滞留时间法评价吡罗昔康等五种药物的体外经皮渗透试验  

EVALUATION OF THE PERCUTANEOUS PERMEATION OF FIVE KINDS OF MEDICINES BY LAG TIME METHODS

作　　者：齐瑗晶[1] 薛克亮[1] 唐纯青[2] 李惠金[1] 于盛海[1] 孟晓东[1] 

机构地区：[1]山东省医学科学院药物研究所 [2]济南市第五人民医院

出　　处：《山东医科大学学报》2001年第6期565-567,共3页Acta Academiae Medicinae Shandong

摘　　要：目的 :用滞留时间法验证从渗透试验中所得的五种药物的D和Km等参数的可靠性。方法 :将吡罗昔康、甲巯咪唑、布洛芬、氢化可的松、盐酸氯丙嗪五种药物经鼠皮及新西兰家兔皮肤的体外经皮渗透数据 ,用滞时间法计算出稳态通量 (Jss)、滞留时间 (Tlag)、扩散系数 (D)和皮肤 /供体分配系数 (Km )等参数。用一基于Fick’s扩散定律的公式 ,通过扩散系数D和皮肤 /供体相分配系数 (Km)可再生整个渗透曲线 (包括稳态前和稳态 )。用观测数据作为自变量 ,经直线回归计算出观测数据和再生曲线的拟合度。结果 :在该试验中 ,除氢化可的松外的四种药物的R2 值均大于 0 .99,所得的D与Km准确。结论 :氢化可的松的试验持续时间小于 3×Tlag ,没有达到稳态 。Objective:To evaluate the permeation of five kinds of medicines using lag time method.Methods:Piroxican,Methimazole,Hydrocortisone,Ibuprofen,and Chlorpromazine were studied across NZWR skin and Kunming mouse skin.The resulted permeation profile for each individual drug was analyzed by the lag time method to estimate parameters such as the steady state flux(Jss),lag time (Tlag),skin/donor phase partition coefficient(Km).The diffusion coefficent(D) and skin/donor phase partition coefficient(Km) were used to regenerate the entire permeation profile(pre steady states and steady states) using an equation based on Fick's laws of diffusion.The goodness of fit was calculated through observed date as the independent variables.Results:R 2 of all drugs except Hydrocortisone was greater than 0.99.Conclusion:The experimental duration of Hydrocortisone was less than three times Tlag and steady state isn't achieved, which may result in inaccurate estimates of D and Km.

关 键 词：经皮渗透 滞留时间法 吡罗昔康 甲巯咪唑 布洛芬 氢化可的松 盐酸氯丙嗪 

分 类 号：R969.1[医药卫生—药理学]