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  

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

作　　者：迟丹怡[1] 焦正[1] 李中东[1] 施孝金[1] 钟明康[1] 

机构地区：[1]复旦大学附属华山医院临床药学研究室,上海200040

出　　处：《中国新药与临床杂志》2007年第4期252-255,共4页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：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～(<?))分别为(18±4)和(20．1±2．2)h。104对样本的唾液浓度(C_S)和血浆浓度(C_P)具有显著相关性(r=0．92,P＜0．01),总变异为51．5％,个体内变异为29．0％,个体间变异为21．6％。在不同时间点C_S/C_P的差异也非常显著。结论:静息唾液样本不适合替代血浆样本进行10-羟基卡马西平的治疗药物监测。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： AUC0-∞ was （162 ± s 86） and （186 ± 27） mg·h·L^-1, cmax was （8.1±1.4） and （7.2 ± 1.3） mg·L^-1, tmax was （4.7 ± 2.7） and （5.4 ± 1.5） h, t1/2was （11.1 ± 2.5） and （10.2 ±1.7） h, MRT0-1 was （18 ± 4） and （20.1 ± 2.2） h, respectively. A significant correlation was found between saliva concentrations （Cs） and plasma concentrations （ce） of 104 paired samples （r = 0.92, P 〈 0.01）. The total variation of 104 paired Cs/Cp was 51.5 %, intraindividual variation was 29.0 % and interindividual were also significant difference of Cs/Cp at different time point. CONCLUSION： good alternative to plasma for therapeutic drug monitoring of 10-hydroxycarbazepine. variation was Unstimulated 21.6 %. There saliva is not a

关 键 词：奥卡西平 卡马西平 唾液 血浆 药动学 药物监测 色谱法 高压液相 相关性 10-羟基卡马西平 

分 类 号：R969.1[医药卫生—药理学] R971.6[医药卫生—药学]