| 摘要: |
| 目的：建立LC-MS法测定人体血浆中苯磺酸氨氯地平的药物浓度,并进行两种制剂的生物等效性评价。方法：20例健康受试者单剂量交叉口服10 mg苯磺酸氨氯地平供试制剂或参比制剂后,采用LC-MS测定人体血浆中不同时间点苯磺酸氨氯地平的浓度,计算其药代动力学参数和相对生物利用度,评价两制剂的生物等效性。结果：苯磺酸氨氯地平供试制剂和参比制剂主要药代动力学参数如下：Cmax分别为（6.21±1.88）（、6.03±1.08）ng/ml,AUC0-120分别为（250.68±52.61）、（246.14±52.11）ng·h/ml,Tmax分别为（6.0±2.3）、（6.1±2.5）h,t1/2分别为（40.45±6.68）、（43.74±9.05）h。本方法在0.1-20.0 ng/ml浓度范围内线性关系良好。最低可定量浓度为0.1 ng/ml,两制剂主要药动学参数经统计学检验无显著性差异。结论：本方法简单、快速、准确,两种制剂具有生物等效性。[ |
| 关键词: 氨氯地平 苯磺酸盐类 色谱法,高压液相 光谱分析,质量 药代动力学 生物 |
| DOI：10.3724/SP.J.1008.2007.00299 |
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| 基金项目: |
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| Liquid chromatography-mass spectrometry in evaluation of bioequivalence of two kinds of amlodipine besylate tablets |
| LIANG Chao , CHENG Xiao-hua , ZHANG Hong , XU Wen-wei , HU Xiao |
| (1. Department of General Surgery, The People＇s Hospital of Jiangxi Province, Nanchang 330006, China; 2. Institute of Clinical Pharmacology, Medical School, Nanchang University, Nanchang 330006) |
| Abstract: |
| Objective： To establish a liquid chromatography-mass spectrometry （LC-MS） method for determining the concentration of amlodipine besylate in human plasma and to evaluate the bioequivalence of 2 kinds of amlodipine besylate tablets. Methods： Twenty healthy male volunteers were enrolled into a single crossover study. A single dose of the suspension equivalent to 10 mg amlodipine besylate or a reference preparation was given in a crossover way. The plasma concentrations of amlodipine besylate were determined by LC-MS method in the volunteers at different time points; the pharmacokinetic parameters and relative bioavailability were calculated and the bioequivalence of the 2 preparations were evaluated. Results： The pharrnacokinetic parameters for experimental and the reference preparations were： Cmax （6. 21 ± 1. 88） vs（ 6. 03 ± 1. 08） ng/ml; AUC0-120（250. 68±52. 61） vs （246.14±52.11） ng h/ml; Tmax（6.0±2.3） vs （6. 1± 2.5） h; t1/2（40.45±6.68） vs （43.74±9.05） h, respectively. The linear range of the present method was 0. 1-20. 0 ng/ml; the lowest detectable concentration of amlodipine besylate was 0.1 ng/ml. There was no significant difference in pharmacokinetic parameters between the 2 tablets. Conclusion： The present method is simple to use, fast, and accurate. The 2 preparations of amlodipine besylate are bioequivalent.[ |
| Key words: amlodipine benzenesulfonates chromatography, high pressure liquid spectrum analysis, mass pharmacokinetics biological availability |
