| 摘要: |
| 目的:探讨氨氯地平与厄贝沙坦联用时有无显著的药动学相互作用.方法:采用自身对照、随机交叉试验方法,将比格犬分为3组,每组2条,分别按试验周期服用苯磺酸氨氯地平对照药物(给药剂量以氨氯地平计5 mg)、厄贝沙坦对照药物(给药剂量为250 mg)和厄贝沙坦氨氯地平复方试验药物(给药剂量为以氨氯地平计5 mg,厄贝沙坦250 mg).采用HPLCESI-MS/MS和HPLC荧光法分别测定不同时间点氨氯地平和厄贝沙坦的血药浓度,计算药动学参数.结果:单用氨氯地平cmax为(267.63±38.49)ng/ml,AUC0～∞为(5 648.71±871.68)ng·h/ml,联用氨氯地平cmax为(267.43±37.97)ng/ml,AUC0～∞为(5 751.60±924.49)ng·h/ml;单用厄贝沙坦cmax为(2 623.56±198.65)ng/ml,AUC0～∞为(10 327.53±1 522.58)ng·h/ml,联用厄贝沙坦cmax为(2 345.61±42.32)ng/ml,AUC0～∞为(10 217.12±1 239.13)ng·h/ml.故与两种药物分别使用的情况相比,联用时的cmax、AUC并不存在显著性差异.结论:氨氯地平与厄贝沙坦联用不存在显著的药动学相互作用. |
| 关键词: 氨氯地平、厄贝沙坦、药物疗法,联合、药动学 |
| DOI：10.3724/SP.J.1008.2006.00763 |
| 投稿时间：2006-04-10修订日期：2006-05-30 |
| 基金项目:上海市药物(中药)代谢产物研究重点实验室资助课题(036505016). |
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| Pharmacokinetic interaction between amlodipine and irbesartan in beagle dogs |
| ZHONG Xiang-ping,CHEN Yi,GAO Shou-hong,FAN Guo-rong |
| (上海市药物代谢产物研究重点实验室,第二军医大学药学院药物分析学教研室,上海,200433) |
| Abstract: |
| Objective： To investigate whether there is pharmacokinetic interaction between amlodipine and irbesarta when they are administered together into beagle dogs. Methods： Six healthy adult beagle dogs were evenly divided into 3 groups according to a self-controlled randomized 2-way crossover design. Animals in 3 groups were given a single oral dose of 5 mg amlodipine powder, 250 mg irbesartan powder and compound powder of amlodipine and irbesartan （containing 5 mg amlodipine and 250 mg irbesartan）, respectively. The concentrations of amlodipine and irbesartan in beagle dog plasma were determined at specified time points by HPLC-ESI-MS/MS and HPLC-Fluorescence method, respectively; the pharmacokinetic parameters were calculated subsequently. Results： Cm,xand AUC0-∞ of amlodipine were （267.63±38.49） ng/ml and （5 648.71±871.68） ng · h/ml when administered alone and were （267.43±37.97） ng/ml and （5 751.60±924.49） ng · h/ml when combined with irbesartan,respectively. Cmaxand AUC0-∞ of irbesartan were （2 623.56±198.65） ng/ml and （10 327.53±1 522.58） ng · h/ml when administered alone and were （2 345.61±42.32） ng/ml and （10 217.12±1 239.13） ng · h/ml when combined with amlodipine,respectively. There was no significant difference in cmax and AUC of the 2 drugs when they were used alone or jointly. Conclusion： There is no obvious pharmacokinetic interaction between amlodipine and irbesarta when they are administered jointly into beagle dogs. |
| Key words: amlodipine irbesartan drug therapy,combination pharmacokinetic |
