Trenk D, Winkelmann B, Jähnchen E, Oie S
Division of Clinical Pharmacology, Reha-Zentrum, Bad Krozingen, West Germany.
J Pharmacokinet Biopharm. 1988 Feb;16(1):1-12. doi: 10.1007/BF01061859.
The dose-dependency of phenprocoumon disposition was determined in rats by iv administration of 0.1 and 1.0 mg/kg doses to separate groups of animals. The intrinsic clearance (unbound clearance) was 33% lower in the animals given 1.0 mg/kg dose than in the animals given 0.1 mg/kg dose. The apparent unbound volume of distribution was 55% lower and the elimination rate constant 54% higher in the high dose group than in the lower dose group. Binding of phenprocoumon to liver showed saturability with a two- to threefold higher apparent unbound fraction of phenprocoumon in liver in animals given the high dose in comparison to animals given the low dose.
通过向不同组大鼠静脉注射0.1和1.0mg/kg剂量的苯丙香豆素，测定了苯丙香豆素处置的剂量依赖性。给予1.0mg/kg剂量的动物的内在清除率（非结合清除率）比给予0.1mg/kg剂量的动物低33%。高剂量组的表观非结合分布容积比低剂量组低55%，消除速率常数高54%。与低剂量组动物相比，高剂量组动物肝脏中苯丙香豆素的结合具有饱和性，其在肝脏中的表观非结合分数高两到三倍。
