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  

Bioequivalence of amlodipine besylate tablets in Chinese healthy subjects

作　　者：高茸 马亚中 赵海霞 王肇源 张伟红 袁海龙 GAO Rong;MA Yazhong;ZHAO Haixia;WANG Zhaoyuan;ZHANG Weihong;YUAN Hailong(Department of Pharmacy,Air Force Medical Center,PLA,Beijing 100142,China)

机构地区：[1]中国人民解放军空军特色医学中心药学部,北京100142

出　　处：《中国临床药理学与治疗学》2022年第1期56-62,共7页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金(81903680)。

摘　　要：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C_(max)、AUC_(0-t)、AUC_(0-∞)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C_(max)、AUC_(0-t)、AUC_(0-∞)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。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 C_(max), AUC_(0-t), and AUC_(0-∞)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 C_(max), AUC_(0-t), and AUC_(0-∞)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.

关 键 词：氨氯地平 健康志愿者 液质联用 生物等效 

分 类 号：R969[医药卫生—药理学]