Bendayan R, Pieper J A, Stewart R B, Caranasos G J
Eur J Clin Pharmacol. 1984;26(2):251-4. doi: 10.1007/BF00630294.
The extent of propranolol protein binding was determined in three different age groups of healthy drug-free caucasian males. Volunteers selected for study were 6-15 years old, 25-36 years old and 68-76 years old. Ten milliliters of blood were obtained via venipuncture and collected in glass tubes from the subjects after an overnight fast. Binding determinations were performed by equilibrium dialysis using radiolabelled propranolol. Serum albumin and alpha 1-acid glycoprotein concentrations were determined in all subjects by radial immunodiffusion. The results obtained showed wide intersubject variability in the binding ratio of propranolol and serum concentrations of alpha 1-acid glycoprotein. Mean albumin serum concentration was found to be significantly lower in the elderly group as compared to the adult and pediatric groups (p less than 0.02). A positive correlation was found between the binding ratio of propranolol and the serum concentration of alpha 1-acid glycoprotein in all the subjects (r = + 0.66, p less than 0.005). No significant correlation was found between the binding ratio of propranolol and the serum concentration of albumin (r = -0.03, p less than 0.88). These data suggest that the extent of propranolol binding is influenced primarily by serum concentrations of alpha 1-acid glycoprotein and not by differences in age.
在三组不同年龄的无用药史的健康白人男性中测定了普萘洛尔的蛋白结合程度。入选研究的志愿者年龄分别为6 - 15岁、25 - 36岁和68 - 76岁。经过一夜禁食后,通过静脉穿刺从受试者采集10毫升血液,并收集于玻璃管中。使用放射性标记的普萘洛尔通过平衡透析进行结合测定。通过放射免疫扩散法测定所有受试者的血清白蛋白和α1 - 酸性糖蛋白浓度。所得结果显示,普萘洛尔的结合率和α1 - 酸性糖蛋白的血清浓度在受试者之间存在很大差异。与成人组和儿童组相比,老年组的血清白蛋白平均浓度显著更低(p < 0.02)。在所有受试者中,普萘洛尔的结合率与α1 - 酸性糖蛋白的血清浓度之间存在正相关(r = + 0.66,p < 0.005)。普萘洛尔的结合率与血清白蛋白浓度之间未发现显著相关性(r = -0.03,p < 0.88)。这些数据表明,普萘洛尔的结合程度主要受α1 - 酸性糖蛋白血清浓度的影响,而非年龄差异的影响。