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目的建立人血浆中石杉碱甲浓度的LC-MS/MS测定方法,研究石杉碱甲在健康人体内的药动学行为,评价两种制剂的生物等效性。方法血浆样品经碱化后,乙酸乙酯提取,LC-MS/MS内标法分析。检测对象为石杉碱甲,m/z243/210,内标(磷酸可待因),m/z300/199。24名健康受试者交叉口服供试片和参比片,剂量均为0.4mg。结果石杉碱甲测定的线性范围为0.252～25.2μg·L-1;口服供试制剂和参比制剂后石杉碱甲的AUC0→t分别为:(1384.079±325.094),(1479.165±288.738)μg·h·L-1;ρmax分别为:(3.062±0.821),(3.558±0.973)μg·L-1;tmax分别为:(47.92±12.85),(44.17±20.62)min。结论本法灵敏、准确、简便。供试品的相对生物利用度为:以AUC0→t计算为(94.4±18.7)%;以ρmax计算为(86.3±15.4)%。统计学结果表明,两种制剂生物等效。
Objective To establish a LC-MS/MS method for determination of Huperzine A in human plasma, study the pharmacokinetics of Huperzine A in healthy volunteers, and evaluate the bioequivalence of the two preparations. Methods The plasma samples were alkalized, extracted with ethyl acetate, and analyzed by LC-MS/MS internal standard method. The test subjects were huperzine A, m/z 243/210, internal standard (codeine phosphate), m/z 300/199. 24 healthy subjects crossed the oral test and reference tablets at a dose of 0.4 mg. . Results The linear range of Huperzine A was 0.252-25.2 μg·L-1. The AUC0→t of Huperzine A after oral preparations and reference preparations was (1384.079±325.094), (1479.165±288.738). The μg·h·L-1; ρmax were (3.062±0.821), (3.558±0.973) μg·L-1, and the tmax were (47.92±12.85), (44.17±20.62) min. Conclusion This method is sensitive, accurate, and simple. The relative bioavailability of the test sample was: (94.4±18.7)% calculated as AUC0→t and (86.3±15.4)% calculated as ρmax. Statistical results show that the two formulations are bioequivalent.