Sakai K, Nishiura A, Fujihara Y, Kutsuna T, Nishino T
J Pharmacobiodyn. 1983 Dec;6(12):991-9. doi: 10.1248/bpb1978.6.991.
The salivary excretion of warfarin was investigated following intravenous and oral administration to rabbits. The salivary decay curves following intravenous injection (50 mg/kg) fitted to the two-compartment open model. On the other hand, following oral administration (100 mg/kg) the disposition of warfarin fitted to the one-compartment open model. There was a good linear relationship between the warfarin concentrations in saliva and plasma. The saliva vs. plasma (S/P) ratio was approximately 0.07. A good correlation was also observed between the warfarin concentrations in saliva and plasma protein-unbound fraction. The saliva vs. plasma protein-unbound fraction (S/Pf) ratio was approximately 0.92. Therefore, salivary concentration of warfarin corresponded with plasma free warfarin concentration. Furthermore, warfarin concentration in saliva was correlated with pharmacological effect, prothrombin complex activity. These results suggested that salivary warfarin concentration which was correlated with pharmacological effect had a possibility of utilization in pharmacokinetic studies and therapeutic drug monitoring.
对家兔静脉注射和口服华法林后，研究了其唾液排泄情况。静脉注射（50mg/kg）后的唾液消除曲线符合二室开放模型。另一方面，口服给药（100mg/kg）后，华法林的处置符合一室开放模型。唾液和血浆中的华法林浓度之间存在良好的线性关系。唾液与血浆（S/P）比值约为0.07。唾液和血浆蛋白未结合部分中的华法林浓度之间也观察到良好的相关性。唾液与血浆蛋白未结合部分（S/Pf）比值约为0.92。因此，华法林的唾液浓度与血浆游离华法林浓度相对应。此外，唾液中的华法林浓度与药理作用、凝血酶原复合物活性相关。这些结果表明，与药理作用相关的唾液华法林浓度有可能用于药代动力学研究和治疗药物监测。
