tissue distribution and exhibits a strong antibacterial activity in vivo. In this study, the tissue distribution characteristics of GPFX were examined using tissue concentration-time profiles following intravenous administration to rats. Subsequently, the pharmacokinetics of GPFX were analyzed based on the physiological pharmacokinetic model. The tissue-to-plasma partition coefficients (K_p) of GPFX in rats were high in all tissues except brain. A pharmacokinetic model for rabbits, monkeys and dogs was constructed using the tissue-to-plasma free concentration ratio (K_<p, f>) of GPFX in rats to simulate the GPFX concentration-time profile in plasma following intravenous administration of GPFX to each animal. The calculation-derived concentrations correlated well with the experimentally-derived data, suggesting that there are no interspecies differences in the high tissue distribution characteristics of GPFX. The clearance rates of GPFX in humans were predicted from the pharmacokinetic parameters of rats, rabbits, monkeys and dogs by an animal scale-up method and a pharmacokinetic model for humans was constructed. The GPFX concentration-time profiles in plasma, following oral administration of GPFX to humans, were predicted within 0.5-1.0 h of mean absorption time and the calculation-derived results were in good agreement with the experimental data. Thus, it is suggested that the concentration-time profile in plasma and all human organs can be predicted from the pharmacokinetic data of animals.
- 公益社団法人日本薬学会の論文
- 2000-09-01
著者
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Nakajima Yukiko
共立薬科大学 薬剤
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Nakajima Yukiko
Department Of Pharmacy The University Of Tokyo Hospital Faculty Of Medicine The University Of Tokyo
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Kose Matsunaga
Department Of Practical Pharmacy Kyoritsu College Of Pharmacy
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Nakashima E
Dep. Of Pharmaceutics Kyoritsu Univ. Of Pharmacy
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Nakashima Emi
Faculty Of Pharmaceutical Sciences Kanazawa University
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Nakashima Emi
Department Of Pharmaceutics Kyoritsu University Of Pharmacy
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Nakashima Emi
Department Of Pediatrics:hospital Pharmacy:and Faculty Of Pharmaceutical Sciences University Of Kana
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Iizasa H
Kyoritsu Univ. Pharmacy Tokyo Jpn
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Iizasa Hisashi
Department Of Pharmaceutics Kyoritsu University Of Pharmacy
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HATTORI Kenji
Department of Otolaryngology, Sumitomo Hospital
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SASABE Hiroyuki
Department of Photonics Materials Science, Chitose Institute of Science and Technology (CIST)
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Nakashima Emi
Faculty Of Pharmaceutical Sciences And Hospital Pharmacy Kanazawa University
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Nakajima Yukiko
Department Of Pharmaceutics Kyoritsu College Of Pharmacy
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MIYAMOTO Gohachiro
Department of Drug Metabolism, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.
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Hattori Kenji
Department Of Pharmaceutics Kyoritsu College Of Pharmacy
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Matsunaga Noriko
Department Of Practical Pharmacy Kyoritsu College Of Pharmacy
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SHINSEI Machiko
Department of Pharmaceutics, Kyoritsu College of Pharmacy
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AKIYAMA Hitoshi
Department of Drug Metabolism, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,
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Shinsei Machiko
Department Of Pharmaceutics Kyoritsu College Of Pharmacy
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中島 恵美
Department Of Pharmaceutics Kyoritsu University Of Pharmacy
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Miyamoto Gohachiro
Department Of Drug Metabolism Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.
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Sasabe Hiroyuki
Department Of Drug Metabolism Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.
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Akiyama H
Department Of Drug Metabolism Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.
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Hattori Kenji
Department Of Otolaryngology Sumitomo Hospital
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Akiyama Hitoshi
Department Of Drug Metabolism Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.
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HATTORI Kenji
Department of Material Physics, Faculty of Engineering Science, Osaka University
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