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目的:研究健康人口服石杉碱甲片后的药动学及生物等效性。方法:20名健康受试者采用随机分组自身交叉对照试验设计,口服石杉碱甲片200μg后用液相色谱质谱联用技术(LC/MS/MS)测定血浆中石杉碱甲浓度,以BAPP程序计算其药动学参数和评价生物等效性。结果:在选定的色谱/质谱条件下石杉碱甲与内标及血浆杂质分离无干扰,在0.10～6.38μg·L-1范围内线性良好。石杉碱甲的提取回收率>73.1%,日内和日间RSD<10.2%。石杉碱甲片受试制剂(T)和参比制剂(R)的主要药动学参数:tmax分别为(0.6±0.3)h(T)和(0.60±0.20)h(R),Cmax分别为(1.9±0.5)μg·L-1(T)和(2.0±0.4)μg·L-1(R);t1/2分别为(13.6±1.3)h(T)和(13.6±1.1)h(R);AUC0-48分别为(19.9±2.7)μg·L-1·h(T)和(20.6±2.2)μg·L-1·h(R);石杉碱甲片相对生物利用度为(96.8±10.1)%。结论:用LC/MS/MS法测定血浆中石杉碱甲浓度,杂质无干扰,定量限低,重复性好,准确度高。受试的石杉碱甲片与参比的石杉碱甲片生物等效。
Objective: To study the pharmacokinetics and bioequivalence of huperzine tablets in healthy subjects. Methods: Twenty healthy subjects were randomized to receive crossover randomized controlled crossover study. 200 μg of huperzine A was administered orally and the concentration of huperzine A in plasma was determined by liquid chromatography-mass spectrometry (LC / MS / MS) The program calculates its pharmacokinetic parameters and evaluates the bioequivalence. RESULTS: Huperzine A had no interference with internal standard and plasma impurity separation under the selected chromatographic / mass spectrometry conditions and was linear over the range of 0.10-6.38 μg · L -1. Huperzine A recovery rate of> 73.1%, intraday and daytime RSD <10.2%. The main pharmacokinetic parameters of huperzine A tablets (T) and reference formulation (R) were as follows: tmax were (0.6 ± 0.3) h (T) and (0.60 ± 0.20) h Were (1.9 ± 0.5) μg · L-1 (T) and (2.0 ± 0.4) μg · L-1 (R); t1 / 2 were (13.6 ± 1.3) h (R); AUC0-48 were (19.9 ± 2.7) μg · L-1 · h (T) and (20.6 ± 2.2) μg · L-1 · h (R) respectively; relative bioavailability (96.8 ± 10.1)%. Conclusion: The plasma concentration of huperzine A was determined by LC / MS / MS method with no interference of impurities, low quantitation limit, good reproducibility and high accuracy. The tested huperzine tablets were bioequivalent to the reference huperzine tablets.