苯磺酸氨氯地平片在中国健康受试者中的生物等效性研究

目的：在空腹和餐后条件下，评价两种苯磺酸氨氯地平片在中国健康受试者中的生物等效性。方法：入组24例健康受试者，采用随机、开放、两周期自身交叉试验设计，分别在空腹和餐后条件下给予受试制剂或参比制剂，用液质联用法（LC-MS/MS）测定给药后氨氯地平的血浆浓度，计算主要药代动力学参数，评价受试制剂与参比制剂的生物等效性。结果：健康受试者在空腹口服氨氯地平片后，受试制剂和参比制剂Cmax、AUC0-t、AUC0-∞的均值分别为（3 462.08±683.46） pg/mL、（159 891.00±45 951.00）pg·mL-1·h、（194 850.00±63 829.00） pg·mL-1·h和（3 346.09±710.09） pg/mL、（159 065.00±45 214.00） pg·mL-1·h、（190 461.00±66 160.00） pg·mL-1·h；几何均值的比值及其90%置信区间分别为104.82%（100.35%，109.50%）、103.32%（98.13%，108.78%）、103.98%（97.95%，110.38%）。餐后服用盐酸氨氯地平片后，受试制剂和参比制剂Cmax、AUC0-t、AUC0-∞的均值分别为（2 785.00±600.91） pg/mL、（138 289.00±30 684.00） pg·mL-1·h、（158 765.00±39 260.00） pg·mL-1·h和（2 960.00±671.27） pg/mL、（140 990.00±33 326.00） pg·mL-1·h、（163 996.00±43 606.00） pg·mL-1·h；几何均数的比值及其90%置信区间分别为94.89%（88.94%，101.23%）、97.96%（92.85%，103.34%）、97.26%（91.61%，103.25%）。结论：在空腹和餐后状态下受试制剂和参比制剂的吸收速度和程度均一致，两制剂生物等效，同时两制剂在中国健康受试人群中具有相似的安全性和耐受性。

Bioequivalence of amlodipine besylate tablets in Chinese healthy subjects

AIM: To evaluate the bioequivalence of two kinds of amlodipine besylate tablets in Chinese healthy subjects under fasting and fed conditions. METHODS: Twenty-four healthy subjects were enrolled, and a random, open, single-dose, two preparations, two sequences and double-crossover design was used to give the test or reference preparations under fasting and postprandial conditions. The concentration of metformin in plasma was detected by LC-MS/MS, and the main pharmacokinetic parameters were calculated to evaluate the bioequivalence. RESULTS: In fasting state, the mean of Cmax, AUC0-t, and AUC0-∞ of the test and reference preparations was (3 462.08±683.46) pg/mL, (159 891.00±45 951.00) pg·mL-1·h, (194 850.00±63 829.00) pg·mL-1·h, (3 346.09±710.09) pg/mL, (159 065.00±45 214.00) pg·mL-1·h, (190 461.00±66 160.00) pg·mL-1·h, respectively. The ratio of geometric mean and its 90% confidence interval are 104.82% (100.35%, 109.50%), 103.32% (98.13%, 108.78%), 103.98% (97.95%, 110.38%). In fed condition, the mean of Cmax, AUC0-t, and AUC0-∞ of the test and reference preparations was (2 785.00±600.91) pg/mL, (138 289.00±30 684.00) pg·mL-1·h, (158 765.00±39 260.00) pg·mL-1·h, (2 960.00±671.27) pg/mL, (140 990.00±33 326.00) pg·mL-1·h, (163 996.00±43 606.00) pg·mL-1·h, respectively. The ratio of geometric mean and its 90% confidence interval are 94.89% (88.94%, 101.23%), 97.96% (92.85%, 103.34%) and 97.26% (91.61%, 103.25%). CONCLUSION: Two kinds of amlodipine besylate tablets are bioequivalent, and have similar safety and tolerability in Chinese healthy subjects.