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本文进行了两组不同剂量的阿芬太尼在14例手术病人中药代动力学研究。7例一次性iv 80μg·kg~(-1)阿芬太尼,另7例一次性iv 40μg·kg~(-1)。用RIA方法测定0-8 h阿芬太尼的血浆浓度和0-48 h尿中的回收率。研究表明:阿芬太尼在两组病人体内的药代动力学过程均为3室模型。阿芬太尼的初级消除很快,给药后30 min内90％的原型药被消除。病人血浆浓度未发现2次上升现象。二者药-时曲线接近平行,说明阿芬太尼的代谢过程为1级消除。两组阿芬太尼的药代动力学数据经t检验无显著差异(P>0.05)。阿芬太尼的快、慢分布相和消除相的半衰期t_(1/2)π,t_(1/2)α和t_(1/2)β分别为0.71 min±s 0.37 min,11.66 min±s 3.46 min和86.12 min±s 19.15 min;平均总体和中心室的分布容积Vd、Vc分别为34.22L±s 8.27L和4.23L±s 1.72L;平均总体清除率Cl为0.29 L·min~(-1)±s 0.08L·min~(-1)。另外,k_(12)/k_(21)为1.5,k_(13)/k_(31)为3.5,k_(10)大于k_(31)。用药后48 h以内,40μg·kg~(-1)组和80μg·kg~(-1)组的病人尿中排出的原形阿芬太尼分别占总给药量的0.68％±s 0.72％和0.66％±s 0.54％。其肾清除率分别为0.0016 L·min~(-1)±s 0.0011 L·min~(-1)和0.0021 L·min~(-1)±s 0.0015 L·min~(-1)。
In this paper, two groups of different doses of alfentanil in 14 cases of surgical patients pharmacokinetic study. 7 cases were given iv 80μg · kg -1 alfentanil, and the other 7 cases were iv iv 40μg · kg -1. The plasma concentration of alfentanil 0-8 h and the recovery rate in 0-48 h urine were determined by RIA method. Studies have shown that the pharmacokinetics of alfentanil in both groups is a 3-compartment model. The primary elimination of alfentanil is rapid and 90% of the prototype drug is eliminated within 30 min of administration. Patient plasma concentration did not find 2 increases. The two drugs - time curve close to parallel, indicating that the metabolic process of alfentanil 1 level elimination. Pharmacokinetic data of two groups of alfentanil by t test showed no significant difference (P> 0.05). The half-lives t 1/2, t 1/2 and t 1/2 of alfentanil were 0.71 min ± s 0.37 min and 11.66 min ±, respectively s 3.46 min and 86.12 min ± s 19.15 min, respectively; mean volume and center ventricular volume distribution Vd and Vc were 34.22L ± s 8.27L and 4.23L ± s 1.72L respectively; mean overall clearance rate Cl was 0.29L · min ~ ( -1) ± s 0.08L · min ~ (-1). In addition, k_ (12) / k_ (21) is 1.5, k_ (13) / k_ (31) is 3.5, and k_ (10) is greater than k_ (31). Within 48 h after treatment, the original form of alfentanil excreted in the urine of 40 μg · kg -1 group and 80 μg · kg -1 group respectively accounted for 0.68% ± 0.72% of the total dose and 0.66% ± s 0.54%. The renal clearance rates were 0.0016 L · min -1 s 0.0011 L · min -1 and 0.0021 L · min -1 s 0.0015 L · min -1, respectively.