本文選題：枸地氯雷他定 + 色譜法��； 參考：《中國(guó)新藥與臨床雜志》2015年11期

【摘要】：目的建立測(cè)定大鼠血漿和尿液中枸地氯雷他定的液相色譜-串聯(lián)質(zhì)譜(LC-MS/MS)法,并將其應(yīng)用于枸地氯雷他定在大鼠體內(nèi)的藥動(dòng)學(xué)研究。方法 12只成年健康SD大鼠,隨機(jī)分成兩組,各6只,分別單劑量尾靜脈注射枸地氯雷他定0.5 mg·kg-1和灌胃枸地氯雷他定2 mg·kg-1后,于一定時(shí)間點(diǎn)采集血漿或尿液,取生物樣品50μL經(jīng)液液萃取后,以甲醇-0.1%甲酸水溶液(70∶30,V/V)為流動(dòng)相,選用Diamonsil 5u C18色譜柱(4.6 mm×100 mm,5μm)分離,采用電噴霧離子化進(jìn)行正離子檢測(cè)。用于定量分析的離子反應(yīng)分別為m/z 311→259(枸地氯雷他定)和m/z 327→270(氯氮平)。使用Win Nonlin軟件計(jì)算藥動(dòng)學(xué)參數(shù)。結(jié)果單劑量靜脈注射枸地氯雷他定0.5 mg·kg-1和單劑量灌胃枸地氯雷他定2 mg·kg-1的主要藥動(dòng)學(xué)參數(shù):ρmax分別為(457.00±49.76)和(17.25±4.09)μg·L-1,AUC0-∞分別為(128.80±19.40)和(107.38±10.74)μg·h·L-1,t1/2分別為(3.47±0.27)和(5.33±0.22)h,MRT分別為(4.19±0.62)和(7.22±0.39)h,絕對(duì)生物利用度為20.86%;0~72 h的尿藥累積排泄率分別為(1.19±0.21)%和(0.38±0.11)%。結(jié)論建立的液質(zhì)聯(lián)用測(cè)定枸地氯雷他定在血漿和尿液樣品的方法 ,專屬靈敏快速,適用于大鼠藥動(dòng)學(xué)研究。
[Abstract]:Aim to establish a liquid chromatography-tandem mass spectrometry (LC-MS / MS) method for the determination of loratadine in plasma and urine of rats and to study its pharmacokinetics in rats. Methods Twelve adult healthy SD rats were randomly divided into two groups, 6 rats in each group. The plasma or urine was collected at a certain time after a single dose of clocloatadine 0.5 mg kg-1 and 2 mg kg-1 intragastric administration. After 50 渭 L biological samples were extracted by liquid-liquid extraction, the mobile phase of methanol-0.1% formic acid solution (70: 30 V / V) was used. The column of Diamonsil 5u C18 was used to separate the samples. The positive ions were detected by electrospray ionization. The ion reactions used for quantitative analysis were m / z 311 n 259 and m / z 327 n 270, respectively. The pharmacokinetic parameters were calculated by Win Nonlin software. Results the main pharmacokinetic parameters were: 蟻 max = 457.00 鹵49.76) and 17.25 鹵4.09 渭 g / L AUC0- 鈭，

本文編號(hào)：1941063