Modification of Ceftibuten Transport by Changes in Lipid Fluidity Caused by Fatty Acid Glycerol Esters

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概要

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• The effects of various fatty acid glycerol esters (FAGE) on the transport of ceftibuten in rat intestinal brushborder membrane vesicles (BBMV) were investigated. The HLB numbers of FAGE used were in the range of 6.5 to 15.7. The ceftibuten uptake by BBMV was examined by a rapid filtration method in the presence or absence of FAGE of a non-solubilizing concentration (0.03%, w/v). Tetraglycerol monostearate, hexaglycerol monostearate, hexaglycerol sesquistearate, hexaglycerol tristearate and decaglycerol tristearate were found significantly to enhance the ceftibuten uptake under an inward H^+-gradient condition, while FAGE with oleate or laurate did not affect it. The extent of ceftibuten uptake with FAGE correlated with the HLB of the esters (r=-0.90,p<0.001).To elucidate the mechanism of its enhancing action, the effects of FAGE on the membrane lipid fluidity were examined using the fluorescence probes diphenylhexatriene (DPH) and trimethylammonium diphenylhexatriene(TMA-DPH) which distribute in the hydrophobic inner and outer regions of the lipid layer, respectively. The increase in ceftibuten uptake induced by FAGE proved to correlate with an increase in fluidity of the outer lipid layer (r=-0.83,p<0.003) but not the inner lipid layer of BBMV. Hence, the enhancing effect of FAGE with the lower HLB on the ceftibuten transport in the presence of the H^+-gradient should, at least in part, be explainded by the interaction with the outer lipid regions of BBMV.

• 公益社団法人日本薬学会の論文
• 1999-01-15

著者

• 村上 正裕

  京都薬科大学 薬剤

• 村上 正裕

  天藤製薬

• Koga Kenjiro

  Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Hokuriku University

• Koga Kenjiro

  Division Of Pharmaceutical Information Research Laboratory For Development Of Medicine Faculty Of Ph

• Murakami Masahiro

  Kyoto Research Laboratory Amato Pharmaceutical Products

• KAWASHIMA Susumu

  Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Hokuriku University

• MURAKAMI Masahiro

  Research and Development Department, Amato Pharmaceutical Products, Ltd.

• 古賀 憲司

  Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Hokuriku University

• Murakami M

  Showa Univ. Tokyo Jpn

• Kawashima S

  Faculty Of Pharmaceutical Science Hokuriku University

• 村上 正裕

  京都薬大 薬剤学

• 村上 正裕

  京都薬科大学

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