水杨酸二乙胺乳膏(柳胺霜)人体透皮吸收的药动学研究
PHARMACOKINETIC STUDIES ON THE PERCUTANEOUS ABSORPTION OF DIETHYLAMINE SALICYLATE CREAM FROM HUMAN SKIN
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摘要: 按非线性最小二乘法,经 TRS—80Ⅱ型微电子计算机上自装的 NLFT-ZHU 程序系列,对实验数据进行药动学处理的结果显示:水杨酸二乙胺(Diethyl-amine Salicylate—DEAS)乳膏中药物的透皮吸收为带有较长时滞的零级速度过程。吸收入血所需时间(时滞)为5~8小时,零级吸收速度为25.46±10.70mg/h,一级消除速度常数为0.3ˉ49±0.1214h~(-1)。由电子计算机作的单剂量与多剂量给药后血药水平经时过程数据模拟结果表明,单剂量按最大可涂布剂量3.5g 或多剂量按每天2次、每次1g 给药后,其最大血浓均在2~6μg/ml 左右,远低于水杨酸发挥全身作用的最低有效血药水平(50μg/ml)。可见该药主要起局部的治疗作用。Abstract: Diethylamine salicylate (DEAS) cream was spread with rubbing on the inner part of two arms. The total amount of salicylic acid and its metabolite in urine were determined with spectrophotometry. Based on the non-linear least square method, the experimental data were treated using NLFTZHU program fixed on TRS—80 Ⅱ microcomputer system. The pharmacokinetic analysis showed that the absorption rate of DEAS cream is normal zero order with the absorption constant of 25.45±10.70 mg/h(time lag is 5—8b), and the first order elimination rate constant was 0.375±0.124h^-1. The plasma levels, after a large single dose (3.5g) and a multiple dose administrations were computer-simulated. The maximum plasma levels range from 2 to 6 μg/ml. They are remarkable lower than minimum effective plasma level of salicylic acid (50μg/ml). Diethylamine salicylate cream seems to be only responsible for a topical therapeuic effect.