几种增渗剂对吡喹酮经离体鼠皮渗透性的影响

本文利用水平式Ｖａｌｉａ－Ｃｈｉｅｎ扩散池考察了过饱和生理盐水溶液中药物经离体鼠皮的渗透性及不同增渗剂的促渗作用，同时考察了吡喹酮体外经活性表皮的渗透性，结果表明吡喹酮经离体鼠皮及其活性表皮的渗透系数分别为４．７３×１０~（－６）ｃｍ／ｓ和２．９２５×１０~（－５）ｃｍ／ｓ，稳态流量分别为１．３１３×１０~（－３）μｇ／ｃｍ~２．ｓ和８．１１１×１０~（－３）μｇ／ｃｍ~２·ｓ，滞后时间分别为１．５２５ｈ和０．８６４ｈ，对皮肤经增渗剂处理前后，吡喹酮体外经皮的渗透实验结果表明月桂氮酮、泊洛沙姆１８８和油酸对其经皮渗透均有一定的促进作用，其中３％月桂氮酮的促渗作用最为显著，而Ｎ－乙基－２－吡咯烷酮则无明显增渗作用。此外，测定了吡喹酮在正辛醇／水、全皮／水和角质层／水的分配系数，结果表明药物的亲脂性极强。

EFFECTS OF PENETRATION ENHANCERS ON THE PERMEATION OF PRAZIQUANTEL THROUGH EXCISED MOUSE SKIN

In this study,the basic permeation of praziquantel(PZQ) in normal saline through excised mouse skin in vitro was investigated using Valia-Chien diffusion cell, and the basic permeation parameters were obtained.The permeation coefficient was 4.73×10-6cm/s,the steady state flux was 1.313×10-3μg/cm2·s,and the lag time was 1.525h.At the same time,the pemeation of PZQ through viable epidermis was studied.The results showed that the permeation coefficient increased to 2.925×10-5 cm/s,the steaty-state flux increased to 8.111×10-3μg/cm2·s,and the lag time decreased to 0.864h.The results of the permeation coefficient of PZQ through skin with pretreatment or without in vitro suggested that Azone,poloxamer 188 and oleic acid could enhance the percutaneous penetration to some extent where the enhancement of 3% Azone was significant and N-ethyl-2-pyrrolidone had no distinct enhancement.Besides, the n-octanol/water, skin/water and stratum corneum/water partition coefficients of the drug were determined and the results suggested that the drug was highly hydrophobic.