液质联用法对于人血浆中左乙拉西坦浓度的测定及在缓释片空腹和餐后药动学研究中的应用

发布时间：2018-11-08 11:27

【摘要】：目的建立LC-MS/MS测定人血浆中左乙拉西坦浓度,应用于左乙拉西坦缓释片空腹和餐后药动力学研究。方法采用Waters Symmetry C_(18)(3.9 mm×150 mm,5μm)色谱柱,流动相为乙腈-5 mmol·L~(-1)醋酸铵水溶液(含0.3%甲酸)=10∶90(V/V)。2名受试者交叉空腹或餐后单次口服左乙拉西坦缓释片1 000 mg。通过LC-MS/MS测定左乙拉西坦浓度。结果左乙拉西坦血浆质量浓度在0.100 0~80.00μg·mL~(-1)内线性良好,空腹与餐后的主要药动学参数如下:ρ_(max)分别为20.50和19.09μg·mL~(-1),AUC_(0-48 h)分别为345.4和336.3μg·h·mL~(-1),t_(max)分别为4.5和7.0 h。结论该方法简便、特异性高、灵敏度高,可用于受试者空腹和餐后口服1 000 mg左乙拉西坦缓释片后血浆样品中左乙拉西坦药动学研究。高脂高热量饮食对左乙拉西坦缓释片的药动学特征有影响,左乙拉西坦的达峰时间延长。
[Abstract]:Objective to establish a LC-MS/MS method for the determination of levoethylacetam in human plasma and to study the pharmacokinetics of levoethoxetam sustained-release tablets on fasting and postprandial basis. Methods Waters Symmetry C18 (3.9 mm 脳 150 mm,5 渭 m) column was used. The mobile phase consisted of acetonitrile-5 mmol L ~ (-1) ammonium acetate aqueous solution (containing 0.3% formic acid) = 10:90 (V / V). Two subjects took levoethiracetam sustained-release tablets for a single time on an empty stomach or after a meal. The concentration of levoethylacetam was determined by LC-MS/MS. Results the plasma concentration of levoethiracetam was linear at 0.100 渭 g mL~ (-1). The main pharmacokinetic parameters were as follows: 蟻 _ (max) were 20.50 渭 g mL~ (-1) and 19.09 渭 g mL~ (-1), respectively. AUC_ (0-48 h) was 345.4 渭 g mL~ (-1) and 336.3 渭 g h mL~ (-1), and t _ (max) was 4.5,7.0 h. Conclusion the method is simple, specific and sensitive. It can be used to study the pharmacokinetics of levoethylacetam in plasma samples after oral administration of 1 000 mg levoethlacetam after fasting and postprandial oral administration. High fat and high calorie diet had an effect on the pharmacokinetic characteristics of levoethiracetam sustained-release tablets, and the peak time of levoethylacetam was prolonged.
【作者单位】：苏州大学医学部药学院;苏州大学附属第二医院临床药理实验室;
【分类号】：R969.1

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