苯磺酸氨氯地平/阿托伐他汀钙片在健康人体的药代动力学

目的研究苯磺酸氨氯地平/阿托伐他汀钙片在中国健康人体的药代动力学。方法用随机、开放的拉丁方试验设计,12名健康受试者入选,男女各半,随机交叉单剂量口服苯磺酸氨氯地平/阿托伐他汀钙片、苯磺酸氨氯地平片、阿托伐他汀钙片。用LC-MS/MS测定2种成分的血药浓度,用DAS 2.1软件计算药代动力学参数。结果单次口服苯磺酸氨氯地平/阿托伐他汀钙片与苯磺酸氨氯地平片、阿托伐他汀钙片后药代动力学参数分别如下:t1/2为(46.11±11.05),(7.64±4.23)与(42.75±10.48),(8.42±4.24)h;Tmax为(8.67±3.11),(0.54±0.23)与(6.00±1.71),(1.13±1.55)h;Cmax为(4.13±1.86),(5.19±2.38)与(4.63±1.79),(3.46±2.23)ng.mL-1;AUC0-t为(200.25±91.89),(19.06±6.39)与(210.55±99.58),(19.26±6.55)ng.h.mL-1。结论苯磺酸氨氯地平与阿托伐他汀钙制成复方制剂,对阿托伐他汀的药代动力学无明显影响,氨氯地平的吸收速度略有加快。

Pharmacokinetics of amlodipine besylate/ atorvastatin calcium combination tablet in healthy volunteers

Objective To study the pharmacokinetics of combination tablet containing amlodipine besylate and atorvastatin calcium in healthy volunteers.Methods According to the Latin square design,each volunteer was orally given the combination of amlodipine besylate and atorvastatin calcium,amlodipine besylate and atorvastatin calcium tablets.The plasma concentrations were measured by a fully validated LC-MS/MS method.The pharmacokinetic parameters were calculated by DAS 2.1 software.Results The main pharmacokinetic parameters after a single oral amlodipine besylate/atorvastatin calcium combination tablets and administration of amlodipine besylate,atorvastatin calcium as follow: t1/2were(46.11±11.05),(7.64±4.23)and(42.75±10.48),(8.42±4.24)h;Tmax were(8.67±3.11),(0.54±0.23) and(6.00±1.71),(1.13±1.55)h;Cmax were(4.13±1.86),(5.19±2.38)and(4.63±1.79),(3.46±2.23)ng·mL-1;AUC0-t were(200.25±91.89),(19.06±6.39)and(210.55±99.58),(19.26±6.55) ng·h·mL-1.Conclusion After making into a compound preparation,the pharmacokinetic parameters of atorvastatin have no sex statistical differences,while the amlodipine absorption rate of compound preparation was higher than that of single preparation.