Effect of Carrier-Mediated Transport System on Intestinal Fosfomycin Absorption in Situ and in Vivo
スポンサーリンク
概要
- 論文の詳細を見る
Intestinal absorption mechanism of fosfomycin (FOM), a water-soluble and small molecular antibiotic, at the clinical dose level was examined by both in situ single-pass perfusion technique of rat small intestine and oral administration in rat in vivo. Analyzing the luminal concentrationdependence of FOM absorption rates in situ by the equation composed of two terms of carrier transport of Michaelis-Menten type and simple-diffusion, apparent Michaelis constant (K_1), maximal transport velocity (J_<max>), and first-order diffusive absorption clearance (K_d) were 1.13 mM, 2.54 nmol/min/cm length, and 0.551μl/min/cm length, respectively. At the low FOM concentration in the lumen (0.1 mM), its absorption was reduced to about 60% of the control by inorganic phosphate ion at 1.0 mM in the same manner as the uptake in brush border membrane vesicles of rat small intestine (BBMVs) in vitro. Both the glycol form of FOM at 10 mM, the hydrolyzed metabolite of FOM in the stomach juice, and FOM itself at 10 mM reduced FOM absorption by about 50%, indicating the metabolite to be transported by the same carriers as those of FOM. At the higher FOM concentration (5 mM), its absorption was not reduced by any inhibitor described above. No inhibitory effect of 50 mM phosphate ion on FOM absorption following the oral dosing of 20 mg/kg FOM was found. It was concluded that FOM absorption at the clinical dose (10-20 mg/kg) is barely inhibited by the carrier-mediated system via phosphate transport system observed in the in vitro BBMVs.
- 公益社団法人日本薬学会の論文
著者
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HAYASHI Masahiro
Department of Dermatology, Yamagata University School of Medicine
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AWAZU Shoji
Department of Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Science
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AWAZU Shoji
東京薬科大学薬学部 薬物動態制御学教室
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Awazu S
Tokyo Coll. Pharmacy Tokyo Jpn
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Awazu Shoji
Department Of Biopharmaceutics Tokyo College Of Pharmacy:department Of Pharmaceutics Research Center
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Awazu Shoji
Department Of Biopharmaceutics Tokyo College Of Pharmacy
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Awazu Shoji
Deparment Of Biopharmaceutics Tokyo College Of Pharmacy
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ISHIZAWA Takayuki
Pharmaceutical Research Laboratories, Meiji Seika Kaisha, Ltd.
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Hayashi Masahiro
Department Of Biological Production And Enviromental Science Faculty Of Agriculture The University O
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Ishizawa Takayuki
Meiji Seika Kaisha Ltd. Pharmaceutical Research Center:department Of Surgery Kawasaki City Ida Hospi
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Awazu S
Department Of Biopharmaceutics School Of Pharmacy Tokyo University Of Pharmacy And Life Science
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Awazu S
Department Of Biopharmaceutics Tokyo College Of Pharmacy
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Hayashi Masahiro
Department of Absorption and Pharmacokinetics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences
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