进食或空腹口服国产氯沙坦钾片对健康志愿者药动学及血压的影响研究  

Influence of Oral Dose of Losartan in Fasting and Postprandial State on Pharmacokinetics and Blood Pressure in Healthy Volunteers

作　　者：陈欣[1] 王茜[1] 赵立波[1] 李玉珍[1] 方翼[1] 

机构地区：[1]北京大学人民医院药剂科,北京市100044

出　　处：《中国药房》2011年第22期2059-2060,共2页China Pharmacy

摘　　要：目的:研究进食或空腹口服国产氯沙坦钾片对健康志愿者药动学及血压的影响。方法:选取10名男性健康志愿者,按两周期交叉自身对照试验设计,随机分为进食组与空腹组各5名,口服氯沙坦钾片50mg,清洗期1周后交叉试验。记录给药前和给药后1、4、8h时血压,并应用高效液相色谱串联质谱电喷雾(HPLC-MS/MS)法检测氯沙坦和代谢产物E-3174的血药浓度,采用DAS2.1.1软件计算药动学参数并以SASv8.02软件统计分析血压变化。结果:进食对各主要药动学参数无影响。空腹组血压下降较快,幅度较大,舒张压下降更为显著(P<0.05)。结论:进食或空腹对口服氯沙坦的代谢无影响,但可能导致降压效果的差异。OBJECTIVE： To investigate the influence of oral dose of losartan in fasting and postprandial state on pharmacokinetics and blood pressure in healthy volunteers. METHODS： 10 healthy male volunteers were randomly divided into postprandial state group and fasting state group with 5 volunteers in each group in double cross-over design. Both groups were treated with oral dose of 50 mg Losartan tablets. Cross experiment was conducted 1 week after wash-out period. Blood pressures of patients were recorded before medication and 1 h, 4 h and 8 h after medication. Plasma concentrations of losartan and E-3174 were determined by HPLC-MS/MS. Pharmacokinetic parameters were calculated by DAS 2.1.1 software and the change of blood pressure was analyzed by SAS v 8.02 software. RESULTS： Postprandial state had no effect on main pharmacokinetic parameters. In fasting state group, blood pressure decreased significantly, especially diastolic pressure（P0.05）. CONCLUSION：Fasting and postprandial states have no influence on metabolism of losartan, but may result in diversity in effect and degree of lowering blood pressure.

关 键 词：氯沙坦 E-3174 空腹 进食 药动学 血压 高效液相色谱串联质谱电喷雾法 

分 类 号：R969.1[医药卫生—药理学] R972.4[医药卫生—药学]