间苯三酚栓剂在家兔体内的药动学研究

发布时间：2018-12-26 14:48

【摘要】：建立液相色谱-质谱联用(LC-MS)测定间苯三酚血药浓度的方法,并研究间苯三酚栓剂在家兔体内的药动学特征。取6只健康家兔直肠给予间苯三酚栓剂,于给药前和给药后5,10,15,18,20,25,30,45,60,90,120,180 min分别自耳动脉采血0.5 mL。采用LC-MS检测其血药浓度,安捷伦C18柱(4.6 mm×50 mm,1.7μm),流动相甲醇-水(含0.1%甲酸)梯度洗脱,三重串联四级杆质谱电喷雾(ESI)离子源,多反应监测(MRM)方式进行检测,离子化方式为正模式,进样量为2μL。采用DAS3.0药动学软件计算其在家兔体内的药动力学参数。间苯三酚在0.1725~5.52mg/L质量浓度范围内与其峰面积与内标峰面积的比值呈良好的线性关系。间苯三酚在家兔体内的药动学参数t_(1/2),T_(max),C_(max),AUC_(0-∞)分别为65.733 min,15 min,1.277 3 mg/L,39.993(mg·min)/L。该方法专属性强、精密度好,可用于间苯三酚家兔体内的药动学研究。间苯三酚栓剂在家兔体内代谢过程符合一室模型。
[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，

本文编号：2392274