Honoré B, Brodersen R, Robertson A
Dev Pharmacol Ther. 1983;6(5):347-55. doi: 10.1159/000457335.
The binding of indomethacin to albumin was investigated at 37 degrees C, pH 7.4. The first stoichiometric binding constant is 2.5 X 10(5) M-1. Indomethacin utilizes both the bilirubin and diazepam binding functions equally. The effect on bilirubin binding to albumin is negligible at therapeutic indomethacin blood levels. Oleic acid does not affect indomethacin binding until the oleate/albumin molar ratio exceeds 2. A method for measuring the reserve albumin equivalent for binding indomethacin is described. Measurement of this reserve binding equivalent in 33 neonatal serum samples shows no significant correlation of the reserve binding to the albumin level. This methodology may be useful in studying the variable response of infants with patent ductus arteriosus to indomethacin.
在37摄氏度、pH值为7.4的条件下研究了吲哚美辛与白蛋白的结合情况。第一个化学计量结合常数为2.5×10⁵ M⁻¹。吲哚美辛对胆红素和地西泮的结合功能利用程度相同。在治疗性吲哚美辛血药浓度下,其对胆红素与白蛋白结合的影响可忽略不计。直到油酸/白蛋白摩尔比超过2时,油酸才会影响吲哚美辛的结合。描述了一种测量结合吲哚美辛的储备白蛋白当量的方法。对33份新生儿血清样本中这种储备结合当量的测量表明,储备结合与白蛋白水平之间无显著相关性。该方法可能有助于研究动脉导管未闭婴儿对吲哚美辛的不同反应。