【摘要】 目的研究苯磺酸氨氯地平片(抗高血压药)的相对生物利用度,并求证该制剂的生物等效性。方法24名男性健康受试者随机交叉给药,先后口服单剂量试验制剂及参比制剂苯磺酸氨氯地平片剂5 mg,采用LC-MS/MS法测定血药浓度,计算2者的药代动力学参数及相对生物利用度,并评价2制剂的生物等效性。结果口服试验制剂及参比制剂5 mg的主要药代动力学参数如下:t1/2分别为(47.15±17.28)、(43.22±16.63)h;tmax分别为(5.81±2.09)、(6.38±2.33)h;Cmax分别为(4.77±1.28)、(4.37±1.14)ng·mL-1;AUC0-t分别为(176.39±57.95)、(182.55±58.36)ng·mL-1h;AUC0-t分别为(185.65±59.01)、(192.83±62.72)ng·mL-1h;试验制剂对于参比制剂的平均相对生物利用度F值:AUC0-t为(98.1±18.5)%,AUC0-∞为(98.6±20.0)%;tmax经非参数检验无显著性差异,试验制剂的平均生物利用度(AUC0-t、AUC0-∞)均大于98%,2种制剂的Cmax、AUC0-t和AUC0-∞双向单侧t检验和[1-2α]置信区间法的等效性分析均为合格,tmax经非参数秩和检验无显著性差异。结论2种氨氯地平片剂为生物等效制剂。更多还原

【Abstract】 Objective To study the bioequivalence of two kinds of amlodipine besylate tablets in Chinese healthy volunteers.Methods Twenty four male subjects enrolled the study and took 5 mg test drug(domestic) and reference drug(imported) according to the randomized scheme in the first and second period.LC-MS/MS was used to assay the concentration of amlodipine in plasma.DAS statstic ananlysis software was use to evaluate the bioequivalene of two kinds of amlodipine besylate tablets.Results Main pharmacokiretic parameters of 5 mg test drug and reference drug were as follow: t1/2 were(47.15 ±17.28) and(43.22 ±16.63)h respectively;tmax were(5.81 ±2.09) and(6.38 ±2.33)h respectively;Cmax were(4.77 ±1.28) and(4.37 ±1.14)ng·mL-1respectively;AUC0-t were(176.39 ±57.95)and(182.55 ±58.36)ng·mL-1· h;AUC0-∞ were(185.65 ±59.01)and(192.83 ±62.72)ng·mL-1·h respectively.The mean bioavalibility values of AUC0-t and AUC0-∞ were(98.1±18.5)% and(98.6±20.0)%.Conclusion Two kinds of amlodipine besylate tablets were bioequivalent drug products.更多还原