Pharmacokinetic study of biliary excretion. 3. Comparison of excretion behavior in xanthene dyes, fluorescein and bromsulphthalein.

Abstract

In the previous papers, the authors reported the kinetic studies on the factors affecting the biliary excretion using Azo, Indigoid and Triphenylmethane dyes. The further study was tried using Xanthene dyes, Fluorescein and Bromsulphthalein, and the effect of halogenation was discussed. Four Xanthene dyes, i.e. Eosine Y, Phloxine B, Erythrosine B, Rose Bengal, and Fluorescein and Bromsulphthalein were used. (1) The excretion behaviors were similar to those of Azo and Triphenylmethane dyes which had the dose dependency, but the excretion ratios showed common larger values than 75% except Fluorescein which had no halogen group. (2) It was found that the halogen group had great influence on the biliary excretion as well as the sulfonate group. And it was also suggested that the effect of halogen group depended on the total electro negativity of substituents. And furthermore it was found that the increasing in molecular weight had not so much effect than the increasing of polarity. (3) It was also suggested that the -I gave the delay of excretion in the early period and this was probably due to the larger uptake into liver cells. (4) BSP showed markedly concentrical excretion pattern and large excretion ratio in a short period and it was found that these characteristic behavior was mainly ascribed to both halogen groups and sulfonate groups.