Colangelo P, Chandler M, Blouin R, McNamara P
College of Pharmacy, University of Kentucky, Lexington 40356.
Br J Clin Pharmacol. 1989 Apr;27(4):519-22. doi: 10.1111/j.1365-2125.1989.tb05402.x.
The influence of age on the stereoselective serum protein binding of propranolol was investigated. Serum was obtained from 10 young (mean age 23 +/- 2 years) and ten elderly (mean age 68 +/- 2 years) healthy male volunteers. The free fraction of propranolol (fu) was measured by equilibrium dialysis, using tritium labeled (+/-)- and (-)-propranolol. The fu values were 0.159 +/- 0.049 and 0.148 +/- 0.028 (+/-), 0.135 +/- 0.041 and 0.136 +/- 0.04 (-), 0.174 +/- 0.056 and 0.161 +/- 0.028 (+) in the young and elderly subjects, respectively. Serum alpha 1-acid glycoprotein (AAG) concentrations were 81.4 +/- 33.0 and 81.0 +/- 21.6 mg 100 ml-1 in young and elderly respectively (P greater than 0.05). Variability in AAG concentration accounted for most of the observed intersubject variability in the binding of both propranolol isomers. The stereoselective binding of propranolol does not appear to be affected by age.
研究了年龄对普萘洛尔立体选择性血清蛋白结合的影响。从10名年轻(平均年龄23±2岁)和10名老年(平均年龄68±2岁)健康男性志愿者中获取血清。使用氚标记的(±)-和(-)-普萘洛尔,通过平衡透析法测定普萘洛尔的游离分数(fu)。年轻受试者和老年受试者的fu值分别为:(±)-普萘洛尔为0.159±0.049和0.148±0.028,(-)-普萘洛尔为0.135±0.041和0.136±0.04,(+)-普萘洛尔为0.174±0.056和0.161±0.028。年轻组和老年组血清α1-酸性糖蛋白(AAG)浓度分别为81.4±33.0和81.0±21.6mg/100ml(P>0.05)。AAG浓度的变异性占观察到的两种普萘洛尔异构体结合的受试者间变异性的大部分。普萘洛尔的立体选择性结合似乎不受年龄影响。