盐酸纳美芬注射液在健康人体的药动学研究  

Pharmacokinetics of Nalmefene Hydrochloride Injection in Healthy Volunteers

作　　者：温预关[1] 喻凌寒[2] 杨梦心[1] 马崔[1] 熊令辉[1] 胡号应[1] 

机构地区：[1]广州市脑科医院国家药品临床研究基地,广州510370 [2]广东省化学危害应急检测技术重点实验室,中国广州分析测试中心,广州510070

出　　处：《中国药学杂志》2008年第13期1015-1018,共4页Chinese Pharmaceutical Journal

基　　金：广州市医药卫生科技立项项目(2007-YB-106);广东省医院药学研究基金立项(2008B001);广东省医学科学技术研究基金立项(WSTJJ20071214110108197210249714)

摘　　要：目的建立快速、灵敏的纳美芬人体内血药浓度的液相色谱-质谱测定法,并对静脉注射盐酸纳美芬注射液后在人体内的药动学过程进行研究。方法12名健康志愿者单剂量静脉给药2 mg后,分别于给药前和给药后0.083,0.25,0.5,1,2,3,4,6,8,10,12,24,36及48 h采集血样。用高效液相色谱-质谱法测定血浆中纳美芬的浓度,并采用PKS药动学程序对试验数据进行处理,求算有关药动学参数。结果单剂量静脉给药盐酸纳美芬注射液2 mg后,其药-时曲线拟合符合二室模型,t_(1/2),AUC_(0-48),AUC_(0-∞)分别为(12.01±2.20)h,(30.29±9.84)μg·h·L^(-1),(32.23±9.94)μg·h·L^(-1)。结论试验建立的纳美芬人体内血药浓度测定方法灵敏、简便、可靠;盐酸纳美芬注射液单剂量给药后在中国健康人体内耐受良好,人体内的药动学行为与国外文献报道基本一致。OBJECTIVE To develop a rapid and sensitive HPLC-MS method for the analysis of namefene in human plasma, and study the pharmacokinetic characteristics of namefene hydrochloride injection after a single intravenous dose of 2 mg in healthy volunteers. METHODS A single intravenous dose of 2 mg namefene hydrochloride injection was given to 12 healthy volunteers. Blood samples were taken for detecting plasma concentration before dosing and at 0. 083, 0. 25, 0. 5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 h after a single intravenous administration of 2 mg namefene. A HPLC-MS method was used to assay the namefene concentration in plasma. The pharmacokinetic parameters were evaluated with PKS program. RESULTS The namefene concentrations in plasma were fitted with a two-compartment model. The main pharmacokinetic parameters of namefene by intravenous adminisitration were as follows：t1/2 was（12.01±2.20）h, AUC0-48 was（30.29±9.84）μg·h·L^-1, AUC0-∞ was（32.23±9.94） μg·h·L^-1. CONCLUSION The analytical method appeared to be accurate, sensitive and convenient. Namefene hydrochloride injection was well tolerance in healthy Chinese volunteers after a single dose. The pharmacokinetic characteristics of namefene hydrochloride injection were similar to the publicated reports.

关 键 词：盐酸纳美芬注射液 药动学 高效液相色谱-质谱法 

分 类 号：R969[医药卫生—药理学]