盐酸纳美芬注射液在健康人体的药动学研究

 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。

Pharmacokinetics of Naimefene Hydrochloride Injection in Healthy Volunteers

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:t_1/2was(12.01±2.20)h,AUC_0-48 was(30.29±9.84)μg·h·L^-1,AUC_0-∞ 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.