中文摘要：

目的：研究非洛地平缓释片在中国健康人体内的药动学特征和生物等效性。方法：采用双周期、随机、交叉试验设计，22名健康男性受试者先后在空腹状态和餐后状态下随机交叉单剂量口服受试制剂和参比制剂10mg，在不同时间点采集血浆样本，周期间的清洗期为14d。采用LC-MS/MS法测定血浆中非洛地平浓度，计算主要药动学参数并评价两种非洛地平制剂的生物等效性。结果：空腹状态下受试制剂与参比制剂的主要药动学参数如下：t1/z分别为（12．96±6．75）h和（14．15±6．19）h，￡。。分别为（3．41±1．32）h和（3．66±1．43）h，Cmax瑚，分别为（3．42±1．38）/2g·L^-1和（3．30±1．09）/2g·L^-1，AUQC1-t。分别为（43．24±14．52）μg·h·L^-1。和（40．84±13．05）μg·h·L^-1，AUCm。。分别为（47．60±20．38）μg·h·L^-1和（46．44±19．30）μg·h·L^-1餐后状态下受试制剂与参比制剂的主要药动学参数如下：t1/2分别为（12．78±4．33）h和（12．11±7．44）h，tmax。分别为（4．50±0．67）h和（4．41±1．22）h，Cmax分别为（7．92±2．88）ptg·L^-1和（7．74±2．81）μg·L^-1，AUGF。分别为（51．12±13．35）μg·h·L^-1和（50．38±15．86）μg·h·L^-1，AUGm分别为（53．71±14．48）μg·h·L^-1和（52．39±16．04）μg·h·L^-1。空腹和餐后状态下，受试制剂与参比制剂经方差分析和双单侧t检验，主要药动学参数无显著性差异。结论：2种制剂在空腹和餐后2种状态下均生物等效；食物对非洛地平缓释片的药动学有明显的影响。

英文摘要：

OBJECTIVE To study the pharmacokinetics and bioequivalence of felodipine sustained-release tablets in healthy Chinese volunteers. METHODS In the two randomized, cross-over, two-periods study, 22 healthy Chinese volunteers were randomly divided into two groups and given with a single oral dosage of 10 mg felodipine test and reference formulation respec tively under fasted or fed conditions. The wash period was 14 days. Blood samples were collected at different time points. The concentrations of felodipine in plasma were determined by LC-MS-MS method. The main pharmacokinetic parameters were cal culated and the bioequivalence of the two formulations was evaluated. IIFNIJLTS The main pharmacokinetic parameters of test and reference formulations were shown as follows：tl/2were （12. 96 ± 6. 75） and （14. 15 ± 6. 19） h, tmax were （3.41 ± 1.32） and （3.66±1.43） h, Cmax were （3.42±1.38） and （3.30±1.09） μg.L^-1, AgCo-t were （43.24±14.52） and （40.84±13.05） μg.h.L^-1 , AUGo-∞ were （47.60± 20. 38） and （46. 44 ± 19. 30） μg.h.L 1 under fasted state; tl/2 were （12. 78 ± 4. 33） and （12. 11± 7. 44） h,tmax were （4. 50 ± 0. 67） and （4.41 ±1.22） h, Crax were （7. 92 ±2. 88） and （7. 74 ± 2. 81）μg.L^-1 , AUGht were （ 51.12 ± 13.35） and （50. 38 ± 15.9）μg. h,. L ^-1, AUGo-∞ were （53.71 ± 14. 48） and （52. 39 ± 16. 04 ）μg . h. L^-1 under fed state. Test and reference formulations showed no obvious difference. CONCLUSION The two kinds of felodipine formulations are bioequivalent both under fasted and fed conditions. Food could significantly affect pharmacokinetics of felodipine sustained-re- lease tablets.