Ochs H R, Greenblatt D J, Arendt R M, Schäfer-Korting M, Mutschler E
Arzneimittelforschung. 1985;35(10):1580-2.
Nine healthy volunteers received single oral doses of the following four beta-adrenergic blocking agents: propranolol (160 mg), metoprolol (100 mg), atenolol (200 mg), and sotalol (320 mg). The kinetics of each drug were determined from multiple serum concentrations measured during 24-48 h after each dose, and in vitro lipid solubility determined using the liquid chromatographic (HPLC) retention index. Oral clearance for the four drugs ranged from 40.2 ml/min/kg for propranolol down to 2.1 for sotalol. Oral clearance was highly correlated (r = 0.99) with in vitro lipid solubility, with propranolol being the most lipophilic drug and sotalol the least. Thus lipophilicity is a physicochemical property of beta-adrenergic blockers that appears to influence their intrinsic clearance after oral dosage.
九名健康志愿者分别单次口服以下四种β-肾上腺素能阻滞剂：普萘洛尔（160毫克）、美托洛尔（100毫克）、阿替洛尔（200毫克）和索他洛尔（320毫克）。每种药物的动力学通过在每次给药后24至48小时内多次测量血清浓度来确定，体外脂溶性则使用液相色谱（HPLC）保留指数来测定。四种药物的口服清除率范围从普萘洛尔的40.2毫升/分钟/千克到索他洛尔的2.1毫升/分钟/千克。口服清除率与体外脂溶性高度相关（r = 0.99），普萘洛尔是最具亲脂性的药物，而索他洛尔亲脂性最低。因此，亲脂性是β-肾上腺素能阻滞剂的一种物理化学性质，似乎会影响其口服给药后的内在清除率。
