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兔静脉注射后茶碱和二羟丙茶碱的比较药代动力学

Comparative pharmacokinetics of theophylline and dyphylline following intravenous injection in rabbits.

作者信息

Ng P K, Locock R A

出版信息

Res Commun Chem Pathol Pharmacol. 1979 Dec;26(3):509-24.

PMID:523786
Abstract

The pharmacokinetics of theophylline and dyphylline in four rabbits were investigated following intravenous injection. Each rabbit received theophylline (10 mg/kg) first then dyphylline (25 mg/kg) two weeks afterwards as an intravenous bolus injection. The serum concentration-time data for both theophylline and dyphylline were best fitted to the two compartment open model. The half-lives of theophylline and dyphylline were 5.5 +/- 1.3 and 0.74 +/- 0.10 hr, respectively. The apparent volume of distribution (Vdbeta) and total body clearance (TBC) of dyphylline (Vdbeta = 1008 +/- 156 ml/kg; TBC = 942 +/- 118 ML/HR/KG)a = 1008 +/- 156 ml/kg; TBC = 942 +/- 118 ml/hr/kg) were much higher than those of theophylline (Vdbeta = 545 +/- 160 ml/kg; TBC = 69 +/- 10 ml/hr/kg). Thus both theophylline and dyphylline showed pronounced difference in their pharmacokinetic profile.

摘要

静脉注射后,对4只兔子体内茶碱和二羟丙茶碱的药代动力学进行了研究。每只兔子先接受茶碱(10mg/kg)静脉推注,两周后再接受二羟丙茶碱(25mg/kg)静脉推注。茶碱和二羟丙茶碱的血清浓度-时间数据均最符合二室开放模型。茶碱和二羟丙茶碱的半衰期分别为5.5±1.3小时和0.74±0.10小时。二羟丙茶碱的表观分布容积(Vdbeta)和总体清除率(TBC)(Vdbeta = 1008±156ml/kg;TBC = 942±118ml/小时/千克)远高于茶碱(Vdbeta = 545±160ml/kg;TBC = 69±10ml/小时/千克)。因此,茶碱和二羟丙茶碱在药代动力学特征上表现出明显差异。

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