摘要
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 A in healthy volunteers. METHODS Twenty volunteers took the huperzine A tablets by oral with 2-way crossover design. The concentration of hu perzine A in plasma was determined by HPLC/MS/MS. The pharmacokinetics parameters were calculated by BAPP software. RESULTS The calibration curve was linear in the range from 0. 10μg·L^-1 to 6. 38 μg·L^-1. The extract recovery was more than 73.1%. The intra and inter RSD was less than 10. 2 %. The main pharmacokinetics parameters T1/2, Cmax, Tmax and AUC0-48 Of the test tablets were （13.6±1.3） h, （1.9± 0. 5） μg·L^-1 , （0. 6±0. 3） h and （19. 9 ± 2. 7） μg·L^-1·h, respectively. The pharmaeokinetics parameters T1/2, Cmax, Tmax and AUC-048 of the reference tablets were （ 13. 6±1.1 ） h, （2. 0±0. 4） μg·L^-1, （0. 60± 0. 20） h and （20. 6 ± 2. 2） μg·L^-1·h, respectively. The relative bioavalability of the test tablets was （96. 8 ± 10. 1） %. CONCLUSION The HPLC/MS/MS method for determination of huperzine A in plasma is proved to be sensitive, accurate and convenient. The reference and test tablets are bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2009年第9期699-702,共4页
Chinese Journal of Hospital Pharmacy
基金
国家科技支撑计划课题(编号:2006BAI14B07)
