苯磺酸氨氯地平片在健康人体的生物等效性

Bioequivalence of amlodipine besylate tablets in Chinese healthy volunteers

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。

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^-1 respectively;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.