Pharmacokinetic Studies of Biliary Excretion. V. The Relationship between the Biliary Excretion Behavior and the Elimination from Plasma of Xanthene Dyes and Bromsulphthalein in Rat

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The relationship between the biliary excretion behavior and the elimination from plasma was studied using five xanthene dyes, i. e. Phloxine B (PB), Rose Bengal (RB), Erythrosine B (EB), Eosine Y (EY) and Fluorescein sodium (FS), and Bromsulphthalein (BSP) in vivo and in vitro in rat. 1) It was of interest that the plasma elimination patterns of xanthene dyes showed two types, the elimination following the one and two compartments models. PB and RB were the former group, and EB, EY and FS were the latter group. 2) The plasma elimination of xanthene dyes except for FS which has no halogen substituent, were relatively rapid (T_<1/2>=3-12min). But the elimination of FS was very slow (T_<1/2>=60 min), and it was suggested that the effect of the halogen substituent was shown in the plasma elimination as well as in the biliary excretion. 3) The binding ratio with rat plasma of xanthene dyes showed similar ratios (55-70%) with each other except for FS. The ratio of FS was very low (15%) in spite of it's slow plasma elimination. 4) The plasma elimination of BSP was very rapid (T_<1/2>=3.3 min) and followed the two compartment model, but the binding ratio with plasma protein was rather high (about 50%) in spite of its rapid plasma elimination and concentrical biliary excretion. 5) It was also found that the bile acid gave some influence on the binding with BSA.
社団法人日本薬学会の論文
1972-02-25