Kitayama R, Hayashi T, Minami S, Watanabe Y, Narita H
Research Laboratories, Toyama Chemical Co., Ltd.
Jpn J Antibiot. 1995 May;48(5):643-8.
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 0.25-20 micrograms/ml. 3. The binding rates of T-3761 lowered as the decrease of protein concentration. 4. The binding rates of T-3761 (2 micrograms/ml) to human serum protein were 12.4, 21.3 and 32.1% at pH 7.0, 7.4 and 8.0, respectively, showing the effect of the pH. 5. The binding of T-3761 to human serum protein was reversible. 6. In vivo binding rates of T-3761 in rabbits after a single oral administration of 20 mg/kg were 26.1-33.2%, which were similar to those obtained in vitro.
我们研究了T - 3761与血清蛋白的结合程度，得到以下结果。1. T - 3761与各种动物及人类血清蛋白的结合率为16.9 - 27.7%，略高于环丙沙星和氧氟沙星。2. 在浓度为0.25 - 20微克/毫升时，T - 3761与人类血清蛋白的结合率为19.1 - 23.8%。3. T - 3761的结合率随蛋白质浓度的降低而降低。4. 在pH值为7.0、7.4和8.0时，T - 3761（2微克/毫升）与人类血清蛋白的结合率分别为12.4%、21.3%和32.1%，显示出pH值的影响。5. T - 3761与人类血清蛋白的结合是可逆的。6. 单次口服20毫克/千克后，家兔体内T - 3761的结合率为26.1 - 33.2%，与体外实验结果相似。
