摘要
目的 探讨健康人单用美多洛尔 (Met)、卡托普利 (Cap)及合用两药时体内的药代动力学过程并进行比较 ,考察两药同时服用后其药代动力学特性和相互作用。方法 对 12名健康志愿受试者进行随机交叉实验 ,分 3组 ,每组 4人 ,每组先后分别给予Met 5 0mg ,Cap 5 0mg,Met+Cap各 5 0mg。采用HPLC测定血药浓度。用 3P87药代动力学程序对受试者药 时数据进行处理 ,拟合房室模型 ,求算药代动力学参数。结果 美多洛尔的Ke值较单用时明显减少 (P <0 .0 1) ;而t1/2K,cmax和AUC则明显增大。卡托普利在单用及合用时药代动力学参数无明显变化。结论 两药合用后美多洛尔的肝脏代谢受到抑制。提示临床联合用药时应监测患者体内美多洛尔血药浓度 ,避免不良反应发生。
OBJECTIVE To investigate the pharmacokinetic processes in 12 healthy volunteers after taking a single oral dose of metoprolol 50 mg,captopril 50 mg and both of them respectively,and to examine the pharmacokinetic characteristics and interaction when the two drugs being given simultaneously.METHODS 12 healthy volunteers were divided into three groups.A single dose of metoprolol 50 mg,captopril 50 mg and both of them were given successively in an open randomized crossover study.HPLC method was used to determine the concentrations of two drugs in plasma.The plasma concentration time values was fitted to 3P87 programe to get the pharmacokinetic parameters.RESULTS The pharmacokinetic parameters ke of metoprolol was decreased while t 1/2k , c max , AUC were increased significantly.The parameters of captopril had no change when the two drugs being taken simultaneously.CONCLUSION The blood concentration of metoprolol is suggested to be monitored in averting harmful reactions because captopril may inhibit the metabolism of metoprolol in liver.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2001年第2期111-113,共3页
Chinese Pharmaceutical Journal
