摘要
目的:研究健康受试者接受单剂量和多剂量注射国产盐酸纳美芬后的人体药代动力学。方法:30名志愿者按照随机原则分为3组,每组分别静脉推注0.5、1、2mg盐酸纳美芬注射液,采用LC-MS/MS以纳络酮为内标测定其血浆和尿药物浓度。用3P87软件进行数据处理,求出药代动力学参数。结果:其Cmax分别为(1.74±0.48)μg/L、(4.17±1.08)μg/L、(7.88±2.89)μg/L,t1/2β分别为(12.83±3.98)h、(12.6±6.4)h、(10.58±3.74)h,V分别为(3.45±0.16)L/kg、(4.11±0.0716)L/kg)、(4.25±0.56)L/kg;CL分别为(0.81±0.11)L(/h·kg)、(0.85±0.15)L(/h·kg)、(0.87±0.11)L/(h·kg);AUC0-∞分别为(21.62±9.34)(ng/L)*h、(24.89±8.52)(ng/L)*h、(35±11.2)ng/L)*h;尿药累计排泄率分别为(78±21)%、(71±29)%、(78±19)%。结论:国产注射用盐酸纳美芬在健康人体内的药代动力学符合二房室模型特征。在静脉推注0.5～2.0mg剂量范围内药物体内过程呈线性动力学特征。
Objective：To study the phamacokinetics of Nalmefene hydrochloride. Methods：30 healthy Chinese volunteers were assigned to 3 groups according to randomized design, and each group were given respectively a single intravenous administration dose of 0.5 mg, 1mg and 2mg of Nalmefene hydrochloride. The electrospray ionization positive selected reaction monitoring detections for Nalmefene hydrochloride and allyln-oroxymorphone （the internal standard） in the plasma and in the urine were used. The pharmaceutical parameters were calculated by 3P87 software. Results： The limit of the detection for Nalmefene hydrochloride was 0.0008 ng/ml in plasma and 0.0003 ng/ml in urine. There were good linear relationship range from 0.04 to 625ng/ml in plasma and 0.2 to 625 ng/ml in the urine. The variation coefficient in day and days, and the recoveries fitted the clinical pharmacokinetic study requirements. After a single intravenous administration of 0.5 mg,1mg, and 2mg of Na-lmefene hydrochloride, the obtained pharmacokinetic parameters were respectively as follows：Cmax were（1.74±0.48）μg/L,（4.17±1.08） μg/L,（7.88±2.89） μg/L;t1/2β were（12.83±3.98） h,（12.6±6.4） h, （10.58±3.74） h;V were （3.45±0.16） L/kg;（4.11±0.0716）L/kg、（4.25±0.56）L/kg;CL were （0.81±0.11） L/（h·kg）, （0.85±0.15）L/（h·kg）, （0.87±0.11） L/（h·kg）;AUC0-∞ were （21.62±9.34） （ng/L）＊h,（24.89±8.52） （ng/L）＊h, （35±11.2） ng/L）＊h;the urine accumulatived exc-retory rate were （78±21）%,（71±29）%,（78±19）%. Conclusion： The determination method for Nalmefene hydro-chloride in the plasma and in the urine by the electrosprayionization positive selected reaction monitoring detections is exclusive, accurate, sensitive and suitable. Pharmacokinetic characteristics in 3 groups of human treated with intravenous administration were described by a two-compartment model. The pharmaceutical characteristics of doxycycline hydrochloride in human body were linear in
出处
《重庆医科大学学报》
CAS
CSCD
北大核心
2009年第9期1250-1253,共4页
Journal of Chongqing Medical University
关键词
盐酸纳美芬
药动学
液相色谱-串联质谱法
光谱法
电喷雾电离
Nalmefene hydrochloride Pharmacokinetics HPLC -MS -MS Spectroscopy Elaectrospray ionization（ESI）
