唾液和血浆中10-羟基卡马西平的药动学及其浓度的相关性研究

目的:考察唾液与血浆中10-羟基卡马西平的药动学及其浓度的相关性。方法:20名志愿者禁食1晚后,服用奥卡西平600mg,在96h内同步收集血液和静息唾液样本,用已建立的高效液相色谱方法对10-羟基卡马西平进行分析。结果:唾液和血浆中10-羟基卡马西平的AUC_(0～∞)分别为(162±s 86)和(186±27)mg·h·L~(-1)。c_(m(?))分别为(8．1±1．4)和(7．2±1．3)mg·L~(-1),t_(max)分别为(4．7±2．7)和(5．4±1．5)h,t_(1/2)为(11．1±2．5)和(10．2±1．7)h,MRT_(0～(

Pharmacokinetics and correlation of concentration of 10-hydroxycarbazepine in saliva and plasma

AIM:To study the pharmacokinetics and the correlation of concentration of 10-hydroxycar- bazepine in saliva and serum.METHODS:Twenty volunteers took oxcarbazepine 600 mg after an overnight fast.Blood and unstimulated saliva were collected for 96 h to assay the 10-hydroxycarbazepine with established high performance liquid chromatography.RESULTS:The parameters of 10-hydroxycarbazepine in saliva and plasma were as below:AUC_(0_∞)was(162±s 86)and(186±27)mg·h·L~(-1),c_(max)was(8.1±1.4)and(7.2±1.3)mg·L~(-1),t_(max)was(4.7±2.7)and(5.4±1.5)h,t_(1/2)was(11.1±2.5)and(10.2±1.7)h,MRT_(0-1),was (18±4)and(20.1±2.2)h,respectively.A significant correlation was found between saliva concentrations (C_s)and plasma concentrations(C_P)of 104 paired samples(r=0.92,P＜0.01).The total variation of 104 paired C_S/C_p was 51.5 %,intraindividual variation was 29.0 % and interindividual variation was 21.6 %.There were also significant difference of C_S/C_p at different time point.CONCLUSION:Unstimulated saliva is not a good alternative to plasma for therapeutic drug monitoring of 10-hydroxycarbazepine.