Klitgaard N A, Kristensen O
Eur J Clin Pharmacol. 1986;31(1):91-4. doi: 10.1007/BF00870993.
The utility of saliva sampling in monitoring oxcarbazepine therapy has been assessed in 17 epileptic outpatients treated with a mean dose 22.7 mg/kg/d for 19-411 days, i.e. at steady-state. Blood was collected before the morning dose measurement of the plasma 10-OH-carbazepine concentration and determination of the protein bound fraction. Immediately after blood sampling resting saliva and saliva produced after a masticatory stimulus were collected. Using equilibrium dialysis and an ultrafiltration technique the protein binding of 10-OH-carbazepine was found to be 40% and 45%, respectively. When the degree of protein binding was expressed as the ratio between the corresponding saliva and plasma concentrations of 10-OH-carbazepine, the concentration in resting saliva indicated that no drug was bound to plasma protein, whereas the use of stimulated saliva suggested a protein-bound fraction of 35%. The concentration in stimulated saliva reflects the free fraction of 10-OH-carbazepine, but regression analysis of paired salivary and plasma values showed that the prediction of plasma concentrations from levels in saliva is uncertain. This, together with the low degree of plasma protein binding, leads to the conclusion that it would be preferable to monitor total plasma concentrations if therapeutic drug monitoring of oxcarbazepine were to prove essential in epileptic patients.
在17名癫痫门诊患者中评估了唾液采样在监测奥卡西平治疗中的作用，这些患者平均剂量为22.7mg/kg/d，治疗19 - 411天，即处于稳态。在早晨剂量前采集血液，用于测量血浆10 - 羟基卡马西平浓度并测定蛋白结合分数。采血后立即采集静息唾液和咀嚼刺激后产生的唾液。使用平衡透析和超滤技术，发现10 - 羟基卡马西平的蛋白结合率分别为40%和45%。当蛋白结合程度表示为相应的10 - 羟基卡马西平唾液和血浆浓度之比时，静息唾液中的浓度表明没有药物与血浆蛋白结合，而使用刺激唾液表明蛋白结合分数为35%。刺激唾液中的浓度反映了10 - 羟基卡马西平的游离分数，但对配对唾液和血浆值的回归分析表明，根据唾液水平预测血浆浓度是不确定的。这与血浆蛋白结合程度较低一起得出结论，如果事实证明对癫痫患者进行奥卡西平治疗药物监测至关重要，那么监测血浆总浓度会更可取。
