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間苯三酚栓劑在家兔體內(nèi)的藥動(dòng)學(xué)研究

發(fā)布時(shí)間:2018-12-26 14:48
【摘要】:建立液相色譜-質(zhì)譜聯(lián)用(LC-MS)測定間苯三酚血藥濃度的方法,并研究間苯三酚栓劑在家兔體內(nèi)的藥動(dòng)學(xué)特征。取6只健康家兔直腸給予間苯三酚栓劑,于給藥前和給藥后5,10,15,18,20,25,30,45,60,90,120,180 min分別自耳動(dòng)脈采血0.5 mL。采用LC-MS檢測其血藥濃度,安捷倫C18柱(4.6 mm×50 mm,1.7μm),流動(dòng)相甲醇-水(含0.1%甲酸)梯度洗脫,三重串聯(lián)四級桿質(zhì)譜電噴霧(ESI)離子源,多反應(yīng)監(jiān)測(MRM)方式進(jìn)行檢測,離子化方式為正模式,進(jìn)樣量為2μL。采用DAS3.0藥動(dòng)學(xué)軟件計(jì)算其在家兔體內(nèi)的藥動(dòng)力學(xué)參數(shù)。間苯三酚在0.1725~5.52mg/L質(zhì)量濃度范圍內(nèi)與其峰面積與內(nèi)標(biāo)峰面積的比值呈良好的線性關(guān)系。間苯三酚在家兔體內(nèi)的藥動(dòng)學(xué)參數(shù)t_(1/2),T_(max),C_(max),AUC_(0-∞)分別為65.733 min,15 min,1.277 3 mg/L,39.993(mg·min)/L。該方法專屬性強(qiáng)、精密度好,可用于間苯三酚家兔體內(nèi)的藥動(dòng)學(xué)研究。間苯三酚栓劑在家兔體內(nèi)代謝過程符合一室模型。
[Abstract]:A liquid chromatography-mass spectrometry (LC-MS) method was developed for the determination of phloroglucinol in blood and the pharmacokinetic characteristics of phloroglucinol suppository in rabbits were studied. Rectum of 6 healthy rabbits was treated with isoglucinol suppository. Blood was taken from ear artery for 0.5 mL. before and after administration. LC-MS was used to detect its blood concentration, the mobile phase methanol-water (containing 0.1% formic acid) was eluted on Agilent C18 column (4.6 mm 脳 50 mm,1.7 渭 m), and the (ESI) ion source was electrospray by quadruple tandem mass spectrometry. The method of multi-reaction monitoring (MRM) was used to detect, the ionization mode was positive mode, and the sample quantity was 2 渭 L. The pharmacokinetic parameters in rabbits were calculated by DAS3.0 pharmacokinetic software. The ratio of peak area to internal standard peak area of phloroglucinol in the range of 0.1725~5.52mg/L concentration showed a good linear relationship. The pharmacokinetic parameters t _ (1 / 2) and T _ (max), C _ (max), AUC_ (0- 鈭,

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