Shankaran S, Pantoja A, Poland R L
Dev Pharmacol Ther. 1982;4(3-4):124-31. doi: 10.1159/000457401.
We studied the effects of indomethacin on the bilirubin binding of albumin using the hydroxybenzene azobenzoic acid (HBABA) dye binding method, the estimation of unbound bilirubin concentration (UBC) by the horseradish peroxidase assay and the whole blood fractionation (WBF) technique. The addition of up to 2 micrograms/ml of indomethacin, which is the level obtained with an 0.2 mg/kg dose, did not decrease the mean HBABA dye binding capacity of 29 icteric sera or increase the mean UBC of 11 icteric sera. There was also no additional displacement of bilirubin in 5 icteric sera measured by the WBF technique. However, the addition of 10-40 micrograms/ml of drug, which is the level that would be achieved if a 2 mg/kg dose of indomethacin were administered, resulted in a significant reduction of HBABA in 15 icteric sera (81.74-57.3%, p less than 0.005) and a significant increase of UBC in 11 icteric sera (6.17-37.2 nM/l, p less than 0.001). Therefore, no displacement of bilirubin from albumin occurred in the presence of usual therapeutic level of indomethacin; higher levels displaced bilirubin.
我们使用羟基苯偶氮苯甲酸（HBABA）染料结合法、辣根过氧化物酶法估算未结合胆红素浓度（UBC）以及全血分离（WBF）技术，研究了吲哚美辛对白蛋白结合胆红素的影响。添加高达2微克/毫升的吲哚美辛（这是0.2毫克/千克剂量时的血药浓度水平），并未降低29份黄疸血清的平均HBABA染料结合能力，也未升高11份黄疸血清的平均UBC。通过WBF技术检测，5份黄疸血清中的胆红素也未出现额外的置换。然而，添加10 - 40微克/毫升的药物（这是若给予2毫克/千克剂量的吲哚美辛时可达到的血药浓度水平），导致15份黄疸血清中的HBABA显著降低（从81.74%降至57.3%，p < 0.005），11份黄疸血清中的UBC显著升高（从6.17纳摩尔/升升至37.2纳摩尔/升，p < 0.001）。因此，在通常治疗水平的吲哚美辛存在时，胆红素未从白蛋白上被置换；更高水平则会置换胆红素。
