左西孟旦注射液在中国健康人体的药代动力学  

Pharmacokinetics and safety of levosimendan injection in Chinese healthy volunteers

作　　者：李晓光[1] 张妍[1] 翟所迪[1] 佘飞[2] 赵荣生[1] 杨丽[1] 

机构地区：[1]北京大学第三医院药剂科,北京100191 [2]北京大学第三医院心血管内科,北京100191

出　　处：《中国临床药理学杂志》2012年第2期110-114,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究左西孟旦注射液在中国健康人体的药代动力学。方法 30名健康男性受试者,采用随机、开放、单剂量试验设计,分别单次静脉注射左西孟旦注射液1.0,2.0,3.0 mg。用HPLC法测定血药浓度;用WinNonlin软件计算药代动力学参数。结果 3个剂量左西孟旦的主要药代动力学参数:Cmax分别为(109.24±14.52),(201.38±38.94)和(317.65±45.75)ng.mL-1;Tmax分别为(11.5±2.4),(11.5±3.4)和(11.9±2.6)min;t1/2分别为(0.68±0.10),(0.60±0.08)和(0.80±0.08)h;AUC0-t分别为(81.38±12.64),(143.13±29.63)和(289.86±48.57)μg.h.L-1。结论 1～3 mg给药剂量范围内,左西孟旦均具有线性动力学特征。Objective To investigate the pharmacokinetics and safety of levosimendan injection in Chinese healthy volunteers.Methods Thirty healthy male volunteers were enrolled and divided into three groups（10 volunteers per group）and were administrated a single dose of levosimendan injection intravenously（1 mg or 2 mg or 3 mg）.The concentrations of levosimendan in plasma were determined by HPLC and WinNolin was used to calculate the pharmacokinetic parameters.Results The main pharmacokinetic parameters of three test groups were as follows： Cmax were（109.24±14.52）,（201.38±38.94）and（317.65±45.75）ng·mL-1 respectively;Tmax were（11.5±2.4）,（11.5±3.4）and（11.9±2.6）min,t1/2 were（0.68±0.10）,（0.60±0.08）and（0.80±0.08）h respectively;AUC0-t were（81.38±12.64）,（143.13±29.63）and（289.86±48.57）μg·h·L-1 respectively.Conclusion After intravenous administration of 1,2,3 mg levosimendan injections,pharmacokinetics behaviors showed good linear relationship and safety were acceptable.

关 键 词：左西孟旦 药代动力学 高效液相色谱法 

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