Abstract
We investigated the extent of the binding of T-3761 to serum protein and obtained the following results.
1. The binding rates of T-3761 to serum protein from various animals and human were 16.9-27.7%, and a little higher than those of ciprofloxacin and ofloxacin.
2. The binding rates of T-3761 to human serum protein were 19.1-23.8% at concentrations of 0.25-20μg/ml.
3. The binding rates of T-3761 lowered as the decrease of protein concentration.
4. The binding rates of T-3761 (2μg/ml) to human serum protein we re 12.4, 21.3 and 32.1% at pH7.0, 7.4 and 8.0, respectively, showing the effect of the pH.
5. The binding of T-3761 to human serum protein was re versible.
6. In vivo binding rates of T-3761 in rabbits after a sing le oral administration of 20mg/kg were 26.1-33.2%, which were similar to those obtained in vitro.