Le Jeunne C, Poirier J M, Cheymol G, Ertzbischoff O, Engel F, Hugues F C
Service de Médecine Interne, Hôpital Laennec, France.
Eur J Clin Pharmacol. 1991;41(2):171-4. doi: 10.1007/BF00265912.
The pharmacokinetics of a single i.v. dose of dl-bisoprolol 0.16 mg.kg-1 ideal body weight has been studied in 8 obese women (mean weight 91 kg; 161% of ideal body weight) and 8 non-obese women (51 kg; 94% of ideal body weight). Compared to the controls, the obese subjects showed an increase in the total apparent volume of distribution (Vz) (182 vs 1351) and a decrease in Vz per kg body weight (2 vs 2.71.kg-1). There was a negative correlation between Vz l.kg-1 and the percentage of ideal body weight (r = -0.672). Total body clearance was increased, but t1/2 and renal clearance was unchanged. It is concluded that tissue diffusion of bisoprolol in obese subjects is limited, despite its lipophilicity, possibly because of alteration in the blood flow to adipose tissue produced by bisoprolol.
研究了8名肥胖女性（平均体重91kg，为理想体重的161%）和8名非肥胖女性（51kg，为理想体重的94%）静脉注射单剂量0.16mg·kg⁻¹理想体重的消旋比索洛尔后的药代动力学。与对照组相比，肥胖受试者的总体表观分布容积（Vz）增加（182对1351），每千克体重的Vz降低（2对2.71·kg⁻¹）。Vz·kg⁻¹与理想体重百分比之间存在负相关（r = -0.672）。总体清除率增加，但半衰期和肾清除率未改变。结论是，尽管比索洛尔具有亲脂性，但在肥胖受试者中其组织扩散受限，这可能是由于比索洛尔导致脂肪组织血流改变所致。
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