劳拉西泮注射液在中国人体内的药动学

目的:研究劳拉西泮注射液在中国健康人体内的药动学。方法:9名健康志愿者单剂肌内注射劳拉西泮4mg后,HPLC法测定血药浓度,所得血药浓度-时间数据采用3P97软件处理。结果:本品药-时曲线符合一房室开放模型。在确定的色谱分离条件下,血浆内源性杂质对样品测定无干扰,在3.125~100μg·L-1范围内样品峰面积与内标峰面积之比与血药浓度之间呈良好的线性关系(γ=0.9993)。人体药动学参数:tmax为(2.8±s0.8)h,cmax为(56±19)μg·L-1,t12ke为(17±3)h,t12ka为(1.0±0.8)h,V/F为(78±19)L,Cl/F为(3.3±1.1)L·h-1,AUC0~60为(1251±438)μg·h·L-1,AUC0~∞为(1383±489)μg·h·L-1。结论:本法操作简便,定量准确可靠,适用于劳拉西泮的人体药动学研究。

Pharmacokinetics of lorazepam injection in Chinese healthy volunteers

AIM:To study pharmacokinetics of lorazepam injection in healthy Chin ese volunteers. METHODS: The lorazepam concentrations in 9 serum plasma were de t ermined by HPLC after a single intramuscular dose(4mg) of the lorazepam injectio n, and then followed by 3P97 software processing. RESULTS: The concentration-tim e curves of the formulation fitted to one-compartment open model. Under the con f ormed chromatographic seperation condition, the intrinsic impurity in plasma did not interfere with determination of the sample tests. There was good linear re lationships between peak area ratio of lorazepam to internal standard and c( γ=0 .999 3) within the range of 3.125-100 μg·L -1 . The human pharmacokinetic param eters as follow:t_ max was (2.8±s 0.8) h, c_ max was (56±19) μg ·L -1 , t__ 12ke was (17±3 )h, t__ 12ka was (1.0± 0.8) h, V/F was (78±19 ) L, Cl/F was ( 3.3 ±1.1) L·h - 1 , AUC_ 0-60 was (1 251±438) μg·h·L -1 , AUC_ 0-∞ was (1 383±489) μg·h· L -1 , respectively. CONCLUSI ON: This RP-HPLC method is simple, accurate, reliable and suitable for the phar macokinetic study of lorazepam injection.