摘要
目的:评价2种复方苯磺酸氨氯地平/盐酸贝那普利制剂生物等效性。方法:20名健康男性志愿者随机交叉单剂量口服复方苯磺酸氨氯地平/盐酸贝那普利受试制剂和参比制剂,采用LC-MS/MS法测定血清中氨氯地平、贝那普利及其代谢产物贝那普利拉浓度,DAS2.0软件计算药动学参数与生物等效性。结果:单剂口服受试和参比制剂后的苯磺酸氨氯地平主要药动学参数Cmax分别为(6.6±1.9)μg.L-1和(7.5±2.3)μg.L-1,tmax分别为(6.2±1.4)h和(5.7±1.2)h,AUC0-t分别为(264.2±90.5)μg.h.L-1和(271.3±94.9)μg.h.L-1,受试制剂的苯磺酸氨氯地平相对生物利用度为(97.41±6.04)%;单剂口服受试和参比制剂后的贝那普利主要药动学参数Cmax分别为(136.6±66.1)μg.L-1和(143.3±50.9)μg.L-1,tmax分别为(0.6±0.2)h和(0.6±0.2)h,AUC0-t分别为(139.3±54.0)μg.h.L-1和(137.8±47.2)μg.h.L-1,受试制剂的贝那普利相对生物利用度为(100.8±7.55)%;单剂口服受试和参比制剂后的贝那普利拉主要药动学参数Cmax分别为(166.1±51.0)μg.L-1和(171.3±67.9)μg.L-1,tmax分别为(1.8±0.4)h和(1.6±0.3)h,AUC0-t分别为(874.6±322.7)μg.h.L-1和(832.5±354.1)μg.h.L-1。结论:复方苯磺酸氨氯地平/盐酸贝那普利受试制剂和参比制剂具有生物等效性。
OBJECTIVE To study the bioequivalence of amlodipine besylate/benazepril hydrochloride combination tablets in healthy suhjects. METHODS A single oral dose of 10 mg amlodipine besylate/20 mg benazepril hydrochloride test and reference formulation was administrated to 2（1 healthy male volunteers in a randomized crossover study. The concentrations of amlodipine besylate, benazepril and benazeprilat in serum were determined by LC MS/MS. The pharmacokinetic parameters and bioequivalence were calculated with DAS 2. 0 program. RESULTS The main pharmacokinetic parameters of test and reference preparation for amlodipine besylate were as follows： Cmax were （6.6±1.9）μg·L^-1 and （7.5±2.3）μg·L^-1 ; tmax were （6. 2 ± 1.4）h and （5.7 ±1.2）h; AUC0-t were （264.2±90.5）μg·h·L^-1 and （271.3±94.9）μg·h·L^-1 , respectively. The relative bioavailability of amlodipine besylate was （97. 41 ± 6.04）%. These pharmacokinetic parameters of test and reference preparation for benazepril hydrochloride were as follows： Cmax were （136.6±66.1）μg·L^-1 and （143.3±50.9）μg·L^-1; tmax were （0. 6 ± 0. 2） h and （0. 6±0. 2） h; AUC0-t were （139.3±54.0）μg·h·L^-1 and （137.8±47.2）μg·h·L^-1, respectively, and the relative bioavailability of benazepril hydrochloride was （100. 8 ± 7. 55）%, while the main pharmacokinetic parameters of test and reference preparation for benazeprilat were as follows： Cmax were （166.1±51.0）μg·L^-1 and （171.3±67.9）μg·L^-1; tmax were （1.8± 0. 4） h and （ 1.6 ±0.3） h ; AUC0-t were （874.6±322.7）μg·L^-1 and （832.5±354.1）μg·L^-1, respectively. CONCLUSION The results of the statistic analysis showed that these two formulations were bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第4期286-291,共6页
Chinese Journal of Hospital Pharmacy
