RP-HPLC法测定人血浆中奥卡西平浓度及其药动学研究

目的:建立以反相高效液相色谱法测定人血浆中奥卡西平浓度的方法,并研究其药动学。方法:血样经二氯甲烷提取并速浓采缩用后流进样量分时析间,程色序谱,柱紫为外检Hy测pe波rsi长lC为18,2流57动n相m,为柱甲温醇为-205.1℃m,o固l·L定-进1醋样酸量铵为溶5液0(μ用L,H内3P标O为4调地p西H值泮至。约另4以.8)3p-9三7软乙件胺(计60算∶480名∶0受.1)试,流者清晨空腹单剂量口服奥卡西平胶囊300mg后的平均药动学参数。结果:奥卡西平血药浓度在0.0351～2.245μg·mL-1范围内线性关系良好(r=0.9994),最低定量浓度0.0351μg·mL-1;方法回收率为93.48%～107.29%;日内RSD为1.17%～7.54%,日间RSD为5.88%～10.32%。t1/2Ke为(16.93±5.80)h,tma(x5.88±3.00)h,Cma(x0.56±0.38)μg·mL-1,AUC0～48为(12.11±5.76)ng·h·mL-1。结论:本方法灵敏、准确,可用于奥卡西平的临床血药浓度测定及药动学研究。

Content Determination of Oxcarbazepine in Human Plasma by RP-HPLC and Its Pharmacokinetics Study

OBJECTIVE：To develop an RP-HPLC method for the content determination of oxcarbazepine in human plasma and to study its pharmacokinetics.METHODS：Blood sample was extracted and condensed using dichloromethane.The determination was performed on Hypersil C18 column with mobile phase consisted of methanol-0.1 mol·L-1 ammonium acetate solution（pH awdajsu ssteetd atto 245.78 nbmy Han3PdO c4）ol-uTmEnA（te6m0p ：e 4ra0t u：r0e.1w）.a sF l2o5w ℃ ra.t eI nwjeacst iosent vaoclcuomrdei nwg atso 5f0lo μwL t iamned pdrioazgerapmams.wThase uUsVed daest eicnttieornn awl asvtaenlednagrtdh.Pharmacokinetic parameters of oxcarbazepine in 8 healthy volunteer after a single oral dose of Oxcarbazepine capsules 300 mg were calculated using 3p97 software.RESULTS：The plasma concentration of oxcarbazepine had good linearity during 0.035 1～2.245 μg·mL-（1r=0.999 4）.The lowest detection limit was 0.035 1 μg·mL-1.The recovery ranged from 93.48% to 107.29%.The RSD of intra-day and inter-day were 1.17%～7.54% and 5.88%～10.32%,respectively.Main pharmacokinetic parameters were as follows：t1/2K（e16.93±5.80）h,tma（x5.88±3.00）h,Cma（x0.56±0.38）μg·mL-1,AUC0～4（812.11±5.76）ng·h·mL-1.CONCLUSION：The method is sensitive,accurate and suitable for plasma concentration determination and pharmacokinetic study of oxcarbazepine.